Therapeutic Targets Database
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TTD Target ID: TTDS00288

Target Information
NameMultidrug resistance-associated protein 1    
Type of targetSuccessful target    
SynonymsMrp1    
Multidrug resistance protein 1    
DiseaseCystic fibrosis
[ICD9: 277.0   ICD10: E84]
[1]
Streptococcus pneumoniae infections
[ICD9: 001-139, 480-486, 770.0   ICD10: A00-B99, J12, J13, J14, J15, J16, J17, J18, P23]
[2]
Drug(s)BiricodarApprovedOvarian cancer[3]
SulfinpyrazoneApprovedGout[4][5][6]
BenzbromaronePhase IVHyperuricaemia and gout[7]
BioChemical ClassABC transporter    
UniProt IDP33527
PDB Structure2CBZ.    
FunctionMay participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly.    
SequenceMALRGFCSADGSDPLWDWNVTWNTSNPDFTKCFQNTVLVWVPCFYLWACFPFYFLYLSRH 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
Related US Patent6,673,809
Target ValidationClick to Find Target Validation Information.    
InhibitorL-660771,   MK-571[8]
Pyrrolopyrimidine[9]
XR-9456[10]
XR-9504[10]
XR-9544[10]
XR-9577[10]
StimulatorBenzbromarone[7]
ModulatorBiricodar[3]
Sulfinpyrazone[4][5][6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Evaluation of MRP1-5 gene expression in cystic fibrosis patients homozygous for the delta F508 mutation. Pediatr Res. 2003 Nov;54(5):627-34. Epub 2003 Aug 20. To Reference
Ref 2Mice lacking the multidrug resistance protein 1 are resistant to Streptococcus pneumoniae-induced pneumonia. J Immunol. 2001 Mar 15;166(6):4059-64. To Reference
Ref 3Pharmacological strategies for overcoming multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):861-79. To Reference
Ref 4Species-dependent transport and modulation properties of human and mouse multidrug resistance protein 2 (MRP2/Mrp2, ABCC2/Abcc2). Drug Metab Dispos. 2008 Apr;36(4):631-40. Epub 2008 Jan 7. To Reference
Ref 5Mutation 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. To Reference
Ref 6Genome duplications and other features in 12 Mb of DNA sequence from human chromosome 16p and 16q. Genomics. 1999 Sep 15;60(3):295-308. To Reference
Ref 7Transport of diclofenac by breast cancer resistance protein (ABCG2) and stimulation of multidrug resistance protein 2 (ABCC2)-mediated drug transport by diclofenac and benzbromarone. Drug Metab Dispos. 2009 Jan;37(1):129-36. Epub 2008 Oct 9. To Reference
Ref 8Bioorg Med Chem Lett. 2008 Sep 1;18(17):4761-3. Epub 2008 Aug 3.A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins. To Reference
Ref 9Topological model for the prediction of MRP1 inhibitory activity of pyrrolopyrimidines and templates derived from pyrrolopyrimidine. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4967-72. To Reference
Ref 10Bioorg Med Chem. 2008 Mar 1;16(5):2448-62. Epub 2007 Nov 28.Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors. To Reference



 

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