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Showing drug card for Tretinoin (DB00755)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:47:58
Primary Accession Number DB00755
Secondary Accession Number
  • APRD00362
  • NUTR00051
Name Tretinoin
Drug Type
  • Approved
  • Investigational
  • Nutraceutical
  • Small Molecule
Description Tretinoin, also known as all-trans-retinoic acid (ATRA), is a naturally occurring derivative of vitamin A (retinol). Retinoids such as tretinoin are important regulators of cell reproduction, proliferation, and differentiation and are used to treat acne and photodamaged skin and to manage keratinization disorders such as ichthyosis and keratosis follicularis. Tretinoin also represents the class of anticancer drugs called differentiating agents and is used in the treatment of acute promyelocytic leukemia (APL).
Synonyms
  1. ATRA
  2. All Trans Retinoic Acid
  3. All Trans-Retinoic Acid
  4. Retionic Acid
  5. beta-Retinoic Acid
  6. tretinoin
Brand Names
  1. Aberel
  2. Accutane
  3. Airol
  4. Aknefug
  5. Aknoten
  6. Amnesteem
  7. Atra-IV
  8. Claravis
  9. Dermairol
  10. Eudyna
  11. Lsotretinoin
  12. Retisol-A
  13. Solage
  14. Sotret
  15. Stieva-A
  16. Stieva-a Forte
  17. Tri-Luma
  18. Vitinoin
Brand Mixtures Not Available
Chemical IUPAC Name 3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexenyl)nona-2,4,6,8-tetraenoic acid
Chemical Formula C20H28O2
Chemical Structure Structure
CAS Registry Number 302-79-4
InChI Identifier InChI=1/C20H28O2/c1-15(8-6-9-16(2)14-19(21)22)11-12-18-17(3)10-7-13-20(18,4)5/h6,8-9,11-12,14H,7,10,13H2,1-5H3,(H,21,22)/f/h21H
InChI Key SHGAZHPCJJPHSC-PKSOQXRJCZ
KEGG Drug D00094 Link Image
KEGG Compound C00777 Link Image
PubChem Compound 5538 Link Image
PubChem Substance 7847162 Link Image
ChEBI ID 15367 Link Image
PharmGKB ID PA451746 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 02243914 Link Image
RxList Link http://www.rxlist.com/cgi/generic/tretinoin.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Tretinoin Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Matsui et al.; J.Vitaminol.; 4; 190, 192(1958)
Average Molecular Weight 300.4351
Monoisotopic Molecular Weight 300.2089
State Solid
Melting Point 181 oC
Experimental Water Solubility <0.1 g/100 mL Source: PhysProp
Predicted Water Solubility 4.77e-03 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 4.2 Source: PhysProp
Predicted LogP 5.66 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -4.80 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point Not Available
Mass Spectrum Not Available
MOL File Show Link Image | Download Link Image
SDF File Show Link Image | Download Link Image
PDB File Show Link Image | Download Link Image
2D Structure
3D Structure
Experimental PDB ID 1CBR Link Image
Experimental PDB File Show
Experimental PDB Structure
Isomeric SMILES CC(\C=C\C1=C(C)CCCC1(C)C)=C/C=C/C(C)=C/C(O)=O
Canonical SMILES CC(C=CC1=C(C)CCCC1(C)C)=CC=CC(C)=CC(O)=O
Drug Category
  • Antineoplastic Agents
  • Cell Stimulants and Proliferants
  • Keratolytic Agents
ATC Codes
AHFS Codes
  • 84:16.00
  • 92:00.00
Indication For the the induction of remission in patients with acute promyelocytic leukemia (APL), French-American-British (FAB) classification M3 (including the M3 variant); For the topical treatment of acne vulgaris, flat warts and other skin conditions (psoriasis, ichthyosis congenita, icthyosis vulgaris, lamellar icthyosis, keratosis palmaris et plantaris, epidermolytic hyperkeratosis, senile comedones, senile keratosis, keratosis follicularis (Darier's disease), and basal cell carcinomas.); For palliative therapy to improve fine wrinkling, mottled hyperpigmentation, roughness associated with photodamage.
Pharmacology Tretinoin, also known as all-trans-retinoic acid (ATRA), is a naturally occurring derivative of vitamin A (retinol). Retinoids such as tretinoin are important regulators of cell reproduction, proliferation, and differentiation and are used to treat acne and photodamaged skin and to manage keratinization disorders such as ichthyosis and keratosis follicularis. Tretinoin also represents the class of anticancer drugs called differentiating agents and is used in the treatment of acute promyelocytic leukemia (APL).
Mechanism of Action Tretinoin binds to alpha, beta, and gamma retinoic acid receptors (RARs). RAR-alpha and RAR-beta have been associated with the development of acute promyelocytic leukemia and squamous cell cancers, respectively. RAR-gamma is associated with retinoid effects on mucocutaneous tissues and bone. Although the exact mechanism of action of tretinoin is unknown, current evidence suggests that the effectiveness of tretinoin in acne is due primarily to its ability to modify abnormal follicular keratinization. Comedones form in follicles with an excess of keratinized epithelial cells. Tretinoin promotes detachment of cornified cells and the enhanced shedding of corneocytes from the follicle. By increasing the mitotic activity of follicular epithelia, tretinoin also increases the turnover rate of thin, loosely-adherent corneocytes. Through these actions, the comedo contents are extruded and the formation of the microcomedo, the precursor lesion of acne vulgaris, is reduced. Tretinoin is not a cytolytic agent but instead induces cytodifferentiation and decreased proliferation of APL cells in culture and in vivo. When Tretinoin is given systemically to APL patients, tretinoin treatment produces an initial maturation of the primitive promyelocytes derived from the leukemic clone, followed by a repopulation of the bone marrow and peripheral blood by normal, polyclonal hematopoietic cells in patients achieving complete remission (CR). The exact mechanism of action of tretinoin in APL is unknown.
Absorption 1-31% (topical)
Toxicity Not Available
Protein Binding > 95%
Biotransformation Hepatic
Half Life 0.5-2 hours
Dosage Forms
Form Route
Capsule Oral
Cream Topical
Gel Topical
Liquid Topical
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Atazanavir The strong CYP2C8 inhibitor, Atazanavir, may decrease the metabolism and clearance of oral Tretinoin. Consider alternate therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Atazanavir is initiated, discontinued to dose changed.
Carbamazepine The strong CYP2C8 inducer, Carbamazepine, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Carbamazepine is initiated, discontinued or dose changed.
Celecoxib The moderate CYP2C8 inhibitor, Celecoxib, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Celecoxib is initiated, discontinued to dose changed.
Demeclocycline Demeclocycline may increase the adverse effects of oral Tretinoin. Increased risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Desogestrel Oral Tretinoin may decrease the effect of oral contraceptive, Desogestrel. An alternate form of contraception should be used during concomitant therapy.
Doxycycline Doxycycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Drospirenone Oral Tretinoin may decrease the effect of oral contraceptive, Drospirenone. An alternate form of contraception should be used during concomitant therapy.
Ethinyl Estradiol Oral Tretinoin may decrease the effect of the oral contraceptive, Ethinyl Estradiol. An alternate form of contraception should be used during concomitant therapy.
Ethynodiol Diacetate Oral Tretinoin may decrease the effect of oral contraceptive, Ethynodiol Diacetate. An alternate form of contraception should be used during concomitant therapy.
Etonogestrel Oral Tretinoin may decrease the effect of oral contraceptive, Etonogestrel. An alternate form of contraception should be used during concomitant therapy.
Felodipine The moderate CYP2C8 inhibitor, Felopidine, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Felopidine is initiated, discontinued to dose changed.
Fosphenytoin The strong CYP2C8 inducer, Fosphenytoin, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Fosphenytoin is initiated, discontinued or dose changed.
Gemfibrozil The strong CYP2C8 inhibitor, Gemfibrozil, may decrease the metabolism and clearance of oral Tretinoin. Consider alternate therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Gemfibrozil is initiated, discontinued to dose changed.
Irbesartan The moderate CYP2C8 inhibitor, Irbesartan, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Irbesartan is initiated, discontinued to dose changed.
Lapatinib The moderate CYP2C8 inhibitor, Lapatinib, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Lapatinib is initiated, discontinued to dose changed.
Levonorgestrel Oral Tretinoin may decrease the effect of oral contraceptive, Levonorgestrel. An alternate form of contraception should be used during concomitant therapy.
Losartan The moderate CYP2C8 inhibitor, Losartan, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Losartan is initiated, discontinued to dose changed.
Mestranol Oral Tretinoin may decrease the effect of oral contraceptive, Mestranol. An alternate form of contraception should be used during concomitant therapy.
Minocycline Minocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Natalizumab Oral tretinoin may increase the adverse/toxic effects of Natalizumab. Concurrent therapy should be avoided.
Nilotinib The moderate CYP2C8 inhibitor, Nilotinib, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Nilotinib is initiated, discontinued to dose changed.
Norethindrone Oral Tretinoin may decrease the effect of oral contraceptive, Norethindrone. An alternate form of contraception should be used during concomitant therapy.
Norgestimate Oral Tretinoin may decrease the effect of oral contraceptive, Norgestimate. An alternate form of contraception should be used during concomitant therapy.
Norgestrel Oral Tretinoin may decrease the effect of oral contraceptive, Norgestrel. An alternate form of contraception should be used during concomitant therapy.
Oxytetracycline Oxytetracycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Phenobarbital The strong CYP2C8 inducer, Phenobarbital, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Phenobarbital is initiated, discontinued or dose changed.
Phenytoin The strong CYP2C8 inducer, Phenytoin, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Phenytoin is initiated, discontinued or dose changed.
Pioglitazone The moderate CYP2C8 inhibitor, Pioglitazone, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Pioglitazone is initiated, discontinued to dose changed.
Primidone The strong CYP2C8 inducer, Primidone, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Primidone is initiated, discontinued or dose changed.
Quinine The moderate CYP2C8 inhibitor, Quinine, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Quinine is initiated, discontinued to dose changed.
Rabeprazole The moderate CYP2C8 inhibitor, Rabaprazole, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rabaprazole is initiated, discontinued to dose changed.
Rifampin The strong CYP2C8 inducer, Rifampin, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rifampin is initiated, discontinued or dose changed.
Rifapentine The strong CYP2C8 inducer, Rifapentine, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rifapentine is initiated, discontinued or dose changed.
Ritonavir The strong CYP2C8 inhibitor, Ritonavir, may decrease the metabolism and clearance of oral Tretinoin. Consider alternate therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Ritonavir is initiated, discontinued to dose changed.
Rosiglitazone The moderate CYP2C8 inhibitor, Rosiglitazone, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rosiglitazone is initiated, discontinued to dose changed.
Secobarbital The strong CYP2C8 inducer, Secobarbital, may increase the metabolism and clearance of oral Tretinoin. Consider alternate therapy to avoid failure of Tretinoin therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Secobarbital is initiated, discontinued or dose changed.
Sorafenib The strong CYP2C8 inhibitor, Sorafenib, may decrease the metabolism and clearance of oral Tretinoin. Consider alternate therapy or monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Sorafenib is initiated, discontinued to dose changed.
Tamoxifen The moderate CYP2C8 inhibitor, Tamoxifen, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Tamoxifen is initiated, discontinued to dose changed.
Tetracycline Demeclocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Tigecycline Demeclocycline may increase the adverse effects of oral Tretinoin. Increase risk of pseudotumour cerebri. Concurrent therapy should be avoided.
Trastuzumab Increased risk of leukopenia and anemia due to synergistic effects. Monitor for signs and symptoms of adverse events during concomitant therapy.
Trimethoprim The moderate CYP2C8 inhibitor, Trimethoprim, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Trimethoprim is initiated, discontinued to dose changed.
eltrombopag The moderate CYP2C8 inhibitor, Eltrombopag, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Eltrombopag is initiated, discontinued or dose changed.
Food Interactions Not Available
Pathways Not Available
General References
  1. Mao JT, Goldin JG, Dermand J, Ibrahim G, Brown MS, Emerick A, McNitt-Gray MF, Gjertson DW, Estrada F, Tashkin DP, Roth MD: A pilot study of all-trans-retinoic acid for the treatment of human emphysema. Am J Respir Crit Care Med. 2002 Mar 1;165(5):718-23. [PubMed Link Image]
  2. Roth MD, Connett JE, D'Armiento JM, Foronjy RF, Friedman PJ, Goldin JG, Louis TA, Mao JT, Muindi JR, O'Connor GT, Ramsdell JW, Ries AL, Scharf SM, Schluger NW, Sciurba FC, Skeans MA, Walter RE, Wendt CH, Wise RA: Feasibility of retinoids for the treatment of emphysema study. Chest. 2006 Nov;130(5):1334-45. [PubMed Link Image]
  3. Sanz MA: Treatment of acute promyelocytic leukemia. Hematology Am Soc Hematol Educ Program. 2006;:147-55. [PubMed Link Image]
  4. Castaigne S, Chomienne C, Daniel MT, Ballerini P, Berger R, Fenaux P, Degos L: All-trans retinoic acid as a differentiation therapy for acute promyelocytic leukemia. I. Clinical results. Blood. 1990 Nov 1;76(9):1704-9. [PubMed Link Image]
  5. Huang ME, Ye YC, Chen SR, Chai JR, Lu JX, Zhoa L, Gu LJ, Wang ZY: Use of all-trans retinoic acid in the treatment of acute promyelocytic leukemia. Blood. 1988 Aug;72(2):567-72. [PubMed Link Image]
  6. Drugs.com Link Image
  7. Wikipedia Link Image
  8. RxList Link Image
Organisms Affected
  • Humans and other mammals
Phase 1 Metabolizing Enzymes
  1. Cytochrome P450 2C8 (CYP2C8)
Targets
  1. Nuclear receptor 0B1
  2. Retinoic acid receptor RXR-beta
  3. Retinoic acid receptor gamma-1
  4. Retinoic acid receptor gamma-2
  5. Retinal dehydrogenase 2
  6. Retinal dehydrogenase 1
  7. Retinoic acid receptor responder protein 1
  8. Retinoic acid-induced protein 3
  9. Retinoic acid receptor RXR-gamma
Phase 1 Metabolizing Enzyme 1 [top]
Enzyme 1 Name Cytochrome P450 2C8 (CYP2C8)
Enzyme 1 Gene Name CYP2C8
Enzyme 1 SwissProt ID P10632 Link Image
Enzyme 1 SNPs SNPJam Report Link Image
Enzyme 1 Protein Sequence >sp|P10632|CP2C8_HUMAN Cytochrome P450 2C8 (EC 1.14.14.1) 
MEPFVVLVLCLSFMLLFSLWRQSCRRRKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKV
YGPVFTVYFGMNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRW
KEIRRFSLTTLRNFGMGKRSIEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICS
VVFQKRFDYKDQNFLTLMKRFNENFRILNSPWIQVCNNFPLLIDCFPGTHNKVLKNVALT
RSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKSEFNIENLVGTVADLFVAGTE
TTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDAVVHEIQRYSD
LVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFK
KSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLP
PSYQICFIPV
Drug Target 1 [top]
Target 1 ID 84
Target 1 Name Nuclear receptor 0B1
Target 1 Synonyms
  1. DSS-AHC critical region on the X chromosome protein 1
  2. Nuclear receptor DAX-1
Target 1 Gene Name NR0B1
Target 1 Protein Sequence >Nuclear receptor 0B1 
MAGENHQWQGSILYNMLMSAKQTRAAPEAPETRLVDQCWGCSCGDEPGVGREGLLGGRNV
ALLYRCCFCGKDHPRQGSILYSMLTSAKQTYAAPKAPEATLGPCWGCSCGSDPGVGRAGL
PGGRPVALLYRCCFCGEDHPRQGSILYSLLTSSKQTHVAPAAPEARPGGAWWDRSYFAQR
PGGKEALPGGRATALLYRCCFCGEDHPQQGSTLYCVPTSTNQAQAAPEERPRAPWWDTSS
GALRPVALKSPQVVCEAASAGLLKTLRFVKYLPCFQVLPLDQQLVLVRNCWASLLMLELA
QDRLQFETVEVSEPSMLQKILTTRRRETGGNEPLPVPTLQHHLAPPAEARKVPSASQVQA
IKCFLSKCWSLNISTKEYAYLKGTVLFNPDVPGLQCVKYIQGLQWGTQQILSEHTRMTHQ
GPHDRFIELNSTLFLLRFINANVIAELFFRPIIGTVSMDDMMLEMLCTKI
Target 1 Number of Residues 477
Target 1 Molecular Weight 51718
Target 1 Theoretical pI 8.12
Target 1 GO Classification
Function
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 1 General Function Involved in transcription factor activity
Target 1 Specific Function Receptor that may be a component of a cascade required for development of steroidogenic tissues. Acts as a dominant negative regulator of transcription mediated by the retinoic acid receptor
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • None
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 786532 Link Image
Target 1 UniProtKB/Swiss-Prot ID P51843 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name DAX1_HUMAN Link Image
Target 1 PDB ID Not Available
Target 1 Cellular Location
  • Nucleus
Target 1 Gene Sequence >1413 bp 
ATGGCGGGCGAGAACCACCAGTGGCAGGGCAGCATCCTCTACAACATGCTTATGAGCGCG
AAGCAAACGCGCGCGGCTCCTGAGGCTCCAGAGACGCGGCTGGTGGATCAGTGTTGGGGC
TGTTCGTGCGGCGATGAGCCCGGGGTGGGCAGAGAGGGGCTGCTGGGCGGGCGGAACGTG
GCGCTCCTGTACCGCTGCTGCTTTTGCGGTAAAGACCACCCACGGCAGGGCAGCATCCTC
TACAGCATGCTGACGAGCGCAAAGCAAACGTACGCGGCACCGAAGGCGCCCGAGGCGACG
CTGGGTCCGTGCTGGGGCTGTTCGTGCGGCTCTGATCCCGGGGTGGGCAGAGCGGGGCTT
CCGGGTGGGCGGCCCGTGGCACTCCTGTACCGCTGCTGCTTTTGTGGTGAAGACCACCCG
CGGCAGGGCAGCATCCTCTACAGCTTGCTCACTAGCTCAAAGCAAACGCACGTGGCTCCG
GCAGCGCCCGAGGCACGGCCAGGGGGCGCGTGGTGGGACCGCTCCTACTTCGCGCAGAGG
CCAGGGGGTAAAGAGGCGCTACCAGGCGGGCGGGCCACGGCGCTTCTGTACCGCTGCTGC
TTTTGCGGTGAAGACCACCCGCAGCAGGGCAGCACCCTCTACTGCGTGCCCACGAGCACA
AATCAAGCGCAGGCGGCTCCGGAGGAGCGGCCGAGGGCCCCCTGGTGGGACACCTCCTCT
GGTGCGCTGCGGCCGGTGGCGCTCAAGAGTCCACAGGTGGTCTGCGAGGCAGCCTCAGCG
GGCCTGTTGAAGACGCTGCGCTTCGTCAAGTACTTGCCCTGCTTCCAGGTGCTGCCCCTG
GACCAGCAGCTGGTGCTGGTGCGCAACTGCTGGGCGTCCCTGCTCATGCTTGAGCTGGCC
CAGGACCGCTTGCAGTTCGAGACTGTGGAAGTCTCGGAGCCCAGCATGCTGCAGAAGATC
CTCACCACCAGGCGGCGGGAGACCGGGGGCAACGAGCCACTGCCCGTGCCCACGCTGCAG
CACCATTTGGCACCGCCGGCGGAGGCCAGGAAGGTGCCCTCCGCCTCCCAGGTCCAAGCC
ATCAAGTGCTTTCTTTCCAAATGCTGGAGTCTGAACATCAGTACCAAGGAGTACGCCTAC
CTCAAGGGGACCGTGCTCTTTAACCCGGACGTGCCGGGCCTGCAGTGCGTGAAGTACATT
CAGGGACTCCAGTGGGGAACTCAGCAAATACTCAGTGAACACACCAGGATGACGCACCAA
GGGCCCCATGACAGATTCATCGAACTTAATAGTACCCTTTTCCTGCTGAGATTCATCAAT
GCCAATGTCATTGCTGAACTGTTCTTCAGGCCCATCATCGGCACAGTCAGCATGGATGAT
ATGATGCTGGAAATGCTCTGTACAAAGATATAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID NR0B1 Link Image
Target 1 GenAtlas ID NR0B1 Link Image
Target 1 HGNC ID HGNC:7960 Link Image
Target 1 Chromosome Location X
Target 1 Locus Xp21.3-p21.2
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Zanaria E, Muscatelli F, Bardoni B, Strom TM, Guioli S, Guo W, Lalli E, Moser C, Walker AP, McCabe ER, et al.: An unusual member of the nuclear hormone receptor superfamily responsible for X-linked adrenal hypoplasia congenita. Nature. 1994 Dec 15;372(6507):635-41. [PubMed Link Image]
  2. Muscatelli F, Strom TM, Walker AP, Zanaria E, Recan D, Meindl A, Bardoni B, Guioli S, Zehetner G, Rabl W, et al.: Mutations in the DAX-1 gene give rise to both X-linked adrenal hypoplasia congenita and hypogonadotropic hypogonadism. Nature. 1994 Dec 15;372(6507):672-6. [PubMed Link Image]
  3. Guo W, Burris TP, Zhang YH, Huang BL, Mason J, Copeland KC, Kupfer SR, Pagon RA, McCabe ER: Genomic sequence of the DAX1 gene: an orphan nuclear receptor responsible for X-linked adrenal hypoplasia congenita and hypogonadotropic hypogonadism. J Clin Endocrinol Metab. 1996 Jul;81(7):2481-6. [PubMed Link Image]
  4. Schwartz M, Blichfeldt S, Muller J: X-linked adrenal hypoplasia in a large Greenlandic family. Detection of a missense mutation (N4401) in the DAX-1 gene; implication for genetic counselling and carrier diagnosis. Hum Genet. 1997 Jan;99(1):83-7. [PubMed Link Image]
  5. Takahashi T, Shoji Y, Shoji Y, Haraguchi N, Takahashi I, Takada G: Active hypothalamic-pituitary-gonadal axis in an infant with X-linked adrenal hypoplasia congenita. J Pediatr. 1997 Mar;130(3):485-8. [PubMed Link Image]
  6. Nakae J, Abe S, Tajima T, Shinohara N, Murashita M, Igarashi Y, Kusuda S, Suzuki J, Fujieda K: Three novel mutations and a de novo deletion mutation of the DAX-1 gene in patients with X-linked adrenal hypoplasia congenita. J Clin Endocrinol Metab. 1997 Nov;82(11):3835-41. [PubMed Link Image]
  7. Zhang YH, Guo W, Wagner RL, Huang BL, McCabe L, Vilain E, Burris TP, Anyane-Yeboa K, Burghes AH, Chitayat D, Chudley AE, Genel M, Gertner JM, Klingensmith GJ, Levine SN, Nakamoto J, New MI, Pagon RA, Pappas JG, Quigley CA, Rosenthal IM, Baxter JD, Fletterick RJ, McCabe ER: DAX1 mutations map to putative structural domains in a deduced three-dimensional model. Am J Hum Genet. 1998 Apr;62(4):855-64. [PubMed Link Image]
Target 1 Drug References
  1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 88
Target 2 Name Retinoic acid receptor RXR-beta
Target 2 Synonyms
  1. Retinoid X receptor beta
Target 2 Gene Name RXRB
Target 2 Protein Sequence >Retinoic acid receptor RXR-beta 
MSWAARPPFLPQRHAAGQCGPVGVRKEMHCGVASRWRRRRPWLDPAAAAAAAVAGGEQQT
PEPEPGEAGRDGMGDSGRDSRSPDSSSPNPLPQGVPPPSPPGPPLPPSTAPSLGGSGAPP
PPPMPPPPLGSPFPVISSSMGSPGLPPPAPPGFSGPVSSPQINSTVSLPGGGSGPPEDVK
PPVLGVRGLHCPPPPGGPGAGKRLCAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLTYS
CRDNKDCTVDKRQRNRCQYCRYQKCLATGMKREAVQEERQRGKDKDGDGEGAGGAPEEMP
VDRILEAELAVEQKSDQGVEGPGGTGGSGSSPNDPVTNICQAADKQLFTLVEWAKRIPHF
SSLPLDDQVILLRAGWNELLIASFSHRSIDVRDGILLATGLHVHRNSAHSAGVGAIFDRV
LTELVSKMRDMRMDKTELGCLRAIILFNPDAKGLSNPSEVEVLREKVYASLETYCKQKYP
EQQGRFAKLLLRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQLA
Target 2 Number of Residues 541
Target 2 Molecular Weight 56922
Target 2 Theoretical pI 8.24
Target 2 GO Classification
Function
steroid binding
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 2 General Function Cell cycle control, cell division, chromosome partitioning
Target 2 Specific Function Nuclear hormone receptor. Involved in the retinoic acid response pathway. Binds 9-cis retinoic acid (9C-RA)
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • None
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 30448 Link Image
Target 2 UniProtKB/Swiss-Prot ID P28702 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name RXRB_HUMAN Link Image
Target 2 PDB ID 1UHL Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Nucleus
Target 2 Gene Sequence >1602 bp 
ATGTCTTGGGCCGCTCGCCCGCCCTTCCTCCCTCAGCGGCATGCCGCAGGGCAGTGTGGG
CCGGTGGGGGTGCGAAAAGAAATGCATTGTGGGGTCGCGTCCCGGTGGCGGCGGCGACGG
CCCTGGCTGGATCCCGCAGCGGCGGCGGCGGCGGCGGTGGCAGGCGGAGAACAACAAACC
CCGGAGCCGGAGCCAGGGGAGGCTGGACGGGACGGGATGGGCGACAGCGGGCGGGACTCC
CGAAGCCCAGACAGCTCCTCCCCAAATCCCCTTCCCCAGGGAGTCCCTCCCCCTTCTCCT
CCTGGGCCACCCCTACCCCCTTCAACAGCTCCATCCCTTGGAGGCTCTGGGGCCCCACCC
CCACCCCCGATGCCACCACCCCCACTGGGCTCTCCCTTTCCAGTCATCAGTTCTTCCATG
GGGTCCCCTGGTCTGCCCCCTCCAGCTCCCCCAGGATTCTCCGGGCCTGTCAGCAGCCCC
CAGATTAACTCAACAGTGTCACTCCCTGGGGGTGGGTCTGGCCCCCCTGAAGATGTGAAG
CCACCAGTCTTAGGGGTCCGGGGCCTGCACTGTCCACCCCCTCCAGGTGGCCCTGGGGCT
GGCAAACGGCTATGTGCAATCTGCGGGGACAGAAGCTCAGGCAAACACTACGGGGTTTAC
AGCTGTGAGGGTTGCAAGGGCTTCTTCAAACGCACCATCCGCAAAGACCTTACATACTCT
TGCCGGGACAACAAAGACTGCACAGTGGACAAGCGCCAGCGGAACCGCTGTCAGTACTGC
CGCTATCAGAAGTGCCTGGCCACTGGCATGAAGAGGGAGGCGGTACAGGAGGAGCGTCAG
CGGGGAAAGGACAAGGATGGGGATGGGGAGGGGGCTGGGGGAGCCCCCGAGGAGATGCCT
GTGGACAGGATCCTGGAGGCAGAGCTTGCTGTGGAACAGAAGAGTGACCAGGGCGTTGAG
GGTCCTGGGGGAACCGGGGGTAGCGGCAGCAGCCCAAATGACCCTGTGACTAACATCTGT
CAGGCAGCTGACAAACAGCTATTCACGCTTGTTGAGTGGGCGAAGAGGATCCCACACTTT
TCCTCCTTGCCTCTGGATGATCAGGTCATATTGCTGCGGGCAGGCTGGAATGAACTCCTC
ATTGCCTCCTTTTCACACCGATCCATTGATGTTCGAGATGGCATCCTCCTTGCCACAGGT
CTTCACGTGCACCGCAACTCAGCCCATTCAGCAGGAGTAGGAGCCATCTTTGATCGGGTG
CTGACAGAGCTAGTGTCCAAAATGCGTGACATGAGGATGGACAAGACAGAGCTTGGCTGC
CTGAGGGCAATCATTCTGTTTAATCCAGATGCCAAGGGCCTCTCCAACCCTAGTGAGGTG
GAGGTCCTGCGGGAGAAAGTGTATGCATCACTGGAGACCTACTGCAAACAGAAGTACCCT
GAGCAGCAGGGACGGTTTGCCAAGCTGCTGCTACGTCTTCCTGCCCTCCGGTCCATTGGC
CTTAAGTGTCTAGAGCATCTGTTTTTCTTCAAGCTCATTGGTGACACCCCCATCGACACC
TTCCTCATGGAGATGCTTGAGGCTCCCCATCAACTGGCCTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID RXRB Link Image
Target 2 GenAtlas ID RXRB Link Image
Target 2 HGNC ID HGNC:10478 Link Image
Target 2 Chromosome Location 6
Target 2 Locus 6p21.3
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Leid M, Kastner P, Lyons R, Nakshatri H, Saunders M, Zacharewski T, Chen JY, Staub A, Garnier JM, Mader S, et al.: Purification, cloning, and RXR identity of the HeLa cell factor with which RAR or TR heterodimerizes to bind target sequences efficiently. Cell. 1992 Jan 24;68(2):377-95. [PubMed Link Image]
  2. Fleischhauer K, Park JH, DiSanto JP, Marks M, Ozato K, Yang SY: Isolation of a full-length cDNA clone encoding a N-terminally variant form of the human retinoid X receptor beta. Nucleic Acids Res. 1992 Apr 11;20(7):1801. [PubMed Link Image]
  3. Purification, cloning, and RXR identity of the HeLa cell factor with which RAR or TR heterodimerizes to bind target sequences efficiently. Cell. 1992 Nov 27;71(5):887. [PubMed Link Image]
  4. Mungall AJ, Palmer SA, Sims SK, Edwards CA, Ashurst JL, Wilming L, Jones MC, Horton R, Hunt SE, Scott CE, Gilbert JG, Clamp ME, Bethel G, Milne S, Ainscough R, Almeida JP, Ambrose KD, Andrews TD, Ashwell RI, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Barker DJ, Barlow KF, Bates K, Beare DM, Beasley H, Beasley O, Bird CP, Blakey S, Bray-Allen S, Brook J, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Carder C, Carter NP, Chapman JC, Clark SY, Clark G, Clee CM, Clegg S, Cobley V, Collier RE, Collins JE, Colman LK, Corby NR, Coville GJ, Culley KM, Dhami P, Davies J, Dunn M, Earthrowl ME, Ellington AE, Evans KA, Faulkner L, Francis MD, Frankish A, Frankland J, French L, Garner P, Garnett J, Ghori MJ, Gilby LM, Gillson CJ, Glithero RJ, Grafham DV, Grant M, Gribble S, Griffiths C, Griffiths M, Hall R, Halls KS, Hammond S, Harley JL, Hart EA, Heath PD, Heathcott R, Holmes SJ, Howden PJ, Howe KL, Howell GR, Huckle E, Humphray SJ, Humphries MD, Hunt AR, Johnson CM, Joy AA, Kay M, Keenan SJ, Kimberley AM, King A, Laird GK, Langford C, Lawlor S, Leongamornlert DA, Leversha M, Lloyd CR, Lloyd DM, Loveland JE, Lovell J, Martin S, Mashreghi-Mohammadi M, Maslen GL, Matthews L, McCann OT, McLaren SJ, McLay K, McMurray A, Moore MJ, Mullikin JC, Niblett D, Nickerson T, Novik KL, Oliver K, Overton-Larty EK, Parker A, Patel R, Pearce AV, Peck AI, Phillimore B, Phillips S, Plumb RW, Porter KM, Ramsey Y, Ranby SA, Rice CM, Ross MT, Searle SM, Sehra HK, Sheridan E, Skuce CD, Smith S, Smith M, Spraggon L, Squares SL, Steward CA, Sycamore N, Tamlyn-Hall G, Tester J, Theaker AJ, Thomas DW, Thorpe A, Tracey A, Tromans A, Tubby B, Wall M, Wallis JM, West AP, White SS, Whitehead SL, Whittaker H, Wild A, Willey DJ, Wilmer TE, Wood JM, Wray PW, Wyatt JC, Young L, Younger RM, Bentley DR, Coulson A, Durbin R, Hubbard T, Sulston JE, Dunham I, Rogers J, Beck S: The DNA sequence and analysis of human chromosome 6. Nature. 2003 Oct 23;425(6960):805-11. [PubMed Link Image]
Target 2 Drug References
  1. Redfern CP: Enhancing enhancers: new complexities in the retinoid regulation of gene expression. Biochem J. 2004 Oct 1;383(Pt 1):e1-2. [PubMed Link Image]
  2. Hoegberg P, Schmidt CK, Fletcher N, Nilsson CB, Trossvik C, Gerlienke Schuur A, Brouwer A, Nau H, Ghyselinck NB, Chambon P, Hakansson H: Retinoid status and responsiveness to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in mice lacking retinoid binding protein or retinoid receptor forms. Chem Biol Interact. 2005 Sep 10;156(1):25-39. [PubMed Link Image]
  3. Nagasawa H, Takahashi S, Kobayashi A, Tazawa H, Tashima Y, Sato K: Effect of retinoic acid on murine preosteoblastic MC3T3-E1 cells. J Nutr Sci Vitaminol (Tokyo). 2005 Oct;51(5):311-8. [PubMed Link Image]
  4. Schrage K, Koopmans G, Joosten EA, Mey J: Macrophages and neurons are targets of retinoic acid signaling after spinal cord contusion injury. Eur J Neurosci. 2006 Jan;23(2):285-95. [PubMed Link Image]
  5. Stafslien DK, Vedvik KL, De Rosier T, Ozers MS: Analysis of ligand-dependent recruitment of coactivator peptides to RXRbeta in a time-resolved fluorescence resonance energy transfer assay. Mol Cell Endocrinol. 2007 Jan 29;264(1-2):82-9. Epub 2006 Dec 20. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 162
Target 3 Name Retinoic acid receptor gamma-1
Target 3 Synonyms
  1. RAR-gamma-1
Target 3 Gene Name RARG
Target 3 Protein Sequence >Retinoic acid receptor gamma-1 
MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS
LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK
NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY
ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK
IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH
NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA
LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE
MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA
Target 3 Number of Residues 461
Target 3 Molecular Weight 50342
Target 3 Theoretical pI 7.52
Target 3 GO Classification
Function
retinoic acid receptor activity
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 3 General Function Involved in transcription factor activity
Target 3 Specific Function This is a receptor for retinoic acid. This metabolite has profound effects on vertebrate development. Retinoic acid is a morphogen and is a powerful teratogen. This receptor controls cell function by directly regulating gene expression
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • None
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 306887 Link Image
Target 3 UniProtKB/Swiss-Prot ID P13631 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name RARG1_HUMAN Link Image
Target 3 PDB ID 1EXX Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Nucleus
Target 3 Gene Sequence >1365 bp 
ATGGCCACCAATAAGGAGCGACTCTTTGCGGCTGGTGCCCTGGGGCCTGGATCTGGCTAC
CCAGGGGCAGGTTTCCCCTTCGCCTTCCCAGGGGCACTCAGGGGGTCTCCGCCTTTCGAG
ATGCTGAGCCCTAGCTTCCGGGGCCTGGGCCAGCCTGACCTCCCCAAGGAGATGGCCTCT
CTGTCGGTGGAGACACAGAGCACCAGCTCAGAGGAGATGGTGCCAAGCTCGCCCTCGCCC
CCTCCGCCTCCTCGGGTCTACAAGCCATGCTTCGTGTGCAATGACAAGTCCTCTGGCTAC
CACTATGGGGTCAGCTCTTGTGAAGGCTGCAAGGGCTTCTTTCGCCGAAGCATCCAGAAG
AACATGGTGTACACGTGTCACCGCGACAAAAACTGTATCATCAACAAGGTGACCAGGAAT
CGCTGCCAGTACTGCCGGCTACAGAAGTGCTTCGAAGTGGGCATGTCCAAGGAAGCTGTG
CGAAATGACCGGAACAAGAAGAAGAAAGAGGTGAAGGAAGAAGGGTCACCTGACAGCTAT
GAGCTGAGCCCTCAGTTAGAAGAGCTCATCACCAAGGTCAGCAAAGCCCATCAGGAGACT
TTCCCCTCGCTCTGCCAGCTGGGCAAGTATACCACGAACTCCAGTGCAGACCACCGCGTG
CAGCTGGATCTGGGGCTGTGGGACAAGTTCAGTGAGCTGGCTACCAAGTGCATCATCAAG
ATCGTGGAGTTTGCCAAGCGGTTGCCTGGCTTTACAGGGCTCAGCATTGCTGACCAGATC
ACTCTGCTCAAAGCTGCCTGCCTAGATATCCTGATGCTGCGTATCTGCACAAGGTACACC
CCAGAGCAGGACACCATGACCTTCTCCGACGGGCTGACCCTGAACCGGACCCAGATGCAC
AATGCCGGCTTCGGGCCCCTCACAGACCTTGTCTTTGCCTTTGCTGGGCAGCTCCTGCCC
CTGGAGATGGATGACACCGAGACAGGGCTGCTCAGCGCCATCTGCCTCATCTGCGGAGAC
CGCATGGACCTGGAGGAGCCCGAAAAAGTGGACAAGCTGCAGGAGCCACTGCTGGAAGCC
CTGAGGCTGTACGCCCGGCGCCGGCGGCCCAGCCAGCCCTACATGTTCCCAAGGATGCTA
ATGAAAATCACCGACCTCCGGGGCATCAGCACTAAGGGAGCTGAAAGGGCCATTACTCTG
AAGATGGAGATTCCAGGCCCGATGCCTCCCTTAATCCGAGAGATGCTGGAGAACCCTGAA
ATGTTTGAGGATGACTCCTCGCAGCCTGGTCCCCACCCCAATGCCTCTAGCGAGGATGAG
GTTCCTGGGGGCCAGGGCAAAGGGGGCCTGAAGTCCCCAGCCTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID RARG Link Image
Target 3 GenAtlas ID RARG Link Image
Target 3 HGNC ID HGNC:9866 Link Image
Target 3 Chromosome Location 12
Target 3 Locus 12q13
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Lehmann JM, Hoffmann B, Pfahl M: Genomic organization of the retinoic acid receptor gamma gene. Nucleic Acids Res. 1991 Feb 11;19(3):573-8. [PubMed Link Image]
  2. Ishikawa T, Umesono K, Mangelsdorf DJ, Aburatani H, Stanger BZ, Shibasaki Y, Imawari M, Evans RM, Takaku F: A functional retinoic acid receptor encoded by the gene on human chromosome 12. Mol Endocrinol. 1990 Jun;4(6):837-44. [PubMed Link Image]
  3. Krust A, Kastner P, Petkovich M, Zelent A, Chambon P: A third human retinoic acid receptor, hRAR-gamma. Proc Natl Acad Sci U S A. 1989 Jul;86(14):5310-4. [PubMed Link Image]
  4. Renaud JP, Rochel N, Ruff M, Vivat V, Chambon P, Gronemeyer H, Moras D: Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid. Nature. 1995 Dec 14;378(6558):681-9. [PubMed Link Image]
  5. Klaholz BP, Renaud JP, Mitschler A, Zusi C, Chambon P, Gronemeyer H, Moras D: Conformational adaptation of agonists to the human nuclear receptor RAR gamma. Nat Struct Biol. 1998 Mar;5(3):199-202. [PubMed Link Image]
Target 3 Drug References
  1. Borger DR, Mi Y, Geslani G, Zyzak LL, Batova A, Engin TS, Pirisi L, Creek KE: Retinoic acid resistance at late stages of human papillomavirus type 16-mediated transformation of human keratinocytes arises despite intact retinoid signaling and is due to a loss of sensitivity to transforming growth factor-beta. Virology. 2000 May 10;270(2):397-407. [PubMed Link Image]
  2. Reddy AP, Chen JY, Zacharewski T, Gronemeyer H, Voorhees JJ, Fisher GJ: Characterization and purification of human retinoic acid receptor-gamma 1 overexpressed in the baculovirus-insect cell system. Biochem J. 1992 Nov 1;287 ( Pt 3):833-40. [PubMed Link Image]
  3. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed Link Image]
  4. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed Link Image]
  5. Kamei Y, Kawada T, Kazuki R, Sugimoto E: Retinoic acid receptor gamma 2 gene expression is up-regulated by retinoic acid in 3T3-L1 preadipocytes. Biochem J. 1993 Aug 1;293 ( Pt 3):807-12. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 409
Target 4 Name Retinoic acid receptor gamma-2
Target 4 Synonyms
  1. RAR-gamma-2
Target 4 Gene Name RARG
Target 4 Protein Sequence >Retinoic acid receptor gamma-2 
MYDCMETFAPGPRRLYGAAGPGAGLLRRATGGSCFAGLESFAWPQPASLQSVETQSTSSE
EMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQKNMVYTCHRDKN
CIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSYELSPQLEELIT
KVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIKIVEFAKRLPGF
TGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMHNAGFGPLTDLV
FAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEALRLYARRRRPS
QPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPEMFEDDSSQPGP
HPNASSEDEVPGGQGKGGLKSPA
Target 4 Number of Residues 450
Target 4 Molecular Weight 49308
Target 4 Theoretical pI 7.48
Target 4 GO Classification
Function
retinoic acid receptor activity
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 4 General Function Involved in transcription factor activity
Target 4 Specific Function This is a receptor for retinoic acid. This metabolite has profound effects on vertebrate development. Retinoic acid is a morphogen and is a powerful teratogen. This receptor controls cell function by directly regulating gene expression
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • None
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein Not Available
Target 4 UniProtKB/Swiss-Prot ID P22932 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name RARG2_HUMAN Link Image
Target 4 PDB ID 1EXX Link Image
Target 4 PDB File Show
Target 4 3D Structure
Target 4 Cellular Location
  • Nucleus
Target 4 Gene Sequence >1365 bp 
ATGGCCACCAATAAGGAGCGACTCTTTGCGGCTGGTGCCCTGGGGCCTGGATCTGGCTAC
CCAGGGGCAGGTTTCCCCTTCGCCTTCCCAGGGGCACTCAGGGGGTCTCCGCCTTTCGAG
ATGCTGAGCCCTAGCTTCCGGGGCCTGGGCCAGCCTGACCTCCCCAAGGAGATGGCCTCT
CTGTCGGTGGAGACACAGAGCACCAGCTCAGAGGAGATGGTGCCAAGCTCGCCCTCGCCC
CCTCCGCCTCCTCGGGTCTACAAGCCATGCTTCGTGTGCAATGACAAGTCCTCTGGCTAC
CACTATGGGGTCAGCTCTTGTGAAGGCTGCAAGGGCTTCTTTCGCCGAAGCATCCAGAAG
AACATGGTGTACACGTGTCACCGCGACAAAAACTGTATCATCAACAAGGTGACCAGGAAT
CGCTGCCAGTACTGCCGGCTACAGAAGTGCTTCGAAGTGGGCATGTCCAAGGAAGCTGTG
CGAAATGACCGGAACAAGAAGAAGAAAGAGGTGAAGGAAGAAGGGTCACCTGACAGCTAT
GAGCTGAGCCCTCAGTTAGAAGAGCTCATCACCAAGGTCAGCAAAGCCCATCAGGAGACT
TTCCCCTCGCTCTGCCAGCTGGGCAAGTATACCACGAACTCCAGTGCAGACCACCGCGTG
CAGCTGGATCTGGGGCTGTGGGACAAGTTCAGTGAGCTGGCTACCAAGTGCATCATCAAG
ATCGTGGAGTTTGCCAAGCGGTTGCCTGGCTTTACAGGGCTCAGCATTGCTGACCAGATC
ACTCTGCTCAAAGCTGCCTGCCTAGATATCCTGATGCTGCGTATCTGCACAAGGTACACC
CCAGAGCAGGACACCATGACCTTCTCCGACGGGCTGACCCTGAACCGGACCCAGATGCAC
AATGCCGGCTTCGGGCCCCTCACAGACCTTGTCTTTGCCTTTGCTGGGCAGCTCCTGCCC
CTGGAGATGGATGACACCGAGACAGGGCTGCTCAGCGCCATCTGCCTCATCTGCGGAGAC
CGCATGGACCTGGAGGAGCCCGAAAAAGTGGACAAGCTGCAGGAGCCACTGCTGGAAGCC
CTGAGGCTGTACGCCCGGCGCCGGCGGCCCAGCCAGCCCTACATGTTCCCAAGGATGCTA
ATGAAAATCACCGACCTCCGGGGCATCAGCACTAAGGGAGCTGAAAGGGCCATTACTCTG
AAGATGGAGATTCCAGGCCCGATGCCTCCCTTAATCCGAGAGATGCTGGAGAACCCTGAA
ATGTTTGAGGATGACTCCTCGCAGCCTGGTCCCCACCCCAATGCCTCTAGCGAGGATGAG
GTTCCTGGGGGCCAGGGCAAAGGGGGCCTGAAGTCCCCAGCCTGA
Target 4 GenBank Gene ID
Target 4 GeneCard ID RARG Link Image
Target 4 GenAtlas ID RARG Link Image
Target 4 HGNC ID HGNC:9866 Link Image
Target 4 Chromosome Location 12
Target 4 Locus 12q13
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Lehmann JM, Zhang XK, Pfahl M: RAR gamma 2 expression is regulated through a retinoic acid response element embedded in Sp1 sites. Mol Cell Biol. 1992 Jul;12(7):2976-85. [PubMed Link Image]
  2. Kastner P, Krust A, Mendelsohn C, Garnier JM, Zelent A, Leroy P, Staub A, Chambon P: Murine isoforms of retinoic acid receptor gamma with specific patterns of expression. Proc Natl Acad Sci U S A. 1990 Apr;87(7):2700-4. [PubMed Link Image]
  3. Krust A, Kastner P, Petkovich M, Zelent A, Chambon P: A third human retinoic acid receptor, hRAR-gamma. Proc Natl Acad Sci U S A. 1989 Jul;86(14):5310-4. [PubMed Link Image]
  4. Renaud JP, Rochel N, Ruff M, Vivat V, Chambon P, Gronemeyer H, Moras D: Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid. Nature. 1995 Dec 14;378(6558):681-9. [PubMed Link Image]
  5. Klaholz BP, Renaud JP, Mitschler A, Zusi C, Chambon P, Gronemeyer H, Moras D: Conformational adaptation of agonists to the human nuclear receptor RAR gamma. Nat Struct Biol. 1998 Mar;5(3):199-202. [PubMed Link Image]
Target 4 Drug References
  1. Curtin JC, Spinella MJ: p53 in human embryonal carcinoma: identification of a transferable, transcriptional repression domain in the N-terminal region of p53. Oncogene. 2005 Feb 24;24(9):1481-90. [PubMed Link Image]
  2. Parrella E, Gianni M, Fratelli M, Barzago MM, Raska I Jr, Diomede L, Kurosaki M, Pisano C, Carminati P, Merlini L, Dallavalle S, Tavecchio M, Rochette-Egly C, Terao M, Garattini E: Antitumor activity of the retinoid-related molecules (E)-3-(4'-hydroxy-3'-adamantylbiphenyl-4-yl)acrylic acid (ST1926) and 6-[3-(1-adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid (CD437) in F9 teratocarcinoma: Role of retinoic acid receptor gamma and retinoid-independent pathways. Mol Pharmacol. 2006 Sep;70(3):909-24. Epub 2006 Jun 20. [PubMed Link Image]
Drug Target 5 [top]
Target 5 ID 569
Target 5 Name Retinal dehydrogenase 2
Target 5 Synonyms
  1. Aldehyde dehydrogenase family 1 member A2
  2. EC 1.2.1.36
  3. RALDH 2
  4. RALDH(II)
  5. RalDH2
  6. Retinaldehyde-specific dehydrogenase type 2
Target 5 Gene Name ALDH1A2
Target 5 Protein Sequence >Retinal dehydrogenase 2 
MTSSKIEMPGEVKADPAALMASLHLLPSPTPNLEIKYTKIFINNEWQNSESGRVFPVYNP
ATGEQVCEVQEADKADIDKAVQAARLAFSLGSVWRRMDASERGRLLDKLADLVERDRAVL
ATMESLNGGKPFLQAFYVDLQGVIKTFRYYAGWADKIHGMTIPVDGDYFTFTRHEPIGVC
GQIIPWNFPLLMFAWKIAPALCCGNTVVIKPAEQTPLSALYMGALIKEAGFPPGVINILP
GYGPTAGAAIASHIGIDKIAFTGSTEVGKLIQEAAGRSNLKRVTLELGGKSPNIIFADAD
LDYAVEQAHQGVFFNQGQCCTAGSRIFVEESIYEEFVRRSVERAKRRVVGSPFDPTTEQG
PQIDKKQYNKILELIQSGVAEGAKLECGGKGLGRKGFFIEPTVFSNVTDDMRIAKEEIFG
PVQEILRFKTMDEVIERANNSDFGLVAAVFTNDINKALTVSSAMQAGTVWINCYNALNAQ
SPFGGFKMSGNGREMGEFGLREYSEVKTVTVKIPQKNS
Target 5 Number of Residues 526
Target 5 Molecular Weight 56725
Target 5 Theoretical pI 5.84
Target 5 GO Classification
Function
catalytic activity
oxidoreductase activity
Process
physiological process
metabolism
Component
Not Available
Target 5 General Function Energy production and conversion
Target 5 Specific Function Recognizes as substrates free retinal and cellular retinol-binding protein-bound retinal. Does metabolize octanal and decanal but does not metabolize citral, benzaldehyde, acetaldehyde and propanal efficiently
Target 5 Pathways
Name SMPDB Link KEGG Link
Retinol metabolism SMP00074 Link Image map00830 Link Image
Target 5 Reactions
  • retinal + NAD+ + H2O = retinoate + NADH + 2 H+
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • None
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 3970842 Link Image
Target 5 UniProtKB/Swiss-Prot ID O94788 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name AL1A2_HUMAN Link Image
Target 5 PDB ID 1BI9 Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location
  • Cytoplasm
Target 5 Gene Sequence >1557 bp 
ATGACTTCCAGCAAGATAGAGATGCCCGGCGAGGTGAAGGCCGACCCCGCCGCCCTCATG
GCGTCGCTGCACCTCCTGCCGTCGCCCACGCCCAATCTCGAAATTAAGTACACCAAGATC
TTTATAAACAACGAGTGGCAGAACTCAGAGAGTGGGAGAGTGTTCCCTGTCTATAATCCA
GCCACAGGAGAACAGGTGTGTGAAGTTCAAGAAGCAGACAAGGCAGATATAGACAAAGCA
GTGCAGGCAGCCCGCCTGGCTTTCTCTCTTGGTTCAGTGTGGAGAAGGATGGATGCTTCA
GAAAGGGGACGTCTGTTGGATAAGCTTGCAGACTTGGTGGAACGGGACAGGGCAGTTCTT
GCAACCATGGAATCCCTAAATGGTGGCAAACCATTCCTGCAAGCTTTTTATGTGGATTTG
CAGGGCGTCATCAAAACCTTTCGATATTACGCAGGCTGGGCTGATAAAATTCATGGGATG
ACCATTCCTGTAGATGGAGACTATTTTACCTTTACAAGACATGAACCCATTGGAGTGTGT
GGACAGATCATCCCATGGAACTTCCCCCTGCTGATGTTTGCCTGGAAAATAGCTCCAGCT
TTGTGCTGTGGCAATACAGTAGTTATTAAGCCAGCAGAGCAAACACCACTCAGTGCACTC
TACATGGGAGCCCTCATCAAGGAGGCTGGCTTTCCTCCCGGGGTCATCAATATTTTGCCA
GGATATGGGCCAACGGCTGGGGCAGCAATAGCTTCTCACATTGGCATAGACAAGATTGCA
TTCACAGGGTCTACTGAGGTTGGAAAGCTTATCCAAGAAGCAGCTGGAAGAAGTAATTTG
AAGAGAGTAACTCTGGAACTTGGAGGCAAAAGTCCTAATATTATTTTTGCTGATGCTGAC
TTGGACTATGCTGTGGAGCAGGCCCACCAGGGTGTGTTCTTCAATCAAGGTCAGTGCTGC
ACTGCAGGCTCTCGCATCTTCGTGGAGGAGTCCATCTATGAGGAGTTTGTGAGAAGAAGC
GTGGAGCGGGCCAAGAGGCGCATAGTGGGGAGTCCCTTTGACCCCACCACTGAGCAGGGT
CCCCAGATTGATAAGAAACAGTACAACAAGATCTTGGAACTCATCCAGAGTGGTGTGGCT
GAGGGCGCCAAGCTGGAATGTGGAGGCAAAGGACTGGGCCGAAAGGGGTTTTTCATTGAG
CCCACAGTGTTTTCCAACGTCACTGATGATATGCGGATTGCCAAGGAGGAGATCTTTGGC
CCTGTTCAGGAAATTTTGAGATTTAAGACGATGGATGAAGTTATCGAAAGAGCCAATAAC
TCAGACTTTGGACTCGTAGCAGCTGTCTTTACTAATGACATCAACAAGGCCCTCACAGTG
TCTTCTGCAATGCAAGCTGGGACTGTTTGGATCAATTGTTACAATGCCTTAAATGCCCAG
AGCCCCTTTGGGGGATTCAAGATGTCTGGAAATGGGAGAGAAATGGGAGAATTTGGCTTG
CGGGAGTACTCAGAAGTTAAGACGGTGACAGTAAAGATCCCCCAGAAGAACTCCTAA
Target 5 GenBank Gene ID
Target 5 GeneCard ID ALDH1A2 Link Image
Target 5 GenAtlas ID ALDH1A2 Link Image
Target 5 HGNC ID HGNC:15472 Link Image
Target 5 Chromosome Location 15
Target 5 Locus 15q22.1
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Ono Y, Fukuhara N, Yoshie O: TAL1 and LIM-only proteins synergistically induce retinaldehyde dehydrogenase 2 expression in T-cell acute lymphoblastic leukemia by acting as cofactors for GATA3. Mol Cell Biol. 1998 Dec;18(12):6939-50. [PubMed Link Image]
Target 5 Drug References
  1. Mic FA, Sirbu IO, Duester G: Retinoic acid synthesis controlled by Raldh2 is required early for limb bud initiation and then later as a proximodistal signal during apical ectodermal ridge formation. J Biol Chem. 2004 Jun 18;279(25):26698-706. Epub 2004 Apr 6. [PubMed Link Image]
  2. Bordelon T, Montegudo SK, Pakhomova S, Oldham ML, Newcomer ME: A disorder to order transition accompanies catalysis in retinaldehyde dehydrogenase type II. J Biol Chem. 2004 Oct 8;279(41):43085-91. Epub 2004 Aug 7. [PubMed Link Image]
  3. Mic FA, Molotkov A, Molotkova N, Duester G: Raldh2 expression in optic vesicle generates a retinoic acid signal needed for invagination of retina during optic cup formation. Dev Dyn. 2004 Oct;231(2):270-7. [PubMed Link Image]
  4. Doxakis E, Davies AM: Retinoic acid negatively regulates GDNF and neurturin receptor expression and responsiveness in embryonic chicken sympathetic neurons. Mol Cell Neurosci. 2005 Aug;29(4):617-27. [PubMed Link Image]
  5. Everts HB, Sundberg JP, Ong DE: Immunolocalization of retinoic acid biosynthesis systems in selected sites in rat. Exp Cell Res. 2005 Aug 15;308(2):309-19. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 611
Target 6 Name Retinal dehydrogenase 1
Target 6 Synonyms
  1. ALDH-E1
  2. ALHDII
  3. Aldehyde dehydrogenase family 1 member A1
  4. Aldehyde dehydrogenase, cytosolic
  5. EC 1.2.1.36
  6. RALDH 1
  7. RalDH1
Target 6 Gene Name ALDH1A1
Target 6 Protein Sequence >Retinal dehydrogenase 1 
SSSGTPDLPVLLTDLKIQYTKIFINNEWHDSVSGKKFPVFNPATEEELCQVEEGDKEDVD
KAVKAARQAFQIGSPWRTMDASERGRLLYKLADLIERDRLLLATMESMNGGKLYSNAYLN
DLAGCIKTLRYCAGWADKIQGRTIPIDGNFFTYTRHEPIGVCGQIIPWNFPLVMLIWKIG
PALSCGNTVVVKPAEQTPLTALHVASLIKEAGFPPGVVNIVPGYGPTAGAAISSHMDIDK
VAFTGSTEVGKLIKEAAGKSNLKRVTLELGGKSPCIVLADADLDNAVEFAHHGVFYHQGQ
CCIAASRIFVEESIYDEFVRRSVERAKKYILGNPLTPGVTQGPQIDKEQYDKILDLIESG
KKEGAKLECGGGPWGNKGYFVQPTVFSNVTDEMRIAKEEIFGPVQQIMKFKSLDDVIKRA
NNTFYGLSAGVFTKDIDKAITISSALQAGTVWVNCYGVVSAQCPFGGFKMSGNGRELGEY
GFHEYTEVKTVTVKISQKNS
Target 6 Number of Residues 508
Target 6 Molecular Weight 54731
Target 6 Theoretical pI 6.71
Target 6 GO Classification
Function
catalytic activity
oxidoreductase activity
Process
physiological process
metabolism
Component
Not Available
Target 6 General Function Energy production and conversion
Target 6 Specific Function Binds free retinal and cellular retinol-binding protein- bound retinal. Can convert/oxidize retinaldehyde to retinoic acid
Target 6 Pathways
Name SMPDB Link KEGG Link
Retinol metabolism SMP00074 Link Image map00830 Link Image
Target 6 Reactions
  • retinal + NAD+ + H2O = retinoate + NADH + 2 H+
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • None
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 178372 Link Image
Target 6 UniProtKB/Swiss-Prot ID P00352 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name AL1A1_HUMAN Link Image
Target 6 PDB ID 1BXS Link Image
Target 6 PDB File Show
Target 6 3D Structure
Target 6 Cellular Location
  • Cytoplasm
Target 6 Gene Sequence >1506 bp 
ATGTCATCCTCAGGCACGCCAGACTTACCTGTCCTACTCACCGATTTGAAGATTCAATAT
ACTAAGATCTTCATAAACAATGAATGGCATGATTCAGTGAGTGGCAAGAAATTTCCTGTC
TTTAATCCTGCAACTGAGGAGGAGCTCTGCCAGGTAGAAGAAGGAGATAAGGAGGATGTT
GACAAGGCAGTGAAGGCCGCAAGACAGGCTTTTCAGATTGGATCTCCGTGGCGTACTATG
GATGCTTCCGAGAGGGGGCGACTATTATACAAGTTGGCTGATTTAATCGAAAGAGATCGT
CTGCTGCTGGCGACAATGGAGTCAATGAATGGTGGAAAACTCTATTCCAATGCATATCTG
AATGATTTAGCAGGCTGCATCAAAACATTGCGCTACTGTGCAGGTTGGGCTGACAAGATC
CAGGGCCGTACAATACCAATTGATGGAAATTTTTTTACATATACAAGACATGAACCTATT
GGTGTATGTGGCCAAATCATTCCTTGGAATTTCCCGTTGGTTATGCTCATTTGGAAGATA
GGGCCTGCACTGAGCTGTGGAAACACAGTGGTTGTCAAACCAGCAGAGCAAACTCCTCTC
ACTGCTCTCCACGTGGCATCTTTAATAAAAGAGGCAGGGTTTCCTCCTGGAGTAGTGAAT
ATTGTTCCTGGTTATGGGCCTACAGCAGGGGCAGCCATTTCTTCTCACATGGATATAGAC
AAAGTAGCCTTCACAGGATCAACAGAGGTTGGCAAGTTGATCAAAGAAGCTGCCGGGAAA
AGCAATCTGAAGAGGGTGACCCTGGAGCTTGGAGGAAAGAGCCCTTGCATTGTGTTAGCT
GATGCCGACTTGGACAATGCTGTTGAATTTGCACACCATGGGGTATTCTACCACCAGGGC
CAGTGTTGTATAGCCGCATCCAGGATTTTTGTGGAAGAATCAATTTATGATGAGTTTGTT
CGAAGGAGTGTTGAGCGGGCTAAGAAGTATATCCTTGGAAATCCTCTGACCCCAGGAGTC
ACTCAAGGCCCTCAGATTGACAAGGAACAATATGATAAAATACTTGACCTCATTGAGAGT
GGGAAGAAAGAAGGGGCCAAACTGGAATGTGGAGGAGGCCCGTGGGGGAATAAAGGCTAC
TTTGTCCAGCCCACAGTGTTCTCTAATGTTACAGATGAGATGCGCATTGCCAAAGAGGAG
ATTTTTGGACCAGTGCAGCAAATCATGAAGTTTAAATCTTTAGATGACGTGATCAAAAGA
GCAAACAATACTTTCTATGGCTTATCAGCAGGAGTGTTTACCAAAGACATTGATAAAGCC
ATAACAATCTCCTCTGCTCTGCAGGCAGGAACAGTGTGGGTGAATTGCTATGGCGTGGTA
AGTGCCCAGTGCCCCTTTGGTGGATTCAAGATGTCTGGAAATGGAAGAGAACTGGGAGAG
TACGGTTTCCATGAATATACAGAGGTCAAAACAGTCACAGTGAAAATCTCTCAGAAGAAC
TCATAA
Target 6 GenBank Gene ID
Target 6 GeneCard ID ALDH1A1 Link Image
Target 6 GenAtlas ID ALDH1A1 Link Image
Target 6 HGNC ID HGNC:402 Link Image
Target 6 Chromosome Location 9
Target 6 Locus 9q21.13
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Hsu LC, Chang WC, Yoshida A: Genomic structure of the human cytosolic aldehyde dehydrogenase gene. Genomics. 1989 Nov;5(4):857-65. [PubMed Link Image]
  2. Agarwal DP, Cohn P, Goedde HW, Hempel J: Aldehyde dehydrogenase from human erythrocytes: structural relationship to the liver cytosolic isozyme. Enzyme. 1989;42(1):47-52. [PubMed Link Image]
  3. Hsu LC, Tani K, Fujiyoshi T, Kurachi K, Yoshida A: Cloning of cDNAs for human aldehyde dehydrogenases 1 and 2. Proc Natl Acad Sci U S A. 1985 Jun;82(11):3771-5. [PubMed Link Image]
  4. Abriola DP, Fields R, Stein S, MacKerell AD Jr, Pietruszko R: Active site of human liver aldehyde dehydrogenase. Biochemistry. 1987 Sep 8;26(18):5679-84. [PubMed Link Image]
  5. Yoshida A, Ikawa M, Hsu LC, Tani K: Molecular abnormality and cDNA cloning of human aldehyde dehydrogenases. Alcohol. 1985 Jan-Feb;2(1):103-6. [PubMed Link Image]
  6. Hempel J, von Bahr-Lindstrom H, Jornvall H: Aldehyde dehydrogenase from human liver. Primary structure of the cytoplasmic isoenzyme. Eur J Biochem. 1984 May 15;141(1):21-35. [PubMed Link Image]
  7. Zheng CF, Wang TT, Weiner H: Cloning and expression of the full-length cDNAS encoding human liver class 1 and class 2 aldehyde dehydrogenase. Alcohol Clin Exp Res. 1993 Aug;17(4):828-31. [PubMed Link Image]
  8. Yoshida A, Hsu LC, Yanagawa Y: Biological role of human cytosolic aldehyde dehydrogenase 1: hormonal response, retinal oxidation and implication in testicular feminization. Adv Exp Med Biol. 1993;328:37-44. [PubMed Link Image]
Target 6 Drug References
  1. Everts HB, King LE Jr, Sundberg JP, Ong DE: Hair cycle-specific immunolocalization of retinoic acid synthesizing enzymes Aldh1a2 and Aldh1a3 indicate complex regulation. J Invest Dermatol. 2004 Aug;123(2):258-63. [PubMed Link Image]
  2. Mic FA, Molotkov A, Molotkova N, Duester G: Raldh2 expression in optic vesicle generates a retinoic acid signal needed for invagination of retina during optic cup formation. Dev Dyn. 2004 Oct;231(2):270-7. [PubMed Link Image]
  3. Kim H, Lapointe J, Kaygusuz G, Ong DE, Li C, van de Rijn M, Brooks JD, Pollack JR: The retinoic acid synthesis gene ALDH1a2 is a candidate tumor suppressor in prostate cancer. Cancer Res. 2005 Sep 15;65(18):8118-24. [PubMed Link Image]
  4. Matt N, Dupe V, Garnier JM, Dennefeld C, Chambon P, Mark M, Ghyselinck NB: Retinoic acid-dependent eye morphogenesis is orchestrated by neural crest cells. Development. 2005 Nov;132(21):4789-800. Epub 2005 Oct 5. [PubMed Link Image]
  5. Gidlof AC, Ocaya P, Olofsson PS, Torma H, Sirsjo A: Differences in retinol metabolism and proliferative response between neointimal and medial smooth muscle cells. J Vasc Res. 2006;43(4):392-8. Epub 2006 Jul 6. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 719
Target 7 Name Retinoic acid receptor responder protein 1
Target 7 Synonyms
  1. RAR-responsive protein TIG1
  2. Tazarotene-induced gene 1 protein
Target 7 Gene Name RARRES1
Target 7 Protein Sequence >Retinoic acid receptor responder protein 1 
MQPRRQRLPAPWSGPRGPRPTAPLLALLLLLAPVAAPAGSGDPDDPGQPQDAGVPRRLLQ
QAARAALHFFNFRSGSPSALRVLAEVQEGRAWINPKEGCKVHVVFSTERYNPESLLQEGE
GRLGKCSARVFFKNQKPRPTINVTCTRLIEKKKRQQEDYLLYKQMKQLKNPLEIVSIPDN
HGHIDPSLRLIWDLAFLGSSYVMWEMTTQVSHYYLAQLTSVRQWKTNDDTIDFDYTVLLH
ELSTQEIIPCRIHLVWYPGKPLKVKYHCQELQTPEEASGTEEGSAVVPTELSNF
Target 7 Number of Residues 298
Target 7 Molecular Weight 33285
Target 7 Theoretical pI 8.69
Target 7 GO Classification Not Available
Target 7 General Function Not Available
Target 7 Specific Function Not Available
Target 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • 21-42
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 942585 Link Image
Target 7 UniProtKB/Swiss-Prot ID P49788 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name TIG1_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Membrane
  • single-pass type II membrane protein (Potential)
Target 7 Gene Sequence >885 bp 
ATGCAGCCCCGCCGGCAACGGCTGCCCGCTCCCTGGTCCGGGCCCAGGGGCCCGCGCCCC
ACCGCCCCGCTGCTCGCGCTGCTGCTGTTGCTCGCCCCGGTGGCGGCGCCCGCGGGGTCC
GGGGACCCCGACGACCCTGGGCAGCCTCAGGATGCTGGGGTCCCGCGCAGGCTCCTGCAG
CAGGCGGCGCGCGCGGCGCTTCACTTCTTCAACTTCCGGTCCGGCTCGCCCAGCGCGCTG
CGAGTGCTGGCCGAGGTGCAGGAGGGCCGCGCGTGGATTAATCCAAAAGAGGGATGTAAA
GTTCACGTGGTCTTCAGCACAGAGCGCTACAACCCAGAGTCTTTACTTCAGGAAGGTGAG
GGACGTTTGGGGAAATGTTCTGCTCGAGTGTTTTTCAAGAATCAGAAACCCAGACCAACT
ATCAATGTAACTTGTACACGGCTCATCGAGAAAAAGAAAAGACAACAAGAGGATTACCTG
CTTTACAAGCAAATGAAGCAACTGAAAAACCCCTTGGAAATAGTCAGCATACCTGATAAT
CATGGACATATTGATCCCTCTCTGAGACTCATCTGGGATTTGGCTTTCCTTGGAAGCTCT
TACGTGATGTGGGAAATGACAACACAGGTGTCACACTACTACTTGGCACAGCTCACTAGT
GTGAGGCAGTGGAAAACTAATGATGATACAATTGATTTTGATTATACTGTTCTACTTCAT
GAATTATCAACACAGGAAATAATTCCCTGTCGCATTCACTTGGTCTGGTACCCTGGCAAA
CCTCTTAAAGTGAAGTACCACTGTCAAGAGCTACAGACACCAGAAGAAGCCTCCGGAACT
GAAGAAGGATCAGCTGTAGTACCAACAGAGCTTAGTAATTTCTAA
Target 7 GenBank Gene ID
Target 7 GeneCard ID RARRES1 Link Image
Target 7 GenAtlas ID RARRES1 Link Image
Target 7 HGNC ID HGNC:9867 Link Image
Target 7 Chromosome Location 3
Target 7 Locus 3q25.32-q25.33
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Nagpal S, Patel S, Asano AT, Johnson AT, Duvic M, Chandraratna RA: Tazarotene-induced gene 1 (TIG1), a novel retinoic acid receptor-responsive gene in skin. J Invest Dermatol. 1996 Feb;106(2):269-74. [PubMed Link Image]
Target 7 Drug References
  1. Youssef EM, Chen XQ, Higuchi E, Kondo Y, Garcia-Manero G, Lotan R, Issa JP: Hypermethylation and silencing of the putative tumor suppressor Tazarotene-induced gene 1 in human cancers. Cancer Res. 2004 Apr 1;64(7):2411-7. [PubMed Link Image]
  2. Zirn B, Samans B, Spangenberg C, Graf N, Eilers M, Gessler M: All-trans retinoic acid treatment of Wilms tumor cells reverses expression of genes associated with high risk and relapse in vivo. Oncogene. 2005 Aug 4;24(33):5246-51. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 770
Target 8 Name Retinoic acid-induced protein 3
Target 8 Synonyms
  1. G-protein coupled receptor family C group 5 member A
  2. Orphan G-protein coupling receptor PEIG-1
  3. RAIG-1
  4. Retinoic acid-induced gene 1 protein
Target 8 Gene Name GPRC5A
Target 8 Protein Sequence >Retinoic acid-induced protein 3 
MATTVPDGCRNGLKSKYYRLCDKAEAWGIVLETVATAGVVTSVAFMLTLPILVCKVQDSN
RRKMLPTQFLFLLGVLGIFGLTFAFIIGLDGSTGPTRFFLFGILFSICFSCLLAHAVSLT
KLVRGRKPLSLLVILGLAVGFSLVQDVIAIEYIVLTMNRTNVNVFSELSAPRRNEDFVLL
LTYVLFLMALTFLMSSFTFCGSFTGWKRHGAHIYLTMLLSIAIWVAWITLLMLPDFDRRW
DDTILSSALAANGWVFLLAYVSPEFWLLTKQRNPMDYPVEDAFCKPQLVKKSYGVENRAY
SQEEITQGFEETGDTLYAPYSTHFQLQNQPPQKEFSIPRAHAWPSPYKDYEVKKEGS
Target 8 Number of Residues 362
Target 8 Molecular Weight 40252
Target 8 Theoretical pI 8.26
Target 8 GO Classification
Function
signal transducer activity
receptor activity
transmembrane receptor activity
G-protein coupled receptor activity
metabotropic glutamate, GABA-B-like receptor activity
Process
Not Available
Component
cell
membrane
Target 8 General Function Involved in metabotropic glutamate, GABA-B-like receptor activity
Target 8 Specific Function Unknown. This G-protein coupled receptor could be involved in modulating differentiation and maintaining homeostasis of epithelial cells. The comparable expression level in fetal lung and kidney with adult tissues suggests a possible role in embryonic development and maturation of these organs. This retinoic acid-inducible GPCR provide evidence for a possible interaction between retinoid and G-protein signaling pathways
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • 34-54
  • 69-89
  • 98-118
  • 130-150
  • 177-197
  • 213-233
  • 248-268
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 4063890 Link Image
Target 8 UniProtKB/Swiss-Prot ID Q8NFJ5 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name RAI3_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Cell membrane
  • cytoplasmic vesicle membrane
  • multi
  • multi-pass membrane protein. Cytoplasmic vesicle
Target 8 Gene Sequence >1074 bp 
ATGGCTACAACAGTCCCTGATGGTTGCCGCAATGGCCTGAAATCCAAGTACTACAGACTT
TGTGATAAGGCTGAAGCTTGGGGCATCGTCCTAGAAACGGTGGCCACAGCCGGGGTTGTG
ACCTCGGTGGCCTTCATGCTCACTCTCCCGATCCTCGTCTGCAAGGTGCAGGACTCCAAC
AGGCGAAAAATGCTGCCTACTCAGTTTCTCTTCCTCCTGGGTGTGTTGGGCATCTTTGGC
CTCACCTTCGCCTTCATCATCGGACTGGACGGGAGCACAGGGCCCACACGCTTCTTCCTC
TTTGGGATCCTCTTTTCCATCTGCTTCTCCTGCCTGCTGGCTCATGCTGTCAGTCTGACC
AAGCTCGTCCGGGGGAGGAAGCCCCTTTCCCTGTTGGTGATTCTGGGTCTGGCCGTGGGC
TTCAGCCTAGTCCAGGATGTTATCGCTATTGAATATATTGTCCTGACCATGAATAGGACC
AACGTCAATGTCTTTTCTGAGCTTTCCGCTCCTCGTCGCAATGAAGACTTTGTCCTCCTG
CTCACCTACGTCCTCTTCTTGATGGCGCTGACCTTCCTCATGTCCTCCTTCACCTTCTGT
GGTTCCTTCACGGGCTGGAAGAGACATGGGGCCCACATCTACCTCACGATGCTCCTCTCC
ATTGCCATCTGGGTGGCCTGGATCACCCTGCTCATGCTTCCTGACTTTGACCGCAGGTGG
GATGACACCATCCTCAGCTCCGCCTTGGCTGCCAATGGCTGGGTGTTCCTGTTGGCTTAT
GTTAGTCCCGAGTTTTGGCTGCTCACAAAGCAACGAAACCCCATGGATTATCCTGTTGAG
GATGCTTTCTGTAAACCTCAACTCGTGAAGAAGAGCTATGGTGTGGAGAACAGAGCCTAC
TCTCAAGAGGAAATCACTCAAGGTTTTGAAGAGACAGGGGACACGCTCTATGCCCCCTAT
TCCACACATTTTCAGCTGCAGAACCAGCCTCCCCAAAAGGAATTCTCCATCCCACGGGCC
CACGCTTGGCCGAGCCCTTACAAAGACTATGAAGTAAAGAAAGAGGGCAGCTAA
Target 8 GenBank Gene ID
Target 8 GeneCard ID GPRC5A Link Image
Target 8 GenAtlas ID GPRC5A Link Image
Target 8 HGNC ID HGNC:9836 Link Image
Target 8 Chromosome Location 12
Target 8 Locus 12p13-p12.3
Target 8 SNPs SNPJam Report Link Image
Target 8 General References
  1. Brauner-Osborne H, Krogsgaard-Larsen P: Sequence and expression pattern of a novel human orphan G-protein-coupled receptor, GPRC5B, a family C receptor with a short amino-terminal domain. Genomics. 2000 Apr 15;65(2):121-8. [PubMed Link Image]
  2. Cheng Y, Lotan R: Molecular cloning and characterization of a novel retinoic acid-inducible gene that encodes a putative G protein-coupled receptor. J Biol Chem. 1998 Dec 25;273(52):35008-15. [PubMed Link Image]
Target 8 Drug References
  1. Inoue S, Nambu T, Shimomura T: The RAIG family member, GPRC5D, is associated with hard-keratinized structures. J Invest Dermatol. 2004 Mar;122(3):565-73. [PubMed Link Image]
  2. Xu J, Tian J, Shapiro SD: Normal lung development in RAIG1-deficient mice despite unique lung epithelium-specific expression. Am J Respir Cell Mol Biol. 2005 May;32(5):381-7. Epub 2005 Jan 27. [PubMed Link Image]
Drug Target 9 [top]
Target 9 ID 780
Target 9 Name Retinoic acid receptor RXR-gamma
Target 9 Synonyms
  1. Retinoid X receptor gamma
Target 9 Gene Name RXRG
Target 9 Protein Sequence >Retinoic acid receptor RXR-gamma 
MYGNYSHFMKFPAGYGGSPGHTGSTSMSPSAALSTGKPMDSHPSYTDTPVSAPRTLSAVG
TPLNALGSPYRVITSAMGPPSGALAAPPGINLVAPPSSQLNVVNSVSSSEDIKPLPGLPG
IGNMNYPSTSPGSLVKHICAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLIYTCRDNKD
CLIDKRQRNRCQYCRYQKCLVMGMKREAVQEERQRSRERAESEAECATSGHEDMPVERIL
EAELAVEPKTESYGDMNMENSTNDPVTNICHAADKQLFTLVEWAKRIPHFSDLTLEDQVI
LLRAGWNELLIASFSHRSVSVQDGILLATGLHVHRSSAHSAGVGSIFDRVLTELVSKMKD
MQMDKSELGCLRAIVLFNPDAKGLSNPSEVETLREKVYATLEAYTKQKYPEQPGRFAKLL
LRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLETPLQIT
Target 9 Number of Residues 470
Target 9 Molecular Weight 50872
Target 9 Theoretical pI 7.67
Target 9 GO Classification
Function
steroid binding
signal transducer activity
receptor activity
ligand-dependent nuclear receptor activity
steroid hormone receptor activity
binding
nucleic acid binding
DNA binding
transcription factor activity
Process
regulation of biological process
regulation of physiological process
regulation of metabolism
regulation of cellular metabolism
regulation of nucleobase, nucleoside, nucleotide and nucleic acid metabolism
regulation of transcription
regulation of transcription, DNA-dependent
Component
organelle
membrane-bound organelle
intracellular membrane-bound organelle
nucleus
Target 9 General Function Involved in transcription factor activity
Target 9 Specific Function Nuclear hormone receptor. Involved in the retinoic acid response pathway. Binds 9-cis retinoic acid (9C-RA)
Target 9 Pathways Not Available
Target 9 Reactions Not Available
Target 9 Pfam Domain Function
Target 9 Signals
  • None
Target 9 Transmembrane Regions
  • None
Target 9 Essentiality Non-Essential
Target 9 GenBank ID Protein 1053069 Link Image
Target 9 UniProtKB/Swiss-Prot ID P48443 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name RXRG_HUMAN Link Image
Target 9 PDB ID Not Available
Target 9 Cellular Location
  • Nucleus
Target 9 Gene Sequence >1392 bp 
ATGTATGGAAATTATTCTCACTTCATGAAGTTTCCCGCAGGCTATGGAGGCTCCCCTGGC
CACACTGGCTCTACATCCATGAGCCCATCAGCAGCCTTGTCCACAGGGAAGCCAATGGAC
AGCCACCCCAGCTACACAGATACCCCAGTGAGTGCCCCACGGACTCTGAGTGCAGTGGGG
ACCCCCCTCAATGCCCTGGGCTCTCCATATCGAGTCATCACCTCTGCCATGGGCCCACCC
TCAGGAGCACTTGCAGCGCCTCCAGGAATCAACTTGGTTGCCCCACCCAGCTCTCAGCTA
AATGTGGTCAACAGTGTCAGCAGTTCAGAGGACATCAAGCCCTTACCAGGGCTTCCCGGG
ATTGGAAACATGAACTACCCATCCACCAGCCCCGGATCTCTGGTTAAACACATCTGTGCT
ATCTGTGGAGACAGATCCTCAGGAAAGCACTACGGGGTATACAGTTGTGAAGGCTGCAAA
GGGTTCTTCAAGAGGACGATAAGGAAGGACCTCATCTACACGTGTCGGGATAATAAAGAC
TGCCTCATTGACAAGCGTCAGCGCAACCGCTGCCAGTACTGTCGCTATCAGAAGTGCCTT
GTCATGGGCATGAAGAGGGAAGCTGTGCAAGAAGAAAGACAGAGGAGCCGAGAGCGAGCT
GAGAGTGAGGCAGAATGTGCTACCAGTGGTCATGAAGACATGCCTGTGGAGAGGATTCTA
GAAGCTGAACTTGCTGTTGAACCAAAGACAGAATCCTATGGTGACATGAATATGGAGAAC
TCGACAAATGACCCTGTTACCAACATATGTCATGCTGCTGACAAGCAGCTTTTCACCCTC
GTTGAATGGGCCAAGCGTATTCCCCACTTCTCTGACCTCACCTTGGAGGACCAGGTCATT
TTGCTTCGGGCAGGGTGGAATGAATTGCTGATTGCCTCTTTCTCCCACCGCTCAGTTTCC
GTGCAGGATGGCATCCTTCTGGCCACGGGTTTACATGTCCACCGGAGCAGTGCCCACAGT
GCTGGGGTCGGCTCCATCTTTGACAGAGTTCTAACTGAGCTGGTTTCCAAAATGAAAGAC
ATGCAGATGGACAAGTCGGAACTGGGATGCCTGCGAGCCATTGTACTCTTTAACCCAGAT
GCCAAGGGCCTGTCCAACCCCTCTGAGGTGGAGACTCTGCGAGAGAAGGTTTATGCCACC
CTTGAGGCCTACACCAAGCAGAAGTATCCGGAACAGCCAGGCAGGTTTGCCAAGCTGCTG
CTGCGCCTCCCAGCTCTGCGTTCCATTGGCTTGAAATGCCTGGAGCACCTCTTCTTCTTC
AAGCTCATCGGGGACACCCCCATTGACACCTTCCTCATGGAGATGTTGGAGACCCCGCTG
CAGATCACCTGA
Target 9 GenBank Gene ID
Target 9 GeneCard ID RXRG Link Image
Target 9 GenAtlas ID RXRG Link Image
Target 9 HGNC ID HGNC:10479 Link Image
Target 9 Chromosome Location 1
Target 9 Locus 1q22-q23
Target 9 SNPs SNPJam Report Link Image
Target 9 General References Not Available
Target 9 Drug References
  1. Wang J, Yen A: A novel retinoic acid-responsive element regulates retinoic acid-induced BLR1 expression. Mol Cell Biol. 2004 Mar;24(6):2423-43. [PubMed Link Image]
  2. Schrage K, Koopmans G, Joosten EA, Mey J: Macrophages and neurons are targets of retinoic acid signaling after spinal cord contusion injury. Eur J Neurosci. 2006 Jan;23(2):285-95. [PubMed Link Image]
  3. Day RM, Lee YH, Park AM, Suzuki YJ: Retinoic acid inhibits airway smooth muscle cell migration. Am J Respir Cell Mol Biol. 2006 Jun;34(6):695-703. Epub 2006 Feb 2. [PubMed Link Image]
  4. Koda T, Imai H, Morita M: Antiestrogenic activity of vitamin A in in vivo uterotrophic assay. Life Sci. 2007 Feb 13;80(10):945-9. Epub 2006 Nov 22. [PubMed Link Image]
  5. He JC, Lu TC, Fleet M, Sunamoto M, Husain M, Fang W, Neves S, Chen Y, Shankland S, Iyengar R, Klotman PE: Retinoic acid inhibits HIV-1-induced podocyte proliferation through the cAMP pathway. J Am Soc Nephrol. 2007 Jan;18(1):93-102. Epub 2006 Dec 20. [PubMed Link Image]

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.