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Version 2.5
Creation Date 2005-06-13 13:24:05
Update Date 2009-02-19 16:03:45
Primary Accession Number DB01032
Secondary Accession Number
  • APRD00167
Name Probenecid
Drug Type
  • Approved
  • Small Molecule
Description The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy. [PubChem]
Synonyms Not Available
Brand Names
  1. Apurina
  2. Benecid
  3. Benemid
  4. Benuryl
  5. Col-Probenecid
  6. Colbenemid
  7. Polycillin-PRB
  8. Probalan
  9. Probampacin
  10. Probecid
  11. Proben
  12. Proben-C
  13. Probenecid Acid
  14. Probenemid
  15. Probexin
  16. Prolongine
  17. Synergid R
  18. Tubophan
  19. Uricosid
Brand Mixtures Not Available
Chemical IUPAC Name 4-(dipropylsulfamoyl)benzoic acid
Chemical Formula C13H19NO4S
Chemical Structure Structure
CAS Registry Number 57-66-9
InChI Identifier InChI=1/C13H19NO4S/c1-3-9-14(10-4-2)19(17,18)12-7-5-11(6-8-12)13(15)16/h5-8H,3-4,9-10H2,1-2H3,(H,15,16)/f/h15H
InChI Key DBABZHXKTCFAPX-YAQRNVERCP
KEGG Drug D00475 Link Image
KEGG Compound C07372 Link Image
PubChem Compound 4911 Link Image
PubChem Substance 9576 Link Image
ChEBI ID Not Available
PharmGKB ID PA451106 Link Image
HET ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 00294926 Link Image
RxList Link http://www.rxlist.com/cgi/generic/colbenemid.htm Link Image
PDRhealth Link Not Available
Wikipedia Link http://en.wikipedia.org/wiki/Probenecid Link Image
FDA Label Not Available
Material Safety Data Sheet (MSDS)
Synthesis Reference Not Available
Average Molecular Weight 285.3590
Monoisotopic Molecular Weight 285.1035
State Solid
Melting Point 195 oC
Experimental Water Solubility 27.1 mg/L Source: PhysProp
Predicted Water Solubility 4.25e-01 mg/mL Calculated using ALOGPS
Experimental LogP/Hydrophobicity 2.3 Source: PhysProp
Predicted LogP 1.52 Calculated using ALOGPS
Experimental LogS Not Available
Predicted LogS -2.83 Calculated using ALOGPS
Experimental Caco2 Permeability Not Available
pKa/Isoelectric Point 3.4
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 CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(O)=O
Canonical SMILES CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(O)=O
Drug Category
  • Adjuvants, Pharmaceutic
  • Uricosuric Agents
ATC Codes
AHFS Codes
  • 40:40.00
Indication For the treatment of gout and high levels of uric acid in the blood
Pharmacology Probenecid is a uricosuric and renal tubular blocking agent and is used in combination with colchicine to treat chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout. It inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits.
Mechanism of Action Probenecid inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels.
Absorption Not Available
Toxicity Not Available
Protein Binding 75-95%
Biotransformation Not Available
Half Life 6-12 hours
Dosage Forms
Form Route
Tablet Oral
Patient Information Not Available
Contraindications Show Link Image
Interactions Show Link Image
Drug Interactions
Drug Interaction
Aspirin The salicylate decreases the uricosuric effect of probenecid
Bismuth Subsalicylate The salicylate decreases the uricosuric effect of probenecid
Cefaclor Probenecid increases the antibiotic's level
Cefadroxil Probenecid increases the antibiotic's level
Cefamandole Probenecid increases the antibiotic's level
Cefazolin Probenecid increases the antibiotic's level
Cefepime Probenecid increases the antibiotic's level
Cefixime Probenecid increases the antibiotic's level
Cefmetazole Probenecid increases the antibiotic's level
Cefonicid Probenecid increases the antibiotic's level
Cefotaxime Probenecid increases the antibiotic's level
Cefotetan Probenecid increases the antibiotic's level
Cefoxitin Probenecid increases the antibiotic's level
Cefprozil Probenecid increases the antibiotic's level
Cefradine Probenecid increases the antibiotic's level
Ceftizoxime Probenecid increases the antibiotic's level
Cefuroxime Probenecid increases the antibiotic's level
Cephalexin Probenecid increases the antibiotic's level
Cephaloglycin Probenecid increases the antibiotic's level
Cephalothin Group Probenecid increases the antibiotic's level
Diflunisal Probenecid increases toxicity of diflunisal
Ganciclovir Probenecid increases the effect and toxicity of ganciclovir/valganciclovir
Indomethacin Probenecid increases the effect/toxicity of indomethacin
Ketorolac Probenecid increases toxicity of ketorolac
Loracarbef Probenecid increases the antibiotic's level
Methotrexate Probenecid increases the effect and toxicity of methotrexate
Moxalactam Derivative Probenecid increases the antibiotic's level
Salicylate-magnesium The salicylate decreases the uricosuric effect of probenecid
Salicylate-sodium The salicylate decreases the uricosuric effect of probenecid
Salsalate The salicylate decreases the uricosuric effect of probenecid
Trisalicylate-choline The salicylate decreases the uricosuric effect of probenecid
Valganciclovir Probenecid increases the effect and toxicity of ganciclovir/valganciclovir
Zidovudine Rash, malaise, myalgia
Food Interactions
  • Increase liquid intake, avoid alcohol.
  • Take with food to reduce irritation.
Pathways Not Available
General References
  1. Butler D: Wartime tactic doubles power of scarce bird-flu drug. Nature. 2005 Nov 3;438(7064):6. [PubMed Link Image]
  2. Drugs.com Link Image
  3. Wikipedia Link Image
  4. RxList Link Image
Organisms Affected
  • Humans and other mammals
Targets
  1. Serum albumin
  2. Organic anion transporter 3
  3. Multidrug resistance-associated protein 1
  4. Solute carrier family 22 member 11
Drug Target 1 [top]
Target 1 ID 587
Target 1 Name Serum albumin
Target 1 Synonyms
  1. Serum albumin precursor
Target 1 Gene Name ALB
Target 1 Protein Sequence >Serum albumin precursor 
MKWVTFISLLFLFSSAYSRGVFRRDAHKSEVAHRFKDLGEENFKALVLIAFAQYLQQCPF
EDHVKLVNEVTEFAKTCVADESAENCDKSLHTLFGDKLCTVATLRETYGEMADCCAKQEP
ERNECFLQHKDDNPNLPRLVRPEVDVMCTAFHDNEETFLKKYLYEIARRHPYFYAPELLF
FAKRYKAAFTECCQAADKAACLLPKLDELRDEGKASSAKQRLKCASLQKFGERAFKAWAV
ARLSQRFPKAEFAEVSKLVTDLTKVHTECCHGDLLECADDRADLAKYICENQDSISSKLK
ECCEKPLLEKSHCIAEVENDEMPADLPSLAADFVESKDVCKNYAEAKDVFLGMFLYEYAR
RHPDYSVVLLLRLAKTYETTLEKCCAAADPHECYAKVFDEFKPLVEEPQNLIKQNCELFE
QLGEYKFQNALLVRYTKKVPQVSTPTLVEVSRNLGKVGSKCCKHPEAKRMPCAEDYLSVV
LNQLCVLHEKTPVSDRVTKCCTESLVNRRPCFSALEVDETYVPKEFNAETFTFHADICTL
SEKERQIKKQTALVELVKHKPKATKEQLKAVMDDFAAFVEKCCKADDKETCFAEEGKKLV
AASQAALGL
Target 1 Number of Residues 619
Target 1 Molecular Weight 69367
Target 1 Theoretical pI 6.21
Target 1 GO Classification
Function
transporter activity
carrier activity
Process
physiological process
cellular physiological process
transport
Component
extracellular region
extracellular space
Target 1 General Function Involved in antioxidant activity
Target 1 Specific Function Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood
Target 1 Pathways Not Available
Target 1 Reactions Not Available
Target 1 Pfam Domain Function
Target 1 Signals
  • 1-18
Target 1 Transmembrane Regions
  • None
Target 1 Essentiality Non-Essential
Target 1 GenBank ID Protein 28590 Link Image
Target 1 UniProtKB/Swiss-Prot ID P02768 Link Image
Target 1 UniProtKB/Swiss-Prot Entry Name ALBU_HUMAN Link Image
Target 1 PDB ID 1HA2 Link Image
Target 1 PDB File Show
Target 1 3D Structure
Target 1 Cellular Location
  • Secreted protein
Target 1 Gene Sequence >1830 bp 
ATGAAGTGGGTAACCTTTATTTCCCTTCTTTTTCTCTTTAGCTCGGCTTATTCCAGGGGT
GTGTTTCGTCGAGATGCACACAAGAGTGAGGTTGCTCATCGGTTTAAAGATTTGGGAGAA
GAAAATTTCAAAGCCTTGGTGTTGATTGCCTTTGCTCAGTATCTTCAGCAGTGTCCATTT
GAAGATCATGTAAAATTAGTGAATGAAGTAACTGAATTTGCAAAAACATGTGTTGCTGAT
GAGTCAGCTGAAAATTGTGACAAATCACTTCATACCCTTTTTGGAGACAAATTATGCACA
GTTGCAACTCTTCGTGAAACCTATGGTGAAATGGCTGACTGCTGTGCAAAACAAGAACCT
GGGAGAAATGAATGCTTCTTGCAACACAAAGATGACAACCCAAACCTCCCCCGATTGGTG
AGACCAGAGGTTGATGTGATGTGCACTGCTTTTCATGACAATGAAGAGACATTTTTGAAA
AAATACTTATATGAAATTGCCAGAAGACATCCTTACTTTTATGCCCCGGAACTCCTTTTC
TTTGCTAAAAGGTATAAAGCTGCTTTTACAGAATGTTGCCAAGCTGCTGATAAAGCTGCC
TGCCTGTTGCCAAAGCTCGATGAACTTCGGGATGAAGGGAAGGCTTCGTCTGCCAAACAG
AGACTCAAGTGTGCCAGTCTCCAAAAATTTGGAGAAAGAGCTTTCAAAGCATGGGCAGTA
GCTCGCCTGAGCCAGAGATTTCCCAAAGCTGAGTTTGCAGAAGTTTCCAAGTTAGTGACA
GATCTTACCAAAGTCCACACGGAATGCTGCCATGGAGATCTGCTTGAATGTGCTGATGAC
AGGGCGGACCTTGCCAAGTATATCTGTGAAAATCAAGATTCGATCTCCAGTAAACTGAAG
GAATGCTGTGAAAAACCTCTGTTGGAAAAATCCCACTGCATTGCCGAAGTGGAAAATGAT
GAGATGCCTGCTGACTTGCCTTCATTAGCTGCTGATTTTGTTGAAAGTAAGGATGTTTGC
AAAAACTATGCTGAGGCAAAGGATGTCTTCTTGGGCATGTTTTTGTATGAATATGCAAGA
AGGCATCCTGATTACTCTGTCGTGCTGCTGCTGAGACTTGCCAAGACATATGAAACCACT
CTAGAGAAGTGCTGTGCCGCTGCAGATCCTCATGAATGCTATGCCAAAGTGTTCGATGAA
TTTAAACCTCTTGTGGAAGAGCCTCAGAATTTAATCAAACAAAATTGTGAGCTTTTTGAG
CAGCTTGGAGAGTACAAATTCCAGAATGCGCTGTTAGTTCGTTACACCAAGAAAGTACCC
GAAGTGTCAACTCCAACTCTTGTAGAGGTCTCAAGAAACCTAGGAAAAGTGGGCAGCAAA
TGTTGTAAACATCCTGAAGCAAAAAGAATGCCCTGTGCAGAAGACTATCTATCCGTGGTC
CTGAACCAGTTATGTGTGTTGCATGAGAAAACGCCAGTAAGTGACAGAGTCACCAAATGC
TGCACAGAATCCTTGGTGAACAGGCGACCATGCTTTTCAGCTCTGGAAGTCGATGAAACA
TACGTTCCCAAAGAGTTTAATGCTGAAACATTCACCTTCCATGCAGATATATGCACACTT
TCTGAGAAGGAGAGACAAATCAAGAAACAAACTGCACTTGTTGAGCTCGTGAAACACAAG
CCCAAGGCAACAAAAGAGCAACTGAAAGCTGTTATGGATGATTTCGCTGCTTTTGTAGAG
AAGTGCTGCAAGGCTGACGATAAGGAGACCTGCTTTGCCGAGGAGGGTAAAAAACTTGTT
GCTGCAAGTCAAGCTGCCTTAGGCTTATAA
Target 1 GenBank Gene ID
Target 1 GeneCard ID ALB Link Image
Target 1 GenAtlas ID ALB Link Image
Target 1 HGNC ID HGNC:399 Link Image
Target 1 Chromosome Location 4
Target 1 Locus 4q11-q13
Target 1 SNPs SNPJam Report Link Image
Target 1 General References
  1. Sugio S, Kashima A, Mochizuki S, Noda M, Kobayashi K: Crystal structure of human serum albumin at 2.5 A resolution. Protein Eng. 1999 Jun;12(6):439-46. [PubMed Link Image]
  2. Bhattacharya AA, Curry S, Franks NP: Binding of the general anesthetics propofol and halothane to human serum albumin. High resolution crystal structures. J Biol Chem. 2000 Dec 8;275(49):38731-8. [PubMed Link Image]
  3. Minchiotti L, Campagnoli M, Rossi A, Cosulich ME, Monti M, Pucci P, Kragh-Hansen U, Granel B, Disdier P, Weiller PJ, Galliano M: A nucleotide insertion and frameshift cause albumin Kenitra, an extended and O-glycosylated mutant of human serum albumin with two additional disulfide bridges. Eur J Biochem. 2001 Jan;268(2):344-52. [PubMed Link Image]
  4. Yu Y, Zhang C, Zhou G, Wu S, Qu X, Wei H, Xing G, Dong C, Zhai Y, Wan J, Ouyang S, Li L, Zhang S, Zhou K, Zhang Y, Wu C, He F: Gene expression profiling in human fetal liver and identification of tissue- and developmental-stage-specific genes through compiled expression profiles and efficient cloning of full-length cDNAs. Genome Res. 2001 Aug;11(8):1392-403. [PubMed Link Image]
  5. Spahr CS, Davis MT, McGinley MD, Robinson JH, Bures EJ, Beierle J, Mort J, Courchesne PL, Chen K, Wahl RC, Yu W, Luethy R, Patterson SD: Towards defining the urinary proteome using liquid chromatography-tandem mass spectrometry. I. Profiling an unfractionated tryptic digest. Proteomics. 2001 Jan;1(1):93-107. [PubMed Link Image]
  6. Petitpas I, Grune T, Bhattacharya AA, Curry S: Crystal structures of human serum albumin complexed with monounsaturated and polyunsaturated fatty acids. J Mol Biol. 2001 Dec 14;314(5):955-60. [PubMed Link Image]
  7. Meloun B, Moravek L, Kostka V: Complete amino acid sequence of human serum albumin. FEBS Lett. 1975 Oct 15;58(1):134-7. [PubMed Link Image]
  8. Gevaert K, Goethals M, Martens L, Van Damme J, Staes A, Thomas GR, Vandekerckhove J: Exploring proteomes and analyzing protein processing by mass spectrometric identification of sorted N-terminal peptides. Nat Biotechnol. 2003 May;21(5):566-9. Epub 2003 Mar 31. [PubMed Link Image]
  9. Clark HF, Gurney AL, Abaya E, Baker K, Baldwin D, Brush J, Chen J, Chow B, Chui C, Crowley C, Currell B, Deuel B, Dowd P, Eaton D, Foster J, Grimaldi C, Gu Q, Hass PE, Heldens S, Huang A, Kim HS, Klimowski L, Jin Y, Johnson S, Lee J, Lewis L, Liao D, Mark M, Robbie E, Sanchez C, Schoenfeld J, Seshagiri S, Simmons L, Singh J, Smith V, Stinson J, Vagts A, Vandlen R, Watanabe C, Wieand D, Woods K, Xie MH, Yansura D, Yi S, Yu G, Yuan J, Zhang M, Zhang Z, Goddard A, Wood WI, Godowski P, Gray A: The secreted protein discovery initiative (SPDI), a large-scale effort to identify novel human secreted and transmembrane proteins: a bioinformatics assessment. Genome Res. 2003 Oct;13(10):2265-70. Epub 2003 Sep 15. [PubMed Link Image]
  10. Minchiotti L, Galliano M, Stoppini M, Ferri G, Crespeau H, Rochu D, Porta F: Two alloalbumins with identical electrophoretic mobility are produced by differently charged amino acid substitutions. Biochim Biophys Acta. 1992 Mar 12;1119(3):232-8. [PubMed Link Image]
  11. 1518850 Carlson J, Sakamoto Y, Laurell CB, Madison J, Watkins S, Putnam FW: Alloalbuminemia in Sweden: structural study and phenotypic distribution of nine albumin variants. Proc Natl Acad Sci U S A. 1992 Sep 1;89(17):8225-9.
  12. 1630489 He XM, Carter DC: Atomic structure and chemistry of human serum albumin. Nature. 1992 Jul 16;358(6383):209-15.
  13. 1859851 Peach RJ, Brennan SO: Structural characterization of a glycoprotein variant of human serum albumin: albumin Casebrook (494 Asp----Asn). Biochim Biophys Acta. 1991 Jul 26;1097(1):49-54.
  14. 1946412 Madison J, Arai K, Sakamoto Y, Feld RD, Kyle RA, Watkins S, Davis E, Matsuda Y, Amaki I, Putnam FW: Genetic variants of serum albumin in Americans and Japanese. Proc Natl Acad Sci U S A. 1991 Nov 1;88(21):9853-7.
  15. 2068071 Watkins S, Madison J, Davis E, Sakamoto Y, Galliano M, Minchiotti L, Putnam FW: A donor splice mutation and a single-base deletion produce two carboxyl-terminal variants of human serum albumin. Proc Natl Acad Sci U S A. 1991 Jul 15;88(14):5959-63.
  16. 2104980 Brennan SO, Myles T, Peach RJ, Donaldson D, George PM: Albumin Redhill (-1 Arg, 320 Ala----Thr): a glycoprotein variant of human serum albumin whose precursor has an aberrant signal peptidase cleavage site. Proc Natl Acad Sci U S A. 1990 Jan;87(1):26-30.
  17. 2247440 Galliano M, Minchiotti L, Porta F, Rossi A, Ferri G, Madison J, Watkins S, Putnam FW: Mutations in genetic variants of human serum albumin found in Italy. Proc Natl Acad Sci U S A. 1990 Nov;87(22):8721-5.
  18. 2374930 Carter DC, He XM: Structure of human serum albumin. Science. 1990 Jul 20;249(4966):302-3.
  19. 2404284 Arai K, Madison J, Shimizu A, Putnam FW: Point substitutions in albumin genetic variants from Asia. Proc Natl Acad Sci U S A. 1990 Jan;87(1):497-501.
  20. 2419329 Urano Y, Watanabe K, Sakai M, Tamaoki T: The human albumin gene. Characterization of the 5' and 3' flanking regions and the polymorphic gene transcripts. J Biol Chem. 1986 Mar 5;261(7):3244-51.
  21. 2437111 Carraway RE, Mitra SP, Cochrane DE: Structure of a biologically active neurotensin-related peptide obtained from pepsin-treated albumin(s). J Biol Chem. 1987 May 5;262(13):5968-73.
  22. 2727704 Carter DC, He XM, Munson SH, Twigg PD, Gernert KM, Broom MB, Miller TY: Three-dimensional structure of human serum albumin. Science. 1989 Jun 9;244(4909):1195-8.
  23. 2762316 Arai K, Madison J, Huss K, Ishioka N, Satoh C, Fujita M, Neel JV, Sakurabayashi I, Putnam FW: Point substitutions in Japanese alloalbumins. Proc Natl Acad Sci U S A. 1989 Aug;86(16):6092-6.
  24. 2911589 Arai K, Ishioka N, Huss K, Madison J, Putnam FW: Identical structural changes in inherited albumin variants from different populations. Proc Natl Acad Sci U S A. 1989 Jan;86(2):434-8.
  25. 3009475 Minghetti PP, Ruffner DE, Kuang WJ, Dennison OE, Hawkins JW, Beattie WG, Dugaiczyk A: Molecular structure of the human albumin gene is revealed by nucleotide sequence within q11-22 of chromosome 4. J Biol Chem. 1986 May 25;261(15):6747-57.
  26. 3087352 Mogard MH, Kobayashi R, Chen CF, Lee TD, Reeve JR Jr, Shively JE, Walsh JH: The amino acid sequence of kinetensin, a novel peptide isolated from pepsin-treated human plasma: homology with human serum albumin, neurotensin and angiotensin. Biochem Biophys Res Commun. 1986 May 14;136(3):983-8.
  27. 3474609 Takahashi N, Takahashi Y, Blumberg BS, Putnam FW: Amino acid substitutions in genetic variants of human serum albumin and in sequences inferred from molecular cloning. Proc Natl Acad Sci U S A. 1987 Jul;84(13):4413-7.
  28. 3479777 Takahashi N, Takahashi Y, Isobe T, Putnam FW, Fujita M, Satoh C, Neel JV: Amino acid substitutions in inherited albumin variants from Amerindian and Japanese populations. Proc Natl Acad Sci U S A. 1987 Nov;84(22):8001-5.
  29. 3828358 Brennan SO, Herbert P: Albumin Canterbury (313 Lys----Asn). A point mutation in the second domain of serum albumin. Biochim Biophys Acta. 1987 Apr 8;912(2):191-7.
  30. 6171778 Lawn RM, Adelman J, Bock SC, Franke AE, Houck CM, Najarian RC, Seeburg PH, Wion KL: The sequence of human serum albumin cDNA and its expression in E. coli. Nucleic Acids Res. 1981 Nov 25;9(22):6103-114.
  31. 6275391 Dugaiczyk A, Law SW, Dennison OE: Nucleotide sequence and the encoded amino acids of human serum albumin mRNA. Proc Natl Acad Sci U S A. 1982 Jan;79(1):71-5.
  32. 656055 Jacobsen C: Lysine residue 240 of human serum albumin is involved in high-affinity binding of bilirubin. Biochem J. 1978 May 1;171(2):453-9.
  33. 7852505 Rushbrook JI, Becker E, Schussler GC, Divino CM: Identification of a human serum albumin species associated with familial dysalbuminemic hyperthyroxinemia. J Clin Endocrinol Metab. 1995 Feb;80(2):461-7.
  34. 7895732 Corbett JM, Wheeler CH, Baker CS, Yacoub MH, Dunn MJ: The human myocardial two-dimensional gel protein database: update 1994. Electrophoresis. 1994 Nov;15(11):1459-65.
  35. 7902134 Galliano M, Minchiotti L, Iadarola P, Stoppini M, Giagnoni P, Watkins S, Madison J, Putnam FW: Protein and DNA sequence analysis of a 'private' genetic variant: albumin Ortonovo (Glu-505-->Lys). Biochim Biophys Acta. 1993 Nov 25;1225(1):27-32.
  36. 8022807 Madison J, Galliano M, Watkins S, Minchiotti L, Porta F, Rossi A, Putnam FW: Genetic variants of human serum albumin in Italy: point mutants and a carboxyl-terminal variant. Proc Natl Acad Sci U S A. 1994 Jul 5;91(14):6476-80.
  37. 8048949 Sunthornthepvarakul T, Angkeow P, Weiss RE, Hayashi Y, Refetoff S: An identical missense mutation in the albumin gene results in familial dysalbuminemic hyperthyroxinemia in 8 unrelated families. Biochem Biophys Res Commun. 1994 Jul 29;202(2):781-7.
  38. 8347685 Brennan SO, Fellowes AP: Albumin Hawkes Bay; a low level variant caused by loss of a sulphydryl group at position 177. Biochim Biophys Acta. 1993 Aug 4;1182(1):46-50.
  39. 8513793 Minchiotti L, Galliano M, Zapponi MC, Tenni R: The structural characterization and bilirubin-binding properties of albumin Herborn, a [Lys240-->Glu] albumin mutant. Eur J Biochem. 1993 Jun 1;214(2):437-44.
  40. 9329347 Wada N, Chiba H, Shimizu C, Kijima H, Kubo M, Koike T: A novel missense mutation in codon 218 of the albumin gene in a distinct phenotype of familial dysalbuminemic hyperthyroxinemia in a Japanese kindred. J Clin Endocrinol Metab. 1997 Oct;82(10):3246-50.
  41. 955075 Walker JE: Lysine residue 199 of human serum albumin is modified by acetylsalicyclic acid. FEBS Lett. 1976 Jul 15;66(2):173-5.
  42. 9589637 Sunthornthepvarakul T, Likitmaskul S, Ngowngarmratana S, Angsusingha K, Kitvitayasak S, Scherberg NH, Refetoff S: Familial dysalbuminemic hypertriiodothyroninemia: a new, dominantly inherited albumin defect. J Clin Endocrinol Metab. 1998 May;83(5):1448-54.
  43. 9731778 Curry S, Mandelkow H, Brick P, Franks N: Crystal structure of human serum albumin complexed with fatty acid reveals an asymmetric distribution of binding sites. Nat Struct Biol. 1998 Sep;5(9):827-35.
Target 1 Drug References
  1. Hansen-Moller J, Schmit U: Rapid high-performance liquid chromatographic assay for the simultaneous determination of probenecid and its glucuronide in urine. Irreversible binding of probenecid to serum albumin. J Pharm Biomed Anal. 1991;9(1):65-73. [PubMed Link Image]
  2. Dundee JW, Halliday NJ, McMurray TJ: Aspirin and probenecid pretreatment influences the potency of thiopentone and the onset of action of midazolam. Eur J Anaesthesiol. 1986 May;3(3):247-51. [PubMed Link Image]
  3. Gewirtz DA, Holt SA: Protein binding as a component of drug interaction in cellular pharmacokinetic studies. Effects of probenecid on transport and accumulation of methotrexate in Ehrlich ascites tumor cells in vitro. Biochem Pharmacol. 1985 Mar 15;34(6):747-54. [PubMed Link Image]
  4. Alberghina M, Infarinato S, Anfuso CD, Lupo G: 1-Acyl-2-lysophosphatidylcholine transport across the blood-retina and blood-brain barrier. FEBS Lett. 1994 Sep 5;351(2):181-5. [PubMed Link Image]
Drug Target 2 [top]
Target 2 ID 747
Target 2 Name Organic anion transporter 3
Target 2 Synonyms Not Available
Target 2 Gene Name SLC22A8
Target 2 Protein Sequence >Organic anion transporter 3 
MTFSEILDRVGSMGHFQFLHVAILGLPILNMANHNLLQIFTAATPVHHCRPPHNASTGPW
VLPMGPNGKPERCLRFVHPPNASLPNDTQRAMEPCLDGWVYNSTKDSIVTEWDLVCNSNK
LKEMAQSIFMAGILIGGLVLGDLSDRFGRTILTCSYLLLAASGSGAAFSPTFPIYMVFRF
LCGFGISGITLSTVILNVEWVPTRMRAIMSTALGYCYTFGQFILPGLAYAIPQWRWLQLT
VSIPFFVFFLSSWWTPESIRWWSCLEVLEGPEDTPAGGCLQWQEEGERLSLEELKLNLQK
EISLAKAKYTASDLFRIPIGAPHDLLLSLAWFATGFAYYSLAMGVEEFGVNLYILQIIFG
GVDVPAKFITILSLSYLGRHTTQGRCPAPGRGAILALTFVPLDLQTVETVLAVFGKGCLS
SSFSCLFLYTSELYPTVIRQTGMGVSNLWTRVGSMVSPLVKITGEVQPFIPNIIFTGSTA
LLGGSAALFLPETLNSPCQRRSKTWKTGQSLPLAPSVLLPGEAGLGPGLFLSSLSLGLRA
KKPKQEPEVEKASQRIPLQPHGPGLGSS
Target 2 Number of Residues 577
Target 2 Molecular Weight 62071
Target 2 Theoretical pI 7.82
Target 2 GO Classification
Function
transporter activity
Process
physiological process
cellular physiological process
transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 2 General Function Carbohydrate transport and metabolism
Target 2 Specific Function Not Available
Target 2 Pathways Not Available
Target 2 Reactions Not Available
Target 2 Pfam Domain Function
Target 2 Signals
  • None
Target 2 Transmembrane Regions
  • 124-143; 150-172; 176-198; 210-232; 236-255; 325-344; 354-376
Target 2 Essentiality Non-Essential
Target 2 GenBank ID Protein 4378059 Link Image
Target 2 UniProtKB/Swiss-Prot ID O95820 Link Image
Target 2 UniProtKB/Swiss-Prot Entry Name O95820_HUMAN Link Image
Target 2 PDB ID Not Available
Target 2 Cellular Location Not Available
Target 2 Gene Sequence >1707 bp 
ATGACCTTCTCGGAGATCCTGGACCGTGTGGGAAGCATGGGCCATTTCCAGTTCCTGCAT
GTAGCCATACTGGGCCTCCCGATCCTCAACATGGCCAACCACAACCTGCTGCAGATCTTC
ACAGCCGCCACCCCTGTCCACCACTGTCGCCCGCCCCACAATGCCTCCACAGGGCCTTGG
GTGCTCCCCATGGGCCCAAATGGGAAGCCTGAGAGGTGCCTCCGTTTTGTACATCCGCCC
AATGCCAGCCTGCCCAATGACACCCAGAGGGCCATGGAGCCATGCCTGGATGGCTGGGTC
TACAACAGCACCAAGGACTCCATTGTGACAGAGTGGGACTTGGTGTGCAACTCCAACAAA
CTGAAGGAGATGGCCCAGTCTATCTTCATGGCAGGTATACTGATTGGAGGGCTCGTGCTT
GGAGACCTGTCTGACAGGTTTGGCCGCACCATCCTGACCTGCAGCTACCTGCTGCTGGCA
GCCAGCGGCTCCGGTGCAGCCTTCAGCCCCACCTTCCCCATCTACATGGTCTTCCGCTTC
CTGTGTGGCTTTGGCATCTCAGGCATTACCCTGAGCACCGTCATCTTGAATGTGGAATGG
GTGCCTACCCGGATGCGGGCCATCATGTCGACAGCACTCGGGTACTGCTACACCTTTGGC
CAGTTCATTCTGCCCGGCCTGGCCTACGCCATCCCCCAGTGGCGTTGGCTGCAGTTAACT
GTGTCCATTCCCTTCTTCGTCTTCTTCCTATCATCCTGGTGGACACCAGAGTCCATACGC
TGGTGGTCTTGTCTGGAAGTCCTCGAAGGCCCTGAAGATACTCCGGCGGGTGGCTGTCTT
CAATGGCAAGAAGAGGGAGAAAGGCTCAGCTTGGAGGAGCTCAAACTCAACCTGCAGAAG
GAGATCTCCTTGGCCAAGGCCAAGTACACCGCAAGTGACCTGTTCCGGATACCCATCGGT
GCGCCGCATGACCTTCTGCTTTCCCTGGCCTGGTTTGCTACCGGTTTTGCCTACTATAGT
TTGGCTATGGGTGTGGAAGAATTTGGAGTCAACCTCTACATCCTCCAGATCATCTTTGGT
GGGGTCGATGTCCCAGCCAAGTTCATCACCATCCTCTCCTTAAGCTACCTGGGCCGGCAT
ACCACTCAGGGGCGCTGCCCTGCTCCTGGCAGAGGGGCCATCTTGGCTCTCACCTTTGTG
CCCTTGGACTTGCAGACCGTGGAGACAGTATTGGCTGTGTTTGGGAAGGGATGCCTATCC
AGCTCCTTCAGCTGCCTCTTCCTCTACACAAGTGAATTATACCCCACAGTCATCAGGCAA
ACAGGTATGGGCGTAAGTAACCTGTGGACCCGCGTGGGAAGCATGGTGTCCCCGCTGGTG
AAAATCACGGGTGAGGTACAGCCCTTCATCCCCAATATCATCTTTACGGGATCTACCGCC
CTCCTCGGGGGCAGTGCTGCCCTCTTCCTGCCTGAGACCCTGAACAGCCCTTGCCAGAGA
CGATCGAAGACCTGGAAAACTGGTCAGTCACTGCCTCTGGCCCCATCAGTGCTCCTCCCT
GGGGAAGCAGGTCTGGGCCCAGGGCTTTTCCTTAGCTCTCTGTCCCTAGGTCTGCGGGCA
AAGAAGCCAAAGCAGGAGCCAGAGGTGGAAAAGGCCTCCCAGAGGATCCCTCTACAGCCT
CACGGACCAGGCCTGGGCTCCAGCTGA
Target 2 GenBank Gene ID
Target 2 GeneCard ID SLC22A8 Link Image
Target 2 GenAtlas ID SLC22A8 Link Image
Target 2 HGNC ID HGNC:10972 Link Image
Target 2 Chromosome Location 11
Target 2 Locus 11q11
Target 2 SNPs SNPJam Report Link Image
Target 2 General References
  1. Race JE, Grassl SM, Williams WJ, Holtzman EJ: Molecular cloning and characterization of two novel human renal organic anion transporters (hOAT1 and hOAT3). Biochem Biophys Res Commun. 1999 Feb 16;255(2):508-14. [PubMed Link Image]
Target 2 Drug References
  1. Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. [PubMed Link Image]
  2. Takeda M, Narikawa S, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters. Eur J Pharmacol. 2001 May 11;419(2-3):113-20. [PubMed Link Image]
  3. Jung KY, Takeda M, Kim DK, Tojo A, Narikawa S, Yoo BS, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of ochratoxin A transport by human organic anion transporters. Life Sci. 2001 Sep 21;69(18):2123-35. [PubMed Link Image]
  4. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. [PubMed Link Image]
  5. Sweet DH, Chan LM, Walden R, Yang XP, Miller DS, Pritchard JB: Organic anion transporter 3 (Slc22a8) is a dicarboxylate exchanger indirectly coupled to the Na+ gradient. Am J Physiol Renal Physiol. 2003 Apr;284(4):F763-9. Epub 2002 Dec 17. [PubMed Link Image]
Drug Target 3 [top]
Target 3 ID 862
Target 3 Name Multidrug resistance-associated protein 1
Target 3 Synonyms
  1. ATP-binding cassette sub- family C member 1
  2. LTC4 transporter
  3. Leukotriene C(4
Target 3 Gene Name ABCC1
Target 3 Protein Sequence >Multidrug resistance-associated protein 1 
MALRGFCSADGSDPLWDWNVTWNTSNPDFTKCFQNTVLVWVPCFYLWACFPFYFLYLSRH
DRGYIQMTPLNKTKTALGFLLWIVCWADLFYSFWERSRGIFLAPVFLVSPTLLGITTLLA
TFLIQLERRKGVQSSGIMLTFWLVALVCALAILRSKIMTALKEDAQVDLFRDITFYVYFS
LLLIQLVLSCFSDRSPLFSETIHDPNPCPESSASFLSRITFWWITGLIVRGYRQPLEGSD
LWSLNKEDTSEQVVPVLVKNWKKECAKTRKQPVKVVYSSKDPAQPKESSKVDANEEVEAL
IVKSPQKEWNPSLFKVLYKTFGPYFLMSFFFKAIHDLMMFSGPQILKLLIKFVNDTKAPD
WQGYFYTVLLFVTACLQTLVLHQYFHICFVSGMRIKTAVIGAVYRKALVITNSARKSSTV
GEIVNLMSVDAQRFMDLATYINMIWSAPLQVILALYLLWLNLGPSVLAGVAVMVLMVPVN
AVMAMKTKTYQVAHMKSKDNRIKLMNEILNGIKVLKLYAWELAFKDKVLAIRQEELKVLK
KSAYLSAVGTFTWVCTPFLVALCTFAVYVTIDENNILDAQTAFVSLALFNILRFPLNILP
MVISSIVQASVSLKRLRIFLSHEELEPDSIERRPVKDGGGTNSITVRNATFTWARSDPPT
LNGITFSIPEGALVAVVGQVGCGKSSLLSALLAEMDKVEGHVAIKGSVAYVPQQAWIQND
SLRENILFGCQLEEPYYRSVIQACALLPDLEILPSGDRTEIGEKGVNLSGGQKQRVSLAR
AVYSNADIYLFDDPLSAVDAHVGKHIFENVIGPKGMLKNKTRILVTHSMSYLPQVDVIIV
MSGGKISEMGSYQELLARDGAFAEFLRTYASTEQEQDAEENGVTGVSGPGKEAKQMENGM
LVTDSAGKQLQRQLSSSSSYSGDISRHHNSTAELQKAEAKKEETWKLMEADKAQTGQVKL
SVYWDYMKAIGLFISFLSIFLFMCNHVSALASNYWLSLWTDDPIVNGTQEHTKVRLSVYG
ALGISQGIAVFGYSMAVSIGGILASRCLHVDLLHSILRSPMSFFERTPSGNLVNRFSKEL
DTVDSMIPEVIKMFMGSLFNVIGACIVILLATPIAAIIIPPLGLIYFFVQRFYVASSRQL
KRLESVSRSPVYSHFNETLLGVSVIRAFEEQERFIHQSDLKVDENQKAYYPSIVANRWLA
VRLECVGNCIVLFAALFAVISRHSLSAGLVGLSVSYSLQVTTYLNWLVRMSSEMETNIVA
VERLKEYSETEKEAPWQIQETAPPSSWPQVGRVEFRNYCLRYREDLDFVLRHINVTINGG
EKVGIVGRTGAGKSSLTLGLFRINESAEGEIIIDGINIAKIGLHDLRFKITIIPQDPVLF
SGSLRMNLDPFSQYSDEEVWTSLELAHLKDFVSALPDKLDHECAEGGENLSVGQRQLVCL
ARALLRKTKILVLDEATAAVDLETDDLIQSTIRTQFEDCTVLTIAHRLNTIMDYTRVIVL
DKGEIQEYGAPSDLLQQRGLFYSMAKDAGLV
Target 3 Number of Residues 1556
Target 3 Molecular Weight 171563
Target 3 Theoretical pI 7.11
Target 3 GO Classification
Function
transporter activity
ATPase activity
hydrolase activity, acting on acid anhydrides, catalyzing transmembrane movement of substances
ATPase activity, coupled to transmembrane movement of substances
purine nucleotide binding
adenyl nucleotide binding
ATP binding
catalytic activity
hydrolase activity
hydrolase activity, acting on acid anhydrides
hydrolase activity, acting on acid anhydrides, in phosphorus-containing anhydrides
pyrophosphatase activity
nucleoside-triphosphatase activity
binding
nucleotide binding
Process
physiological process
cellular physiological process
transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 3 General Function Drug defense mechanisms
Target 3 Specific Function May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Confers resistance to anticancer drugs. Transports LTC4. May protect milk against xenobiotics
Target 3 Pathways Not Available
Target 3 Reactions Not Available
Target 3 Pfam Domain Function
Target 3 Signals
  • None
Target 3 Transmembrane Regions
  • 34-54
  • 75-95
  • 101-121
  • 134-154
  • 173-193
  • 317-337
  • 364-384
  • 441-461
  • 465-485
  • 548-568
  • 591-611
  • 968-988
  • 1026-1046
  • 1090-1110
  • 1112-1132
  • 1204-1224
  • 1227-1247
Target 3 Essentiality Non-Essential
Target 3 GenBank ID Protein 1835659 Link Image
Target 3 UniProtKB/Swiss-Prot ID P33527 Link Image
Target 3 UniProtKB/Swiss-Prot Entry Name MRP1_HUMAN Link Image
Target 3 PDB ID Not Available
Target 3 Cellular Location
  • Membrane
  • multi-pass membrane protein
Target 3 Gene Sequence >4596 bp 
ATGGCGCTCCGGGGCTTCTGCAGCGCCGATGGCTCCGACCCGCTCTGGGACTGGAATGTC
ACGTGGAATACCAGCAACCCCGACTTCACCAAGTGCTTTCAGAACACGGTCCTCGTGTGG
GTGCCTTGTTTTTACCTCTGGGCCTGTTTCCCCTTCTACTTCCTCTATCTCTCCCGACAT
GACCGAGGCTACATTCAGATGACACCTCTCAACAAAACCAAAACTGCCTTGGGATTTTTG
CTGTGGATCGTCTGCTGGGCAGACCTCTTCTACTCTTTCTGGGAAAGAAGTCGGGGCATA
TTCCTGGCCCCAGTGTTTCTGGTCAGCCCAACTCTCTTGGGCATCACCACGCTGCTTGCT
ACCTTTTTAATTCAGCTGGAGAGGAGGAAGGGAGTTCAGTCTTCAGGGATCATGCTCACT
TTCTGGCTGGTAGCCCTAGTGTGTGCCCTAGCCATCCTGAGATCCAAAATTATGACAGCC
TTAAAAGAGGATGCCCAGGTGGACCTGTTTCGTGACATCACTTTCTACGTCTACTTTTCC
CTCTTACTCATTCAGCTCGTCTTGTCCTGTTTCTCAGATCGCTCACCCCTGTTCTCGGAA
ACCATCCACGACCCTAATCCCTGCCCAGAGTCCAGCGCTTCCTTCCTGTCGAGGATCACC
TTCTGGTGGATCACAGGGTTGATTGTCCGGGGCTACCGCCAGCCCCTGGAGGGCAGTGAC
CTCTGGTCCTTAAACAAGGAGGACACGTCGGAACAAGTCGTGCCTGTTTTGGTAAAGAAC
TGGAAGAAGGAATGCGCCAAGACTAGGAAGCAGCCGGTGAAGGTTGTGTACTCCTCCAAG
GATCCTGCCCAGCCGAAAGAGAGTTCCAAGGTGGATGCGAATGAGGAGGTGGAGGCTTTG
ATCGTCAAGTCCCCACAGAAGGAGTGGAACCCCTCTCTGTTTAAGGTGTTATACAAGACC
TTTGGGCCCTACTTCCTCATGAGCTTCTTCTTCAAGGCCATCCACGACCTGATGATGTTT
TCCGGGCCGCAGATCTTAAAGTTGCTCATCAAGTTCGTGAATGACACGAAGGCCCCAGAC
TGGCAGGGCTACTTCTACACCGTGCTGCTGTTTGTCACTGCCTGCCTGCAGACCCTCGTG
CTGCACCAGTACTTCCACATCTGCTTCGTCAGTGGCATGAGGATCAAGACCGCTGTCATT
GGGGCTGTCTATCGGAAGGCCCTGGTGATCACCAATTCAGCCAGAAAATCCTCCACGGTC
GGGGAGATTGTCAACCTCATGTCTGTGGACGCTCAGAGGTTCATGGACTTGGCCACGTAC
ATTAACATGATCTGGTCAGCCCCCCTGCAAGTCATCCTTGCTCTCTACCTCCTGTGGCTG
AATCTGGGCCCTTCCGTCCTGGCTGGAGTGGCGGTGATGGTCCTCATGGTGCCCGTCAAT
GCTGTGATGGCGATGAAGACCAAGACGTATCAGGTGGCCCACATGAAGAGCAAAGACAAT
CGGATCAAGCTGATGAACGAAATTCTCAATGGGATCAAAGTGCTAAAGCTTTATGCCTGG
GAGCTGGCATTCAAGGACAAGGTGCTGGCCATCAGGCAGGAGGAGCTGAAGGTGCTGAAG
AAGTCTGCCTACCTGTCAGCCGTGGGCACCTTCACCTGGGTCTGCACGCCCTTTCTGGTG
GCCTTGTGCACATTTGCCGTCTACGTGACCATTGACGAGAACAACATCCTGGATGCCCAG
ACAGCCTTCGTGTCTTTGGCCTTGTTCAACATCCTCCGGTTTCCCCTGAACATTCTCCCC
ATGGTCATCAGCAGCATCGTGCAGGCGAGTGTCTCCCTCAAACGCCTGAGGATCTTTCTC
TCCCATGAGGAGCTGGAACCTGACAGCATCGAGCGACGGCCTGTCAAAGACGGCGGGGGC
ACGAACAGCATCACCGTGAGGAATGCCACATTCACCTGGGCCAGGAGCGACCCTCCCACA
CTGAATGGCATCACCTTCTCCATCCCCGAAGGTGCTTTGGTGGCCGTGGTGGGCCAGGTG
GGCTGCGGAAAGTCGTCCCTGCTCTCAGCCCTCTTGGCTGAGATGGACAAAGTGGAGGGG
CACGTGGCTATCAAGGGCTCCGTGGCCTATGTGCCACAGCAGGCCTGGATTCAGAATGAT
TCTCTCCGAGAAAACATCCTTTTTGGATGTCAGCTGGAGGAACCATATTACAGGTCCGTG
ATACAGGCCTGTGCCCTCCTCCCAGACCTGGAAATCCTGCCCAGTGGGGATCGGACAGAG
ATTGGCGAGAAGGGCGTGAACCTGTCTGGGGGCCAGAAGCAGCGCGTGAGCCTGGCCCGG
GCCGTGTACTCCAACGCTGACATTTACCTCTTCGATGATCCCCTCTCAGCAGTGGATGCC
CATGTGGGAAAACACATCTTTGAAAATGTGATTGGCCCCAAGGGGATGCTGAAGAACAAG
ACGCGGATCTTGGTCACGCACAGCATGAGCTACTTGCCGCAGGTGGACGTCATCATCGTC
ATGAGTGGCGGCAAGATCTCTGAGATGGGCTCCTACCAGGAGCTGCTGGCTCGAGACGGC
GCCTTCGCTGAGTTCCTGCGTACCTATGCCAGCACAGAGCAGGAGCAGGATGCAGAGGAG
AACGGGGTCACGGGCGTCAGCGGTCCAGGGAAGGAAGCAAAGCAAATGGAGAATGGCATG
CTGGTGACGGACAGTGCAGGGAAGCAACTGCAGAGACAGCTCAGCAGCTCCTCCTCCTAT
AGTGGGGACATCAGCAGGCACCACAACAGCACCGCAGAACTGCAGAAAGCTGAGGCCAAG
AAGGAGGAGACCTGGAAGCTGATGGAGGCTGACAAGGCGCAGACAGGGCAGGTCAAGCTT
TCCGTGTACTGGGACTACATGAAGGCCATCGGACTCTTCATCTCCTTCCTCAGCATCTTC
CTTTTCATGTGTAACCATGTGTCCGCGCTGGCTTCCAACTATTGGCTCAGCCTCTGGACT
GATGACCCCATCGTCAACGGGACTCAGGAGCACACGAAAGTCCGGCTGAGCGTCTATGGA
GCCCTGGGCATTTCACAAGGGATCGCCGTGTTTGGCTACTCCATGGCCGTGTCCATCGGG
GGGATCTTGGCTTCCCGCTGTCTGCACGTGGACCTGCTGCACAGCATCCTGCGGTCACCC
ATGAGCTTCTTTGAGCGGACCCCCAGTGGGAACCTGGTGAACCGCTTCTCCAAGGAGCTG
GACACAGTGGACTCCATGATCCCGGAGGTCATCAAGATGTTCATGGGCTCCCTGTTCAAC
GTCATTGGTGCCTGCATCGTTATCCTGCTGGCCACGCCCATCGCCGCCATCATCATCCCG
CCCCTTGGCCTCATCTACTTCTTCGTCCAGAGGTTCTACGTGGCTTCCTCCCGGCAGCTG
AAGCGCCTCGAGTCGGTCAGCCGCTCCCCGGTCTATTCCCATTTCAACGAGACCTTGCTG
GGGGTCAGCGTCATTCGAGCCTTCGAGGAGCAGGAGCGCTTCATCCACCAGAGTGACCTG
AAGGTGGACGAGAACCAGAAGGCCTATTACCCCAGCATCGTGGCCAACAGGTGGCTGGCC
GTGCGGCTGGAGTGTGTGGGCAACTGCATCGTTCTGTTTGCTGCCCTGTTTGCGGTGATC
TCCAGGCACAGCCTCAGTGCTGGCTTGGTGGGCCTCTCAGTGTCTTACTCATTGCAGGTC
ACCACGTACTTGAACTGGCTGGTTCGGATGTCATCTGAAATGGAAACCAACATCGTGGCC
GTGGAGAGGCTCAAGGAGTATTCAGAGACTGAGAAGGAGGCGCCCTGGCAAATCCAGGAG
ACAGCTCCGCCCAGCAGCTGGCCCCAGGTGGGCCGAGTGGAATTCCGGAACTACTGCCTG
CGCTACCGAGAGGACCTGGACTTCGTTCTCAGGCACATCAATGTCACGATCAATGGGGGA
GAAAAGGTCGGCATCGTGGGGCGGACGGGAGCTGGGAAGTCGTCCCTGACCCTGGGCTTA
TTTCGGATCAACGAGTCTGCCGAAGGAGAGATCATCATCGATGGCATCAACATCGCCAAG
ATCGGCCTGCACGACCTCCGCTTCAAGATCACCATCATCCCCCAGGACCCTGTTTTGTTT
TCGGGTTCCCTCCGAATGAACCTGGACCCATTCAGCCAGTACTCGGATGAAGAAGTCTGG
ACGTCCCTGGAGCTGGCCCACCTGAAGGACTTCGTGTCAGCCCTTCCTGACAAGCTAGAC
CATGAATGTGCAGAAGGCGGGGAGAACCTCAGTGTCGGGCAGCGCCAGCTTGTGTGCCTA
GCCCGGGCCCTGCTGAGGAAGACGAAGATCCTTGTGTTGGATGAGGCCACGGCAGCCGTG
GACCTGGAAACGGACGACCTCATCCAGTCCACCATCCGGACACAGTTCGAGGACTGCACC
GTCCTCACCATCGCCCACCGGCTCAACACCATCATGGACTACACAAGGGTGATCGTCTTG
GACAAAGGAGAAATCCAGGAGTACGGCGCCCCATCGGACCTCCTGCAGCAGAGAGGTCTT
TTCTACAGCATGGCCAAAGACGCCGGCTTGGTGTGA
Target 3 GenBank Gene ID
Target 3 GeneCard ID ABCC1 Link Image
Target 3 GenAtlas ID ABCC1 Link Image
Target 3 HGNC ID HGNC:51 Link Image
Target 3 Chromosome Location 16
Target 3 Locus 16p13.1
Target 3 SNPs SNPJam Report Link Image
Target 3 General References
  1. Loftus BJ, Kim UJ, Sneddon VP, Kalush F, Brandon R, Fuhrmann J, Mason T, Crosby ML, Barnstead M, Cronin L, Deslattes Mays A, Cao Y, Xu RX, Kang HL, Mitchell S, Eichler EE, Harris PC, Venter JC, Adams MD: Genome duplications and other features in 12 Mb of DNA sequence from human chromosome 16p and 16q. Genomics. 1999 Sep 15;60(3):295-308. [PubMed Link Image]
  2. Ringpfeil F, Lebwohl MG, Christiano AM, Uitto J: Pseudoxanthoma elasticum: mutations in the MRP6 gene encoding a transmembrane ATP-binding cassette (ABC) transporter. Proc Natl Acad Sci U S A. 2000 May 23;97(11):6001-6. [PubMed Link Image]
  3. Le Saux O, Urban Z, Tschuch C, Csiszar K, Bacchelli B, Quaglino D, Pasquali-Ronchetti I, Pope FM, Richards A, Terry S, Bercovitch L, de Paepe A, Boyd CD: Mutations in a gene encoding an ABC transporter cause pseudoxanthoma elasticum. Nat Genet. 2000 Jun;25(2):223-7. [PubMed Link Image]
  4. Robbiani DF, Finch RA, Jager D, Muller WA, Sartorelli AC, Randolph GJ: The leukotriene C(4) transporter MRP1 regulates CCL19 (MIP-3beta, ELC)-dependent mobilization of dendritic cells to lymph nodes. Cell. 2000 Nov 22;103(5):757-68. [PubMed Link Image]
  5. Perdu J, Germain DP: Identification of novel polymorphisms in the pM5 and MRP1 (ABCC1) genes at locus 16p13.1 and exclusion of both genes as responsible for pseudoxanthoma elasticum. Hum Mutat. 2001;17(1):74-5. [PubMed Link Image]
  6. Ito S, Ieiri I, Tanabe M, Suzuki A, Higuchi S, Otsubo K: Polymorphism of the ABC transporter genes, MDR1, MRP1 and MRP2/cMOAT, in healthy Japanese subjects. Pharmacogenetics. 2001 Mar;11(2):175-84. [PubMed Link Image]
  7. Ito K, Olsen SL, Qiu W, Deeley RG, Cole SP: Mutation of a single conserved tryptophan in multidrug resistance protein 1 (MRP1/ABCC1) results in loss of drug resistance and selective loss of organic anion transport. J Biol Chem. 2001 May 11;276(19):15616-24. Epub 2001 Feb 21. [PubMed Link Image]
  8. Cui L, Hou YX, Riordan JR, Chang XB: Mutations of the Walker B motif in the first nucleotide binding domain of multidrug resistance protein MRP1 prevent conformational maturation. Arch Biochem Biophys. 2001 Aug 1;392(1):153-61. [PubMed Link Image]
  9. Conrad S, Kauffmann HM, Ito K, Deeley RG, Cole SP, Schrenk D: Identification of human multidrug resistance protein 1 (MRP1) mutations and characterization of a G671V substitution. J Hum Genet. 2001;46(11):656-63. [PubMed Link Image]
  10. Cole SP, Bhardwaj G, Gerlach JH, Mackie JE, Grant CE, Almquist KC, Stewart AJ, Kurz EU, Duncan AM, Deeley RG: Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science. 1992 Dec 4;258(5088):1650-4. [PubMed Link Image]
  11. 8098549 Cole SP, Deeley RG: Multidrug resistance-associated protein: sequence correction. Science. 1993 May 14;260(5110):879.
  12. 8649356 Stride BD, Valdimarsson G, Gerlach JH, Wilson GM, Cole SP, Deeley RG: Structure and expression of the messenger RNA encoding the murine multidrug resistance protein, an ATP-binding cassette transporter. Mol Pharmacol. 1996 Jun;49(6):962-71.
  13. 9295302 Hipfner DR, Almquist KC, Leslie EM, Gerlach JH, Grant CE, Deeley RG, Cole SP: Membrane topology of the multidrug resistance protein (MRP). A study of glycosylation-site mutants reveals an extracytosolic NH2 terminus. J Biol Chem. 1997 Sep 19;272(38):23623-30.
  14. 9334225 Kast C, Gros P: Topology mapping of the amino-terminal half of multidrug resistance-associated protein by epitope insertion and immunofluorescence. J Biol Chem. 1997 Oct 17;272(42):26479-87.
  15. 9344662 Grant CE, Kurz EU, Cole SP, Deeley RG: Analysis of the intron-exon organization of the human multidrug-resistance protein gene (MRP) and alternative splicing of its mRNA. Genomics. 1997 Oct 15;45(2):368-78.
  16. 9485377 Kast C, Gros P: Epitope insertion favors a six transmembrane domain model for the carboxy-terminal portion of the multidrug resistance-associated protein. Biochemistry. 1998 Feb 24;37(8):2305-13.
Target 3 Drug References
  1. Hooijberg JH, Broxterman HJ, Kool M, Assaraf YG, Peters GJ, Noordhuis P, Scheper RJ, Borst P, Pinedo HM, Jansen G: Antifolate resistance mediated by the multidrug resistance proteins MRP1 and MRP2. Cancer Res. 1999 Jun 1;59(11):2532-5. [PubMed Link Image]
  2. Legrand O, Simonin G, Beauchamp-Nicoud A, Zittoun R, Marie JP: Simultaneous activity of MRP1 and Pgp is correlated with in vitro resistance to daunorubicin and with in vivo resistance in adult acute myeloid leukemia. Blood. 1999 Aug 1;94(3):1046-56. [PubMed Link Image]
  3. Legrand O, Simonin G, Perrot JY, Zittoun R, Marie JP: Both Pgp and MRP1 activities using calcein-AM contribute to drug resistance in AML. Adv Exp Med Biol. 1999;457:161-75. [PubMed Link Image]
  4. Evers R, de Haas M, Sparidans R, Beijnen J, Wielinga PR, Lankelma J, Borst P: Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83. [PubMed Link Image]
  5. Issandou M, Grand-Perret T: Multidrug resistance P-glycoprotein is not involved in cholesterol esterification. Biochem Biophys Res Commun. 2000 Dec 20;279(2):369-77. [PubMed Link Image]
Drug Target 4 [top]
Target 4 ID 1024
Target 4 Name Solute carrier family 22 member 11
Target 4 Synonyms
  1. Organic anion transporter 4
Target 4 Gene Name SLC22A11
Target 4 Protein Sequence >Solute carrier family 22 member 11 
MAFSKLLEQAGGVGLFQTLQVLTFILPCLMIPSQMLLENFSAAIPGHRCWTHMLDNGSAV
STNMTPKALLTISIPPGPNQGPHQCRRFRQPQWQLLDPNATATSWSEADTEPCVDGWVYD
RSVFTSTIVAKWDLVCSSQGLKPLSQSIFMSGILVGSFIWGLLSYRFGRKPMLSWCCLQL
AVAGTSTIFAPTFVIYCGLRFVAAFGMAGIFLSSLTLMVEWTTTSRRAVTMTVVGCAFSA
GQAALGGLAFALRDWRTLQLAASVPFFAISLISWWLPESARWLIIKGKPDQALQELRKVA
RINGHKEAKNLTIEVLMSSVKEEVASAKEPRSVLDLFCVPVLRWRSCAMLVVNFSLLISY
YGLVFDLQSLGRDIFLLQALFGAVDFLGRATTALLLSFLGRRTIQAGSQAMAGLAILANM
LVPQDLQTLRVVFAVLGKGCFGISLTCLTIYKAELFPTPVRMTADGILHTVGRLGAMMGP
LILMSRQALPLLPPLLYGVISIASSLVVLFFLPETQGLPLPDTIQDLESQKSTAAQGNRQ
EAVTVESTSL
Target 4 Number of Residues 559
Target 4 Molecular Weight 59972
Target 4 Theoretical pI 8.71
Target 4 GO Classification
Function
transporter activity
Process
physiological process
cellular physiological process
transport
Component
cell
membrane
intrinsic to membrane
integral to membrane
Target 4 General Function Carbohydrate transport and metabolism
Target 4 Specific Function Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds
Target 4 Pathways Not Available
Target 4 Reactions Not Available
Target 4 Pfam Domain Function
Target 4 Signals
  • None
Target 4 Transmembrane Regions
  • 11-31
  • 143-163
  • 175-195
  • 201-221
  • 232-252
  • 257-277
  • 347-367
  • 379-399
  • 403-423
  • 431-451
  • 464-484
  • 491-511
Target 4 Essentiality Non-Essential
Target 4 GenBank ID Protein 7707622 Link Image
Target 4 UniProtKB/Swiss-Prot ID Q9NSA0 Link Image
Target 4 UniProtKB/Swiss-Prot Entry Name OAT4_HUMAN Link Image
Target 4 PDB ID Not Available
Target 4 Cellular Location
  • Cell membrane
  • multi-pass membrane protein
Target 4 Gene Sequence >1653 bp 
ATGGCGTTCTCGAAGCTCTTGGAGCAAGCCGGAGGCGTGGGCCTCTTCCAGACCCTGCAG
GTGCTCACCTTCATCCTCCCCTGCCTCATGATACCTTCCCAGATGCTCCTGGAGAACTTC
TCAGCCGCCATCCCAGGCCACCGATGCTGGACACACATGCTGGACAATGGCTCTGCGGTT
TCCACAAACATGACCCCCAAGGCCCTTCTGACCATCTCCATCCCGCCAGGCCCCAACCAG
GGGCCCCACCAGTGCCGCCGCTTCCGCCAGCCACAGTGGCAGCTCTTGGACCCCAATGCC
ACGGCCACCAGCTGGAGCGAAGCTGACACGGAGCCGTGTGTGGACGGCTGGGTCTATGAC
CGCAGCGTCTTCACCTCCACCATCGTGGCCAAGTGGGACCTGGTGTGCAGCTCCCAGGGC
TTGAAGCCCCTAAGCCAGTCCATCTTCATGTCCGGGATCCTGGTGGGCTCCTTTATCTGG
GGCCTCCTCTCCTACCGGTTTGGGAGGAAGCCGATGCTGAGCTGGTGCTGCCTGCAGTTG
GCCGTGGCGGGCACCAGCACCATCTTCGCCCCAACATTCGTCATCTACTGCGGCCTGCGG
TTCGTGGCCGCTTTTGGGATGGCCGGCATCTTTCTGAGTTCACTGACACTGATGGTGGAG
TGGACCACGACCAGCAGGAGGGCGGTCACCATGACGGTGGTGGGATGTGCCTTCAGCGCA
GGCCAGGCGGCGCTGGGCGGCCTGGCCTTTGCCCTGCGGGACTGGAGGACTCTCCAGCTG
GCAGCATCAGTGCCCTTCTTTGCCATCTCCCTGATATCCTGGTGGCTGCCAGAATCCGCC
CGGTGGCTGATTATTAAGGGCAAACCAGACCAAGCACTTCAGGAGCTCAGAAAGGTGGCC
AGGATAAATGGCCACAAGGAGGCCAAGAACCTGACCATAGAGGTGCTGATGTCCAGCGTG
AAGGAGGAGGTGGCCTCTGCAAAGGAGCCGCGGTCGGTGCTGGACCTGTTCTGCGTGCCC
GTGCTCCGCTGGAGGAGCTGCGCCATGCTGGTGGTGAATTTCTCTCTATTGATCTCCTAC
TATGGGCTGGTCTTCGACCTGCAGAGCCTGGGCCGTGACATCTTCCTCCTCCAGGCCCTC
TTCGGGGCCGTGGACTTCCTGGGCCGGGCCACCACTGCCCTCTTGCTCAGTTTCCTTGGC
CGCCGCACCATCCAGGCGGGTTCCCAGGCCATGGCCGGCCTCGCCATTCTAGCCAACATG
CTGGTGCCGCAAGATTTGCAGACCCTGCGTGTGGTCTTTGCTGTGCTGGGAAAGGGATGT
TTTGGGATAAGCCTAACCTGCCTCACCATCTACAAGGCTGAACTCTTTCCAACGCCAGTG
CGGATGACAGCAGATGGCATTCTGCATACAGTGGGCCGGCTGGGGGCTATGATGGGTCCC
CTGATCCTGATGAGCCGCCAAGCCCTGCCCCTGCTGCCTCCTCTCCTCTATGGCGTTATC
TCCATTGCTTCCAGCCTGGTTGTGCTGTTCTTCCTCCCGGAGACCCAGGGACTTCCGCTC
CCTGACACTATCCAGGACCTGGAGAGCCAGAAATCAACAGCAGCCCAGGGCAACCGGCAA
GAGGCCGTCACTGTGGAAAGTACCTCGCTCTAG
Target 4 GenBank Gene ID
Target 4 GeneCard ID SLC22A11 Link Image
Target 4 GenAtlas ID SLC22A11 Link Image
Target 4 HGNC ID HGNC:18120 Link Image
Target 4 Chromosome Location 11
Target 4 Locus 11q13.1
Target 4 SNPs SNPJam Report Link Image
Target 4 General References
  1. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. [PubMed Link Image]
Target 4 Drug References
  1. Enomoto A, Takeda M, Shimoda M, Narikawa S, Kobayashi Y, Kobayashi Y, Yamamoto T, Sekine T, Cha SH, Niwa T, Endou H: Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. J Pharmacol Exp Ther. 2002 Jun;301(3):797-802. [PubMed Link Image]
  2. Babu E, Takeda M, Narikawa S, Kobayashi Y, Enomoto A, Tojo A, Cha SH, Sekine T, Sakthisekaran D, Endou H: Role of human organic anion transporter 4 in the transport of ochratoxin A. Biochim Biophys Acta. 2002 Jun 12;1590(1-3):64-75. [PubMed Link Image]
  3. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. [PubMed Link Image]
  4. Hashimoto T, Narikawa S, Huang XL, Minematsu T, Usui T, Kamimura H, Endou H: Characterization of the renal tubular transport of zonampanel, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, by human organic anion transporters. Drug Metab Dispos. 2004 Oct;32(10):1096-102. [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.