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Showing drug card for Alitretinoin (DB00523)

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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-04-16 16:47:46
Primary Accession Number DB00523
Secondary Accession Number
  • APRD00017
Name Alitretinoin
Drug Type
  • Approved
  • Investigational
  • Small Molecule
Description An important regulator of gene expression during growth and development, and in neoplasms. Tretinoin, also known as retinoic acid and derived from maternal vitamin A, is essential for normal growth; and embryonic development. An excess of tretinoin can be teratogenic. It is used in the treatment of psoriasis; acne vulgaris; and several other skin diseases. It has also been approved for use in promyelocytic leukemia (leukemia, promyelocytic, acute). [PubChem]
Synonyms
  1. ALRT-1057
  2. BAL4079
  3. Retinoic Acid
  4. alitretinoin
Brand Names
  1. Panretin
  2. Panretin Gel
  3. Panretyn
  4. Panrexin
  5. Renova
  6. Retin-A
  7. Retin-A Micro
  8. Vesanoid
Brand Mixtures Not Available
Chemical IUPAC Name (2E,4E,6E,8E)-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 5300-03-8
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)/b9-6+,12-11+,15-8+,16-14+/f/h21H
InChI Key SHGAZHPCJJPHSC-FWNNKZREDV
KEGG Drug Not Available
KEGG Compound Not Available
PubChem Compound 444795 Link Image
PubChem Substance 164122 Link Image
ChEBI ID Not Available
PharmGKB ID PA448089 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available
RxList Link http://www.rxlist.com/cgi/generic2/alitre.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Alitretinoin Link Image
FDA Label
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 300.4351
Monoisotopic Molecular Weight 300.2089
State Solid
Melting Point 189-190 oC
Experimental Water Solubility 0.6 mg/L 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 Not Available
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
  • Keratolytic Agents
ATC Codes
AHFS Codes
  • 84:16.00
  • 92:00.00
Indication For topical treatment of cutaneous lesions in patients with AIDS-related Kaposi's sarcoma.
Pharmacology Alitretinoin (9-cis-retinoic acid) is a naturally-occurring endogenous retinoid indicated for topical treatment of cutaneous lesions in patients with AIDS-related Kaposi's sarcoma. Alitretinoin inhibits the growth of Kaposi's sarcoma (KS) cells in vitro.
Mechanism of Action Alitretinoin binds to and activates all known intracellular retinoid receptor subtypes (RARa, RARb, RARg, RXRa, RXRb and RXRg). Once activated these receptors function as transcription factors that regulate the expression of genes that control the process of cellular differentiation and proliferation in both normal and neoplastic cells.
Absorption Not Available
Toxicity Not Available
Protein Binding Not Available
Biotransformation Not Available
Half Life Not Available
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 Not Available
Food Interactions Not Available
Pathways Not Available
General References
  1. Drugs.com Link Image
  2. Wikipedia Link Image
  3. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Retinoic acid receptor RXR-beta
  2. Retinoic acid receptor gamma-1
  3. Retinoic acid receptor beta
  4. Retinoic acid receptor gamma-2
  5. Retinoic acid receptor RXR-alpha
  6. Cellular retinoic acid-binding protein 1
  7. Retinoic acid receptor alpha
  8. Retinoic acid receptor RXR-gamma
  9. Cellular retinoic acid-binding protein 2
Drug Target 1 [top]
Target 1 ID 88
Target 1 Name Retinoic acid receptor RXR-beta
Target 1 Synonyms
  1. Retinoid X receptor beta
Target 1 Gene Name RXRB
Target 1 Protein Sequence >Retinoic acid receptor RXR-beta 
MSWAARPPFLPQRHAAGQCGPVGVRKEMHCGVASRWRRRRPWLDPAAAAAAAVAGGEQQT
PEPEPGEAGRDGMGDSGRDSRSPDSSSPNPLPQGVPPPSPPGPPLPPSTAPSLGGSGAPP
PPPMPPPPLGSPFPVISSSMGSPGLPPPAPPGFSGPVSSPQINSTVSLPGGGSGPPEDVK
PPVLGVRGLHCPPPPGGPGAGKRLCAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLTYS
CRDNKDCTVDKRQRNRCQYCRYQKCLATGMKREAVQEERQRGKDKDGDGEGAGGAPEEMP
VDRILEAELAVEQKSDQGVEGPGGTGGSGSSPNDPVTNICQAADKQLFTLVEWAKRIPHF
SSLPLDDQVILLRAGWNELLIASFSHRSIDVRDGILLATGLHVHRNSAHSAGVGAIFDRV
LTELVSKMRDMRMDKTELGCLRAIILFNPDAKGLSNPSEVEVLREKVYASLETYCKQKYP
EQQGRFAKLLLRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQLA
Target 1 Number of Residues 541
Target 1 Molecular Weight 56922
Target 1 Theoretical pI 8.24
Target 1 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 1 General Function Cell cycle control, cell division, chromosome partitioning
Target 1 Specific Function Nuclear hormone receptor. Involved in the retinoic acid response pathway. Binds 9-cis retinoic acid (9C-RA)
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 30448 Link Image
Target 1 UniProtKB/Swiss-Prot ID P28702 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name RXRB_HUMAN Link Image
Target 1 PDB ID 1UHL Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Nucleus
Target 1 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 1 GenBank Gene ID
Target 1 GeneCard ID RXRB Link Image
Target 1 GenAtlas ID RXRB Link Image
Target 1 HGNC ID HGNC:10478 Link Image
Target 1 Chromosome Location 6
Target 1 Locus 6p21.3
Target 1 SNPs SNPJam Report Link Image
Target 1 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 1 Drug References
  1. 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]
  2. Bergheim I, Wolfgarten E, Bollschweiler E, Holscher AH, Bode CH, Parlesak A: Role of retinoic acid receptors in squamous-cell carcinoma in human esophagus. J Carcinog. 2005 Nov 8;4:20. [PubMed Link Image]
  3. 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]
  4. Germain P, Chambon P, Eichele G, Evans RM, Lazar MA, Leid M, De Lera AR, Lotan R, Mangelsdorf DJ, Gronemeyer H: International Union of Pharmacology. LXIII. Retinoid X receptors. Pharmacol Rev. 2006 Dec;58(4):760-72. [PubMed Link Image]
  5. Brtko J: Role of retinoids and their cognate nuclear receptors in breast cancer chemoprevention. Cent Eur J Public Health. 2007 Mar;15(1):3-6. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 162
Target 2 Name Retinoic acid receptor gamma-1
Target 2 Synonyms
  1. RAR-gamma-1
Target 2 Gene Name RARG
Target 2 Protein Sequence >Retinoic acid receptor gamma-1 
MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS
LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK
NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY
ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK
IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH
NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA
LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE
MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA
Target 2 Number of Residues 461
Target 2 Molecular Weight 50342
Target 2 Theoretical pI 7.52
Target 2 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 2 General Function Involved in transcription factor activity
Target 2 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 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 306887 Link Image
Target 2 UniProtKB/Swiss-Prot ID P13631 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name RARG1_HUMAN Link Image
Target 2 PDB ID 1EXX Link Image
Target 2 PDB File Show
Target 2 3D Structure
Target 2 Cellular Location
  • Nucleus
Target 2 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 2 GenBank Gene ID
Target 2 GeneCard ID RARG Link Image
Target 2 GenAtlas ID RARG Link Image
Target 2 HGNC ID HGNC:9866 Link Image
Target 2 Chromosome Location 12
Target 2 Locus 12q13
Target 2 SNPs SNPJam Report Link Image
Target 2 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 2 Drug References
  1. 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]
  2. Li M, Hener P, Zhang Z, Kato S, Metzger D, Chambon P: Topical vitamin D3 and low-calcemic analogs induce thymic stromal lymphopoietin in mouse keratinocytes and trigger an atopic dermatitis. Proc Natl Acad Sci U S A. 2006 Aug 1;103(31):11736-41. Epub 2006 Jul 31. [PubMed Link Image]
  3. Dzhagalov I, Chambon P, He YW: Regulation of CD8+ T lymphocyte effector function and macrophage inflammatory cytokine production by retinoic acid receptor gamma. J Immunol. 2007 Feb 15;178(4):2113-21. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 229
Target 3 Name Retinoic acid receptor beta
Target 3 Synonyms
  1. HBV-activated protein
  2. RAR-beta
  3. RAR-epsilon
Target 3 Gene Name RARB
Target 3 Protein Sequence >Retinoic acid receptor beta 
MTTSGHACPVPAVNGHMTHYPATPYPLLFPPVIGGLSLPPLHGLHGHPPPSGCSTPSPAT
IETQSTSSEELVPSPPSPLPPPRVYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM
IYTCHRDKNCVINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKETSKQECTESYEM
TAELDDLTEKIRKAHQETFPSLCQLGKYTTNSSADHRVRLDLGLWDKFSELATKCIIKIV
EFAKRLPGFTGLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA
GFGPLTDLVFTFANQLLPLEMDDTETGLLSAICLICGDRQDLEEPTKVDKLQEPLLEALK
IYIRKRRPSKPHMFPKILMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGH
EPLTPSSSGNTAEHSPSISPSSVENSGVSQSPLVQ
Target 3 Number of Residues 462
Target 3 Molecular Weight 50490
Target 3 Theoretical pI 7.86
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 35883 Link Image
Target 3 UniProtKB/Swiss-Prot ID P10826 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name RARB_HUMAN Link Image
Target 3 PDB ID 1XDK Link Image
Target 3 PDB File Show
Target 3 3D Structure
Target 3 Cellular Location
  • Isoform beta-1, isoform beta-2:Nucleus. Isoform beta-4:Cytoplasm
Target 3 Gene Sequence >1347 bp 
ATGTTTGACTGTATGGATGTTCTGTCAGTGAGTCCTGGGCAAATCCTGGATTTCTACACT
GCGAGTCCGTCTTCCTGCATGCTCCAGGAGAAAGCTCTCAAAGCATGCTTCAGTGGATTG
ACCCAAACCGAATGGCAGCATCGGCACACTGCTCAATCAATTGAAACACAGAGCACCAGC
TCTGAGGAACTCGTCCCAAGCCCCCCATCTCCACTTCCTCCCCCTCGAGTGTACAAACCC
TGCTTCGTCTGCCAGGACAAATCATCAGGGTACCACTATGGGGTCAGCGCCTGTGAGGGA
TGTAAGGGCTTTTTCCGCAGAAGTATTCAGAAGAATATGATTTACACTTGTCACCGAGAT
AAGAACTGTGTTATTAATAAAGTCACCAGGAATCGATGCCAATACTGTCGACTCCAGAAG
TGCTTTGAAGTGGGAATGTCCAAAGAATCTGTCAGGAATGACAGGAACAAGAAAAAAAAG
GAGACTTCGAAGCAAGAATGCACAGAGAGCTATGAAATGACAGCTGAGTTGGACGATCTC
ACAGAGAAGATCCGAAAAGCTCACCAGGAAACTTTCCCTTCACTCTGCCAGCTGGGTAAA
TACACCACGAATTCCAGTGCTGACCATCGAGTCCGACTGGACCTGGGCCTCTGGGACAAA
TTCAGTGAACTGGCCACCAAGTGCATTATTAAGATCGTGGAGTTTGCTAAACGTCTGCCT
GGTTTCACTGGCTTGACCATCGCAGACCAAATTACCCTGCTGAAGGCCGCCTGCCTGGAC
ATCCTGATTCTTAGAATTTGCACCAGGTATACCCCAGAACAAGACACCATGACTTTCTCA
GACGGCCTTACCCTAAATCGAACTCAGATGCACAATGCTGGATTTGGTCCTCTGACTGAC
CTTGTGTTCACCTTTGCCAACCAGCTCCAGCCTTTGGAAATGGATGACACAGAAACAGGC
CTTCTCAGTGCCATCTGCTTAATCTGTGGAGACCGCCAGGACCTTGAGGAACCGACAAAA
GTAGATAAGCTACAAGAACCATTGCTGGAAGCACTAAAAATTTATATCAGAAAAAGACGA
CCCAGCAAGCCTCACATGTTTCCAAAGATCTTAATGAAAATCACAGATCTCCGTAGCATC
AGTGCTAAAGGTGCAGAGCGTGTAATTACCTTGAAAATGGAAATTCCTGGATCAATGCCA
CCTCTCATTCAAGAAATGCTGGAGAATTCTGAAGGACATGAACCCTTGACCCCAAGTTCA
AGTGGGAACACAGCAGAGCACAGTCCTAGCATCTCACCCAGCTCAGTGGAAAACAGTGGG
GTCAGTCAGTCACCACTCCTGCAATAA
Target 3 GenBank Gene ID
Target 3 GeneCard ID RARB Link Image
Target 3 GenAtlas ID RARB Link Image
Target 3 HGNC ID HGNC:9865 Link Image
Target 3 Chromosome Location 3
Target 3 Locus 3p24
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Sommer KM, Chen LI, Treuting PM, Smith LT, Swisshelm K: Elevated retinoic acid receptor beta(4) protein in human breast tumor cells with nuclear and cytoplasmic localization. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8651-6. [PubMed Link Image]
  2. Katahira M, Knegtel RM, Boelens R, Eib D, Schilthuis JG, van der Saag PT, Kaptein R: Homo- and heteronuclear NMR studies of the human retinoic acid receptor beta DNA-binding domain: sequential assignments and identification of secondary structure elements. Biochemistry. 1992 Jul 21;31(28):6474-80. [PubMed Link Image]
  3. Shen S, Kruyt FA, den Hertog J, van der Saag PT, Kruijer W: Mouse and human retinoic acid receptor beta 2 promoters: sequence comparison and localization of retinoic acid responsiveness. DNA Seq. 1991;2(2):111-9. [PubMed Link Image]
  4. Dejean A, de The H: Hepatitis B virus as an insertional mutagene in a human hepatocellular carcinoma. Mol Biol Med. 1990 Jun;7(3):213-22. [PubMed Link Image]
  5. de The H, Marchio A, Tiollais P, Dejean A: A novel steroid thyroid hormone receptor-related gene inappropriately expressed in human hepatocellular carcinoma. Nature. 1987 Dec 17-23;330(6149):667-70. [PubMed Link Image]
  6. Brand N, Petkovich M, Krust A, Chambon P, de The H, Marchio A, Tiollais P, Dejean A: Identification of a second human retinoic acid receptor. Nature. 1988 Apr 28;332(6167):850-3. [PubMed Link Image]
  7. Benbrook D, Lernhardt E, Pfahl M: A new retinoic acid receptor identified from a hepatocellular carcinoma. Nature. 1988 Jun 16;333(6174):669-72. [PubMed Link Image]
  8. Dejean A, Bougueleret L, Grzeschik KH, Tiollais P: Hepatitis B virus DNA integration in a sequence homologous to v-erb-A and steroid receptor genes in a hepatocellular carcinoma. Nature. 1986 Jul 3-9;322(6074):70-2. [PubMed Link Image]
  9. Houle B, Pelletier M, Wu J, Goodyer C, Bradley WE: Fetal isoform of human retinoic acid receptor beta expressed in small cell lung cancer lines. Cancer Res. 1994 Jan 15;54(2):365-9. [PubMed Link Image]
  10. Knegtel RM, Katahira M, Schilthuis JG, Bonvin AM, Boelens R, Eib D, van der Saag PT, Kaptein R: The solution structure of the human retinoic acid receptor-beta DNA-binding domain. J Biomol NMR. 1993 Jan;3(1):1-17. [PubMed Link Image]
Target 3 Drug References
  1. Mizuiri H, Yoshida K, Toge T, Oue N, Aung PP, Noguchi T, Yasui W: DNA methylation of genes linked to retinoid signaling in squamous cell carcinoma of the esophagus: DNA methylation of CRBP1 and TIG1 is associated with tumor stage. Cancer Sci. 2005 Sep;96(9):571-7. [PubMed Link Image]
  2. Milliano MT, Luxon BA: Rat hepatic stellate cells become retinoid unresponsive during activation. Hepatol Res. 2005 Nov;33(3):225-33. Epub 2005 Oct 25. [PubMed Link Image]
  3. Liu Z, Zhang L, Ding F, Li J, Guo M, Li W, Wang Y, Yu Z, Zhan Q, Wu M, Liu Z: 5-Aza-2'-deoxycytidine induces retinoic acid receptor-beta(2) demethylation and growth inhibition in esophageal squamous carcinoma cells. Cancer Lett. 2005 Dec 18;230(2):271-83. [PubMed Link Image]
  4. Nalbandian A, Pang AL, Rennert OM, Chan WY, Ravindranath N, Djakiew D: A novel function of differentiation revealed by cDNA microarray profiling of p75NTR-regulated gene expression. Differentiation. 2005 Oct;73(8):385-96. [PubMed Link Image]
  5. Husson M, Enderlin V, Delacourte A, Ghenimi N, Alfos S, Pallet V, Higueret P: Retinoic acid normalizes nuclear receptor mediated hypo-expression of proteins involved in beta-amyloid deposits in the cerebral cortex of vitamin A deprived rats. Neurobiol Dis. 2006 Jul;23(1):1-10. Epub 2006 Mar 10. [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. Gianni M, Kopf E, Bastien J, Oulad-Abdelghani M, Garattini E, Chambon P, Rochette-Egly C: Down-regulation of the phosphatidylinositol 3-kinase/Akt pathway is involved in retinoic acid-induced phosphorylation, degradation, and transcriptional activity of retinoic acid receptor gamma 2. J Biol Chem. 2002 Jul 12;277(28):24859-62. Epub 2002 May 24. [PubMed Link Image]
  2. 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]
  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 5 [top]
Target 5 ID 459
Target 5 Name Retinoic acid receptor RXR-alpha
Target 5 Synonyms
  1. Retinoid X receptor alpha
Target 5 Gene Name RXRA
Target 5 Protein Sequence >Retinoic acid receptor RXR-alpha 
MDTKHFLPLDFSTQVNSSLTSPTGRGSMAAPSLHPSLGPGIGSPGQLHSPISTLSSPING
MGPPFSVISSPMGPHSMSVPTTPTLGFSTGSPQLSSPMNPVSSSEDIKPPLGLNGVLKVP
AHPSGNMASFTKHICAICGDRSSGKHYGVYSCEGCKGFFKRTVRKDLTYTCRDNKDCLID
KRQRNRCQYCRYQKCLAMGMKREAVQEERQRGKDRNENEVESTSSANEDMPVERILEAEL
AVEPKTETYVEANMGLNPSSPNDPVTNICQAADKQLFTLVEWAKRIPHFSELPLDDQVIL
LRAGWNELLIASFSHRSIAVKDGILLATGLHVHRNSAHSAGVGAIFDRVLTELVSKMRDM
QMDKTELGCLRAIVLFNPDSKGLSNPAEVEALREKVYASLEAYCKHKYPEQPGRFAKLLL
RLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQMT
Target 5 Number of Residues 469
Target 5 Molecular Weight 50812
Target 5 Theoretical pI 7.86
Target 5 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 5 General Function Involved in transcription factor activity
Target 5 Specific Function Nuclear hormone receptor. Involved in the retinoic acid response pathway. Binds 9-cis retinoic acid (9C-RA). ARF6 acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer
Target 5 Pathways Not Available
Target 5 Reactions Not Available
Target 5 Pfam Domain Function
Target 5 Signals
  • None
Target 5 Transmembrane Regions
  • None
Target 5 Essentiality Non-Essential
Target 5 GenBank ID Protein 35885 Link Image
Target 5 UniProtKB/Swiss-Prot ID P19793 Link Image
Target 5 UniProtKB/Swiss-Prot Entry Name RXRA_HUMAN Link Image
Target 5 PDB ID 1LBD Link Image
Target 5 PDB File Show
Target 5 3D Structure
Target 5 Cellular Location
  • Nucleus
Target 5 Gene Sequence >1389 bp 
ATGGACACCAAACATTTCCTGCCGCTCGATTTCTCCACCCAGGTGAACTCCTCCCTCACC
TCCCCGACGGGGCGAGGCTCCATGGCTGCCCCCTCGCTGCACCCGTCCCTGGGGCCTGGC
ATCGGCTCCCCGGGACAGCTGCATTCTCCCATCAGCACCCTGAGCTCCCCCATCAACGGC
ATGGGCCCGCCTTTCTCGGTCATCAGCTCCCCCATGGGCCCCCACTCCATGTCGGTGCCC
ACCACACCCACCCTGGGCTTCAGCACTGGCAGCCCCCAGCTCAGCTCACCTATGAACCCC
GTCAGCAGCAGCGAGGACATCAAGCCCCCCCTGGGCCTCAATGGCGTCCTCAAGGTCCCC
GCCCACCCCTCAGGAAACATGGCTTCCTTCACCAAGCACATCTGCGCCATCTGCGGGGAC
CGCTCCTCAGGCAAGCACTATGGAGTGTACAGCTGCGAGGGGTGCAAGGGCTTCTTCAAG
CGGACGGTGCGCAAGGACCTGACCTACACCTGCCGCGACAACAAGGACTGCCTGATTGAC
AAGCGGCAGCGGAACCGGTGCCAGTACTGCCGCTACCAGAAGTGCCTGGCCATGGGCATG
AAGCGGGAAGCCGTGCAGGAGGAGCGGCAGCGTGGCAAGGACCGGAACGAGAATGAGGTG
GAGTCGACCAGCAGCGCCAACGAGGACATGCCGGTGGAGAGGATCCTGGAGGCTGAGCTG
GCCGTGGAGCCCAAGACCGAGACCTACGTGGAGGCAAACATGGGGCTGAACCCCAGCTCG
CCGAACGACCCTGTCACCAACATTTGCCAAGCAGCCGACAAACAGCTTTTCACCCTGGTG
GAGTGGGCCAAGCGGATCCCACACTTCTCAGAGCTGCCCCTGGACGACCAGGTCATCCTG
CTGCGGGCAGGCTGGAATGAGCTGCTCATCGCCTCCTTCTCCCACCGCTCCATCGCCGTG
AAGGACGGGATCCTCCTGGCCACCGGGCTGCACGTCCACCGGAACAGCGCCCACAGCGCA
GGGGTGGGCGCCATCTTTGACAGGGTGCTGACGGAGCTTGTGTCCAAGATGCGGGACATG
CAGATGGACAAGACGGAGCTGGGCTGCCTGCGCGCCATCGTCCTCTTTAACCCTGACTCC
AAGGGGCTCTCGAACCCGGCCGAGGTGGAGGCGCTGAGGGAGAAGGTCTATGCGTCCTTG
GAGGCCTACTGCAAGCACAAGTACCCAGAGCAGCCGGGAAGGTTCGCTAAGCTCTTGCTC
CGCCTGCCGGCTCTGCGCTCCATCGGGCTCAAATGCCTGGAACATCTCTTCTTCTTCAAG
CTCATCGGGGACACACCCATTGACACCTTCCTTATGGAGATGCTGGAGGCGCCGCACCAA
ATGACTTAG
Target 5 GenBank Gene ID
Target 5 GeneCard ID RXRA Link Image
Target 5 GenAtlas ID RXRA Link Image
Target 5 HGNC ID HGNC:10477 Link Image
Target 5 Chromosome Location 9
Target 5 Locus 9q34.3
Target 5 SNPs SNPJam Report Link Image
Target 5 General References
  1. Lee SK, Anzick SL, Choi JE, Bubendorf L, Guan XY, Jung YK, Kallioniemi OP, Kononen J, Trent JM, Azorsa D, Jhun BH, Cheong JH, Lee YC, Meltzer PS, Lee JW: A nuclear factor, ASC-2, as a cancer-amplified transcriptional coactivator essential for ligand-dependent transactivation by nuclear receptors in vivo. J Biol Chem. 1999 Nov 26;274(48):34283-93. [PubMed Link Image]
  2. Mathur M, Tucker PW, Samuels HH: PSF is a novel corepressor that mediates its effect through Sin3A and the DNA binding domain of nuclear hormone receptors. Mol Cell Biol. 2001 Apr;21(7):2298-311. [PubMed Link Image]
  3. Heyman RA, Mangelsdorf DJ, Dyck JA, Stein RB, Eichele G, Evans RM, Thaller C: 9-cis retinoic acid is a high affinity ligand for the retinoid X receptor. Cell. 1992 Jan 24;68(2):397-406. [PubMed Link Image]
  4. Mangelsdorf DJ, Ong ES, Dyck JA, Evans RM: Nuclear receptor that identifies a novel retinoic acid response pathway. Nature. 1990 May 17;345(6272):224-9. [PubMed Link Image]
  5. Rastinejad F, Perlmann T, Evans RM, Sigler PB: Structural determinants of nuclear receptor assembly on DNA direct repeats. Nature. 1995 May 18;375(6528):203-11. [PubMed Link Image]
  6. Bourguet W, Ruff M, Chambon P, Gronemeyer H, Moras D: Crystal structure of the ligand-binding domain of the human nuclear receptor RXR-alpha. Nature. 1995 Jun 1;375(6530):377-82. [PubMed Link Image]
  7. Lee MS, Sem DS, Kliewer SA, Provencal J, Evans RM, Wright PE: NMR assignments and secondary structure of the retinoid X receptor alpha DNA-binding domain. Evidence for the novel C-terminal helix. Eur J Biochem. 1994 Sep 1;224(2):639-50. [PubMed Link Image]
  8. Chen H, Lin RJ, Schiltz RL, Chakravarti D, Nash A, Nagy L, Privalsky ML, Nakatani Y, Evans RM: Nuclear receptor coactivator ACTR is a novel histone acetyltransferase and forms a multimeric activation complex with P/CAF and CBP/p300. Cell. 1997 Aug 8;90(3):569-80. [PubMed Link Image]
  9. Holmbeck SM, Foster MP, Casimiro DR, Sem DS, Dyson HJ, Wright PE: High-resolution solution structure of the retinoid X receptor DNA-binding domain. J Mol Biol. 1998 Aug 14;281(2):271-84. [PubMed Link Image]
Target 5 Drug References
  1. Bartholin L, Powers SE, Melhuish TA, Lasse S, Weinstein M, Wotton D: TGIF inhibits retinoid signaling. Mol Cell Biol. 2006 Feb;26(3):990-1001. [PubMed Link Image]
  2. Calleja C, Messaddeq N, Chapellier B, Yang H, Krezel W, Li M, Metzger D, Mascrez B, Ohta K, Kagechika H, Endo Y, Mark M, Ghyselinck NB, Chambon P: Genetic and pharmacological evidence that a retinoic acid cannot be the RXR-activating ligand in mouse epidermis keratinocytes. Genes Dev. 2006 Jun 1;20(11):1525-38. [PubMed Link Image]
  3. Zhelyaznik N, Mey J: Regulation of retinoic acid receptors alpha, beta and retinoid X receptor alpha after sciatic nerve injury. Neuroscience. 2006 Sep 15;141(4):1761-74. Epub 2006 Jun 19. [PubMed Link Image]
  4. Fukasawa H, Kagechika H, Shudo K: [Retinoid therapy for autoimmune diseases] Nihon Rinsho Meneki Gakkai Kaishi. 2006 Jun;29(3):114-26. [PubMed Link Image]
  5. Mizuguchi Y, Wada A, Nakagawa K, Ito M, Okano T: Antitumoral activity of 13-demethyl or 13-substituted analogues of all-trans retinoic acid and 9-cis retinoic acid in the human myeloid leukemia cell line HL-60. Biol Pharm Bull. 2006 Sep;29(9):1803-9. [PubMed Link Image]
Drug Target 6 [top]
Target 6 ID 564
Target 6 Name Cellular retinoic acid-binding protein 1
Target 6 Synonyms
  1. CRABP-I
  2. Cellular retinoic acid- binding protein I
  3. Retinoic acid-binding protein I, cellular
Target 6 Gene Name CRABP1
Target 6 Protein Sequence >Cellular retinoic acid-binding protein 1 
PNFAGTWKMRSSENFDELLKALGVNAMLRKVAVAAASKPHVEIRQDGDQFYIKTSTTVRT
TEINFKVGEGFEEETVDGRKCRSLATWENENKIHCTQTLLEGDGPKTYWTRELANDELIL
TFGADDVVCTRIYVRE
Target 6 Number of Residues 138
Target 6 Molecular Weight 15434
Target 6 Theoretical pI 5.03
Target 6 GO Classification
Function
lipid binding
binding
Process
physiological process
cellular physiological process
transport
Component
Not Available
Target 6 General Function Involved in retinoid binding
Target 6 Specific Function Cytosolic CRABPs may regulate the access of retinoic acid to the nuclear retinoic acid receptors
Target 6 Pathways Not Available
Target 6 Reactions Not Available
Target 6 Pfam Domain Function
Target 6 Signals
  • None
Target 6 Transmembrane Regions
  • None
Target 6 Essentiality Non-Essential
Target 6 GenBank ID Protein 241542 Link Image
Target 6 UniProtKB/Swiss-Prot ID P29762 Link Image
Target 6 UniProtKB/Swiss-Prot Entry Name RABP1_HUMAN Link Image
Target 6 PDB ID 2CBR Link Image
Target 6 PDB File Show
Target 6 3D Structure
Target 6 Cellular Location
  • Cytoplasm
Target 6 Gene Sequence >414 bp 
ATGCCCAACTTCGCCGGCACCTGGAAGATGCGCAGCAGCGAGAATTTCGACGAGCTGCTG
AAGGCACTGGGTGTGAACGCCATGCTGAGGAAAGTGGCCGTAGCGGCTGCGTCCAAGCCG
CACGTGGAGATCCGCCAGGACGGGGATCAGTTCTACATCAAGACATCCACCACCGTGCGC
ACCACTGAGATCAACTTCAAGGTCGGAGAAGGCTTTGAGGAGGAGACCGTGGACGGACGC
AAGTGCAGGAGTTTAGCCACTTGGGAGAATGAGAACAAGATCCACTGCACCCAAACTCTT
CTTGAAGGGGACGGCCCCAAAACCTACTGGACCCGTGAGCTGGCCAACGATGAACTTATC
CTGACGTTTGGCGCCGATGACGTGGTCTGCACCAGAATTTATGTCCGGGAATGA
Target 6 GenBank Gene ID
Target 6 GeneCard ID CRABP1 Link Image
Target 6 GenAtlas ID CRABP1 Link Image
Target 6 HGNC ID HGNC:2338 Link Image
Target 6 Chromosome Location 15
Target 6 Locus 15q24
Target 6 SNPs SNPJam Report Link Image
Target 6 General References
  1. Eller MS, Oleksiak MF, McQuaid TJ, McAfee SG, Gilchrest BA: The molecular cloning and expression of two CRABP cDNAs from human skin. Exp Cell Res. 1992 Feb;198(2):328-36. [PubMed Link Image]
  2. Astrom A, Tavakkol A, Pettersson U, Cromie M, Elder JT, Voorhees JJ: Molecular cloning of two human cellular retinoic acid-binding proteins (CRABP). Retinoic acid-induced expression of CRABP-II but not CRABP-I in adult human skin in vivo and in skin fibroblasts in vitro. J Biol Chem. 1991 Sep 15;266(26):17662-6. [PubMed Link Image]
Target 6 Drug References
  1. 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]
  2. Goelden U, Pfoertner S, Hansen W, Toepfer T, von Knobloch R, Hofmann R, Buer J, Schrader AJ: Expression and functional influence of cellular retinoic acid-binding protein II in renal cell carcinoma. Urol Int. 2005;75(3):269-76. [PubMed Link Image]
  3. Levadoux-Martin M, Li Y, Blackburn A, Chabanon H, Hesketh JE: Perinuclear localisation of cellular retinoic acid binding protein I mRNA. Biochem Biophys Res Commun. 2006 Feb 3;340(1):326-31. [PubMed Link Image]
  4. Jetten AM: Multi-stage program of differentiation in human epidermal keratinocytes: regulation by retinoids. J Invest Dermatol. 1990 Nov;95(5 Suppl):44S-46S. [PubMed Link Image]
  5. Bry K, Lappalainen U: Pathogenesis of bronchopulmonary dysplasia: the role of interleukin 1beta in the regulation of inflammation-mediated pulmonary retinoic acid pathways in transgenic mice. Semin Perinatol. 2006 Jun;30(3):121-8. [PubMed Link Image]
Drug Target 7 [top]
Target 7 ID 730
Target 7 Name Retinoic acid receptor alpha
Target 7 Synonyms
  1. RAR-alpha
Target 7 Gene Name RARA
Target 7 Protein Sequence >Retinoic acid receptor alpha 
MASNSSSCPTPGGGHLNGYPVPPYAFFFPPMLGGLSPPGALTTLQHQLPVSGYSTPSPAT
IETQSSSSEEIVPSPPSPPPLPRIYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM
VYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKEVPKPECSESYTL
TPEVGELIEKVRKAHQETFPALCQLGKYTTNNSSEQRVSLDIDLWDKFSELSTKCIIKTV
EFAKQLPGFTTLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA
GFGPLTDLVFAFANQLLPLEMDDAETGLLSAICLICGDRQDLEQPDRVDMLQEPLLEALK
VYVRKRRPSRPHMFPKMLMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGL
DTLSGQPGGGGRDGGGLAPPPGSCSPSLSPSSNRSSPATHSP
Target 7 Number of Residues 469
Target 7 Molecular Weight 50772
Target 7 Theoretical pI 7.95
Target 7 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 7 General Function Involved in transcription factor activity
Target 7 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 7 Pathways Not Available
Target 7 Reactions Not Available
Target 7 Pfam Domain Function
Target 7 Signals
  • None
Target 7 Transmembrane Regions
  • None
Target 7 Essentiality Non-Essential
Target 7 GenBank ID Protein 36157 Link Image
Target 7 UniProtKB/Swiss-Prot ID P10276 Link Image
Target 7 UniProtKB/Swiss-Prot Entry Name RARA_HUMAN Link Image
Target 7 PDB ID Not Available
Target 7 Cellular Location
  • Nucleus
Target 7 Gene Sequence >1389 bp 
ATGGCCAGCAACAGCAGCTCCTGCCCGACACCTGGGGGCGGGCACCTCAATGGGTACCCG
GTGCCTCCCTACGCCTTCTTCTTCCCCCCTATGCTGGGTGGACTCTCCCCGCCAGGCGCT
CTGACCACTCTCCAGCACCAGCTTCCAGTTAGTGGATATAGCACACCATCCCCAGCCACC
ATTGAGACCCAGAGCAGCAGTTCTGAAGAGATAGTGCCCAGCCCTCCCTCGCCACCCCCT
CTACCCCGCATCTACAAGCCTTGCTTTGTCTGTCAGGACAAGTCCTCAGGCTACCACTAT
GGGGTCAGCGCCTGTGAGGGCTGCAAGGGCTTCTTCCGCCGCAGCATCCAGAAGAACATG
GTGTACACGTGTCACCGGGACAAGAACTGCATCATCAACAAGGTGACCCGGAACCGCTGC
CAGTACTGCCGACTGCAGAAGTGCTTTGAAGTGGGCATGTCCAAGGAGTCTGTGAGAAAC
GACCGAAACAAGAAGAAGAAGGAGGTGCCCAAGCCCGAGTGCTCTGAGAGCTACACGCTG
ACGCCGGAGGTGGGGGAGCTCATTGAGAAGGTGCGCAAAGCGCACCAGGAAACCTTCCCT
GCCCTCTGCCAGCTGGGCAAATACACTACGAACAACAGCTCAGAACAACGTGTCTCTCTG
GACATTGACCTCTGGGACAAGTTCAGTGAACTCTCCACCAAGTGCATCATTAAGACTGTG
GAGTTCGCCAAGCAGCTGCCCGGCTTCACCACCCTCACCATCGCCGACCAGATCACCCTC
CTCAAGGCTGCCTGCCTGGACATCCTGATCCTGCGGATCTGCACGCGGTACACGCCCGAG
CAGGACACCATGACCTTCTCGGACGGGCTGACCCTGAACCGGACCCAGATGCACAACGCT
GGCTTCGGCCCCCTCACCGACCTGGTCTTTGCCTTCGCCAACCAGCTGCTGCCCCTGGAG
ATGGATGATGCGGAGACGGGGCTGCTCAGCGCCATCTGCCTCATCTGCGGAGACCGCCAG
GACCTGGAGCAGCCGGACCGGGTGGACATGCTGCAGGAGCCGCTGCTGGAGGCGCTAAAG
GTCTACGTGCGGAAGCGGAGGCCCAGCCGCCCCCACATGTTCCCCAAGATGCTAATGAAG
ATTACTGACCTGCGAAGCATCAGCGCCAAGGGGGCTGAGCGGGTGATCACGCTGAAGATG
GAGATCCCGGGCTCCATGCCGCCTCTCATCCAGGAAATGTTGGAGAACTCAGAGGGCCTG
GACACTCTGAGCGGACAGCCGGGGGGTGGGGGGCGGGACGGGGGTGGCCTGGCCCCCCCG
CCAGGCAGCTGTAGCCCCAGCCTCAGCCCCAGCTCCAACAGAAGCAGCCCGGCCACCCAC
TCCCCGTGA
Target 7 GenBank Gene ID
Target 7 GeneCard ID RARA Link Image
Target 7 GenAtlas ID RARA Link Image
Target 7 HGNC ID HGNC:9864 Link Image
Target 7 Chromosome Location 17
Target 7 Locus 17q21
Target 7 SNPs SNPJam Report Link Image
Target 7 General References
  1. Hjalt TA, Murray JC: Genomic structure of the human retinoic acid receptor-alpha1 gene. Mamm Genome. 1999 May;10(5):528-9. [PubMed Link Image]
  2. Lee SK, Anzick SL, Choi JE, Bubendorf L, Guan XY, Jung YK, Kallioniemi OP, Kononen J, Trent JM, Azorsa D, Jhun BH, Cheong JH, Lee YC, Meltzer PS, Lee JW: A nuclear factor, ASC-2, as a cancer-amplified transcriptional coactivator essential for ligand-dependent transactivation by nuclear receptors in vivo. J Biol Chem. 1999 Nov 26;274(48):34283-93. [PubMed Link Image]
  3. Shao W, Halachmi S, Brown M: ERAP140, a conserved tissue-specific nuclear receptor coactivator. Mol Cell Biol. 2002 May;22(10):3358-72. [PubMed Link Image]
  4. Brand NJ, Petkovich M, Chambon P: Characterization of a functional promoter for the human retinoic acid receptor-alpha (hRAR-alpha). Nucleic Acids Res. 1990 Dec 11;18(23):6799-806. [PubMed Link Image]
  5. Petkovich M, Brand NJ, Krust A, Chambon P: A human retinoic acid receptor which belongs to the family of nuclear receptors. Nature. 1987 Dec 3-9;330(6147):444-50. [PubMed Link Image]
  6. Giguere V, Ong ES, Segui P, Evans RM: Identification of a receptor for the morphogen retinoic acid. Nature. 1987 Dec 17-23;330(6149):624-9. [PubMed Link Image]
  7. Chen Z, Guidez F, Rousselot P, Agadir A, Chen SJ, Wang ZY, Degos L, Zelent A, Waxman S, Chomienne C: PLZF-RAR alpha fusion proteins generated from the variant t(11;17)(q23;q21) translocation in acute promyelocytic leukemia inhibit ligand-dependent transactivation of wild-type retinoic acid receptors. Proc Natl Acad Sci U S A. 1994 Feb 1;91(3):1178-82. [PubMed Link Image]
  8. Redner RL, Rush EA, Faas S, Rudert WA, Corey SJ: The t(5;17) variant of acute promyelocytic leukemia expresses a nucleophosmin-retinoic acid receptor fusion. Blood. 1996 Feb 1;87(3):882-6. [PubMed Link Image]
  9. Chen H, Lin RJ, Schiltz RL, Chakravarti D, Nash A, Nagy L, Privalsky ML, Nakatani Y, Evans RM: Nuclear receptor coactivator ACTR is a novel histone acetyltransferase and forms a multimeric activation complex with P/CAF and CBP/p300. Cell. 1997 Aug 8;90(3):569-80. [PubMed Link Image]
Target 7 Drug References
  1. Baumann L, Vujevich J, Halem M, Martin LK, Kerdel F, Lazarus M, Pacheco H, Black L, Bryde J: Open-label pilot study of alitretinoin gel 0.1% in the treatment of photoaging. Cutis. 2005 Jul;76(1):69-73. [PubMed Link Image]
  2. Milliano MT, Luxon BA: Rat hepatic stellate cells become retinoid unresponsive during activation. Hepatol Res. 2005 Nov;33(3):225-33. Epub 2005 Oct 25. [PubMed Link Image]
  3. Rasooly R, Schuster GU, Gregg JP, Xiao JH, Chandraratna RA, Stephensen CB: Retinoid x receptor agonists increase bcl2a1 expression and decrease apoptosis of naive T lymphocytes. J Immunol. 2005 Dec 15;175(12):7916-29. [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. Ritter M, Kattmann D, Teichler S, Hartmann O, Samuelsson MK, Burchert A, Bach JP, Kim TD, Berwanger B, Thiede C, Jager R, Ehninger G, Schafer H, Ueki N, Hayman MJ, Eilers M, Neubauer A: Inhibition of retinoic acid receptor signaling by Ski in acute myeloid leukemia. Leukemia. 2006 Mar;20(3):437-43. [PubMed Link Image]
Drug Target 8 [top]
Target 8 ID 780
Target 8 Name Retinoic acid receptor RXR-gamma
Target 8 Synonyms
  1. Retinoid X receptor gamma
Target 8 Gene Name RXRG
Target 8 Protein Sequence >Retinoic acid receptor RXR-gamma 
MYGNYSHFMKFPAGYGGSPGHTGSTSMSPSAALSTGKPMDSHPSYTDTPVSAPRTLSAVG
TPLNALGSPYRVITSAMGPPSGALAAPPGINLVAPPSSQLNVVNSVSSSEDIKPLPGLPG
IGNMNYPSTSPGSLVKHICAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLIYTCRDNKD
CLIDKRQRNRCQYCRYQKCLVMGMKREAVQEERQRSRERAESEAECATSGHEDMPVERIL
EAELAVEPKTESYGDMNMENSTNDPVTNICHAADKQLFTLVEWAKRIPHFSDLTLEDQVI
LLRAGWNELLIASFSHRSVSVQDGILLATGLHVHRSSAHSAGVGSIFDRVLTELVSKMKD
MQMDKSELGCLRAIVLFNPDAKGLSNPSEVETLREKVYATLEAYTKQKYPEQPGRFAKLL
LRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLETPLQIT
Target 8 Number of Residues 470
Target 8 Molecular Weight 50872
Target 8 Theoretical pI 7.67
Target 8 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 8 General Function Involved in transcription factor activity
Target 8 Specific Function Nuclear hormone receptor. Involved in the retinoic acid response pathway. Binds 9-cis retinoic acid (9C-RA)
Target 8 Pathways Not Available
Target 8 Reactions Not Available
Target 8 Pfam Domain Function
Target 8 Signals
  • None
Target 8 Transmembrane Regions
  • None
Target 8 Essentiality Non-Essential
Target 8 GenBank ID Protein 1053069 Link Image
Target 8 UniProtKB/Swiss-Prot ID P48443 Link Image
Target 8 UniProtKB/Swiss-Prot Entry Name RXRG_HUMAN Link Image
Target 8 PDB ID Not Available
Target 8 Cellular Location
  • Nucleus
Target 8 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 8 GenBank Gene ID
Target 8 GeneCard ID RXRG Link Image
Target 8 GenAtlas ID RXRG Link Image
Target 8 HGNC ID HGNC:10479 Link Image
Target 8 Chromosome Location 1
Target 8 Locus 1q22-q23
Target 8 SNPs SNPJam Report Link Image
Target 8 General References Not Available
Target 8 Drug References
  1. 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]
  2. Adamczewski Z, Makarewicz J, Mikosinski S, Knapska-Kucharska M, Gunerska-Szadkowska A, Oszukowska L, Karwowska A, Lewinski A: [Application of 13-cis-retinoic acid in patients with 131I scintigraphically-negative metastases of differentiated thyroid carcinoma] Endokrynol Pol. 2006 Jul-Aug;57(4):403-6. [PubMed Link Image]
  3. Germain P, Chambon P, Eichele G, Evans RM, Lazar MA, Leid M, De Lera AR, Lotan R, Mangelsdorf DJ, Gronemeyer H: International Union of Pharmacology. LXIII. Retinoid X receptors. Pharmacol Rev. 2006 Dec;58(4):760-72. [PubMed Link Image]
  4. 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]
  5. Brtko J: Role of retinoids and their cognate nuclear receptors in breast cancer chemoprevention. Cent Eur J Public Health. 2007 Mar;15(1):3-6. [PubMed Link Image]
Drug Target 9 [top]
Target 9 ID 859
Target 9 Name Cellular retinoic acid-binding protein 2
Target 9 Synonyms
  1. CRABP-II
  2. Cellular retinoic acid- binding protein II
  3. Retinoic acid-binding protein II, cellular
Target 9 Gene Name CRABP2
Target 9 Protein Sequence >Cellular retinoic acid-binding protein 2 
PNFSGNWKIIRSENFEELLKVLGVNVMLRKIAVAAASKPAVEIKQEGDTFYIKTSTTVRT
TEINFKVGEEFEEQTVDGRPCKSLVKWESENKMVCEQKLLKGEGPKTSWTRELTNDGELI
LTMTADDVVCTRVYVRE
Target 9 Number of Residues 139
Target 9 Molecular Weight 15562
Target 9 Theoretical pI 5.07
Target 9 GO Classification
Function
lipid binding
binding
Process
physiological process
cellular physiological process
transport
Component
Not Available
Target 9 General Function Involved in retinoid binding
Target 9 Specific Function Cytosolic CRABPs may regulate the access of retinoic acid to the nuclear retinoic acid receptors. CRABP2 may participate in a regulatory feedback mechanism to control the action of retinoic acid on cell differentiation
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 181026 Link Image
Target 9 UniProtKB/Swiss-Prot ID P29373 Link Image
Target 9 UniProtKB/Swiss-Prot Entry Name RABP2_HUMAN Link Image
Target 9 PDB ID 3CBS Link Image
Target 9 PDB File Show
Target 9 3D Structure
Target 9 Cellular Location
  • Cytoplasm
Target 9 Gene Sequence >417 bp 
ATGCCCAACTTCTCTGGCAACTGGAAAATCATCCGATCGGAAAACTTCGAGGAATTGCTC
AAAGTGCTGGGGGTGAATGTGATGCTGAGGAAGATTGCTGTGGCTGCAGCGTCCAAGCCA
GCAGTGGAGATCAAACAGGAGGGAGACACTTTCTACATCAAAACCTCCACCACCGTGCGC
ACCACAGAGATTAACTTCAAGGTTGGGGAGGAGTTTGAGGAGCAGACTGTGGATGGGAGG
CCCTGTAAGAGCCTGGTGAAATGGGAGAGTGAGAATAAAATGGTCTGTGAGCAGAAGCTC
CTGAAGGGAGAGGGCCCCAAGACCTCGTGGACCAGAGAACTGACCAACGATGGGGAACTG
ATCCTGACCATGACGGCGGATGACGTTGTGTGCACCAGGGTCTACGTCCGAGAGTGA
Target 9 GenBank Gene ID
Target 9 GeneCard ID CRABP2 Link Image
Target 9 GenAtlas ID CRABP2 Link Image
Target 9 HGNC ID HGNC:2339 Link Image
Target 9 Chromosome Location 1
Target 9 Locus 1q21.3
Target 9 SNPs SNPJam Report Link Image
Target 9 General References
  1. Chaudhuri BN, Kleywegt GJ, Broutin-L'Hermite I, Bergfors T, Senn H, Le Motte P, Partouche O, Jones TA: Structures of cellular retinoic acid binding proteins I and II in complex with synthetic retinoids. Acta Crystallogr D Biol Crystallogr. 1999 Nov;55(Pt 11):1850-7. [PubMed Link Image]
  2. Eller MS, Oleksiak MF, McQuaid TJ, McAfee SG, Gilchrest BA: The molecular cloning and expression of two CRABP cDNAs from human skin. Exp Cell Res. 1992 Feb;198(2):328-36. [PubMed Link Image]
  3. Astrom A, Pettersson U, Voorhees JJ: Structure of the human cellular retinoic acid-binding protein II gene. Early transcriptional regulation by retinoic acid. J Biol Chem. 1992 Dec 15;267(35):25251-5. [PubMed Link Image]
  4. Astrom A, Tavakkol A, Pettersson U, Cromie M, Elder JT, Voorhees JJ: Molecular cloning of two human cellular retinoic acid-binding proteins (CRABP). Retinoic acid-induced expression of CRABP-II but not CRABP-I in adult human skin in vivo and in skin fibroblasts in vitro. J Biol Chem. 1991 Sep 15;266(26):17662-6. [PubMed Link Image]
  5. Kleywegt GJ, Bergfors T, Senn H, Le Motte P, Gsell B, Shudo K, Jones TA: Crystal structures of cellular retinoic acid binding proteins I and II in complex with all-trans-retinoic acid and a synthetic retinoid. Structure. 1994 Dec 15;2(12):1241-58. [PubMed Link Image]
  6. Chen X, Tordova M, Gilliland GL, Wang L, Li Y, Yan H, Ji X: Crystal structure of apo-cellular retinoic acid-binding protein type II (R111M) suggests a mechanism of ligand entry. J Mol Biol. 1998 May 8;278(3):641-53. [PubMed Link Image]
  7. Wang L, Li Y, Abildgaard F, Markley JL, Yan H: NMR solution structure of type II human cellular retinoic acid binding protein: implications for ligand binding. Biochemistry. 1998 Sep 15;37(37):12727-36. [PubMed Link Image]
  8. Wang L, Yan H: NMR study suggests a major role for Arg111 in maintaining the structure and dynamical properties of type II human cellular retinoic acid binding protein. Biochemistry. 1998 Sep 15;37(37):13021-32. [PubMed Link Image]
Target 9 Drug References
  1. 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]
  2. Donato LJ, Noy N: Suppression of mammary carcinoma growth by retinoic acid: proapoptotic genes are targets for retinoic acid receptor and cellular retinoic acid-binding protein II signaling. Cancer Res. 2005 Sep 15;65(18):8193-9. [PubMed Link Image]
  3. Bry K, Lappalainen U: Pathogenesis of bronchopulmonary dysplasia: the role of interleukin 1beta in the regulation of inflammation-mediated pulmonary retinoic acid pathways in transgenic mice. Semin Perinatol. 2006 Jun;30(3):121-8. [PubMed Link Image]
  4. Wei T, Geiser AG, Qian HR, Su C, Helvering LM, Kulkarini NH, Shou J, N'Cho M, Bryant HU, Onyia JE: DNA microarray data integration by ortholog gene analysis reveals potential molecular mechanisms of estrogen-dependent growth of human uterine fibroids. BMC Womens Health. 2007 Apr 2;7:5. [PubMed Link Image]
  5. Boorjian SA, Milowsky MI, Kaplan J, Albert M, Cobham MV, Coll DM, Mongan NP, Shelton G, Petrylak D, Gudas LJ, Nanus DM: Phase 1/2 clinical trial of interferon alpha2b and weekly liposome-encapsulated all-trans retinoic acid in patients with advanced renal cell carcinoma. J Immunother (1997). 2007 Sep;30(6):655-62. [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.