Target Information

Target General Infomation
Target ID
T25258
Former ID
TTDR00007
Target Name
Multidrug resistance protein 1
Gene Name
ABCB1
Synonyms
CD243 antigen; P-glycoprotein 1; ABCB1
Target Type
Successful
Disease Adrenocortical carcinoma [ICD9: 194; ICD10: C74.0]
Acute myeloid leukemia [ICD9: 205; ICD10: C92.0]
Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Non-small cell lung cancer [ICD10: C33-C34]
Ovarian cancer [ICD9: 183; ICD10: C56]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
BioChemical Class
Acid anhydrides hydrolase
Target Validation
T25258
UniProt ID
P08183
EC Number
EC 3.6.3.44
Sequence
MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAII
HGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSG
IGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVS
KINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFT
DKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIG
AAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARG
AAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSG
QTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLF
ATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIA
IARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAG
FDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRS
SLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAII
NGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKA
GEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNI
ANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEA
IENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFG
AYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDS
YSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVV
QLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVV
SQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLD
EATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQL
LAQKGIYFSMVSVQAGTKRQ
Drugs and Mode of Action
Drug(s) Biricodar Drug Info Approved Ovarian cancer [536248]
CBT-1 Drug Info Phase 3 Non-small cell lung cancer [521968]
EDP-322 Drug Info Phase 1 Bacterial infections [548796]
W-198 Drug Info Phase 1 Cancer [550040]
LY335979 Drug Info Discontinued in Phase 3 Acute myeloid leukemia [545874]
Tariquidar Drug Info Discontinued in Phase 2 Adrenocortical carcinoma [546769]
ELACRIDAR Drug Info Discontinued in Phase 1 Cancer [545232]
ONT-093 Drug Info Discontinued in Phase 1 Solid tumours [546965]
Inhibitor 4,3'',5''-trimethoxy-[1,1':2',1'']-terphenyl Drug Info [528198]
6-(3,5-dimethoxy-phenyl)-naphthalen-2-ol Drug Info [528198]
EDP-322 Drug Info [532939]
ELACRIDAR Drug Info [529846]
ONT-093 Drug Info [527635]
TRISMETHOXYRESVERATROL Drug Info [528198]
XR-9456 Drug Info [529220]
XR-9504 Drug Info [529220]
XR-9544 Drug Info [529220]
XR-9577 Drug Info [529220]
[1,1':2',1'']-terphenyl-4,3'',5''-triol Drug Info [528198]
Modulator Biricodar Drug Info
CBT-1 Drug Info
LY335979 Drug Info
Tariquidar Drug Info
W-198 Drug Info [531954]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway ABC transporters
Bile secretion
MicroRNAs in cancer
NetPath Pathway IL2 Signaling Pathway
TCR Signaling Pathway
Pathway Interaction Database HIF-1-alpha transcription factor network
Reactome ABC-family proteins mediated transport
WikiPathways Nuclear Receptors in Lipid Metabolism and Toxicity
Abacavir transport and metabolism
Multi Drug Resistance Protein 1 (Glycoprotein 1) Regulation
Integrated Pancreatic Cancer Pathway
Allograft Rejection
Drug Induction of Bile Acid Pathway
Codeine and Morphine Metabolism
References
Ref 521968ClinicalTrials.gov (NCT00437749) A Study of CBT-1 and Paclitaxel With Carboplatin in Patients With Advanced Inoperable Non-small Cell Lung Cancer. U.S. National Institutes of Health.
Ref 536248Pharmacological strategies for overcoming multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):861-79.
Ref 545232Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002537)
Ref 545874Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005159)
Ref 546769Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010214)
Ref 546965Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011621)
Ref 548796Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028928)
Ref 550040Pharmacokinetics and safety of bromotetrandrine (BrTet,W198) after single-dose intravenous administration in healthy Chinese volunteers. Journal of Clinical Pharmacy and Therapeutics (2010) 35, 113-119.
Ref 527635A phase I pharmacokinetic study of the P-glycoprotein inhibitor, ONT-093, in combination with paclitaxel in patients with advanced cancer. Invest New Drugs. 2005 Aug;23(4):311-5.
Ref 528198J Med Chem. 2006 May 18;49(10):3012-8.Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells.
Ref 529220Bioorg 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.
Ref 529846J Med Chem. 2008 Dec 11;51(23):7602-13.2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties.
Ref 531954Mechanisms of tetrandrine and 5-bromotetrandrine in reversing multidrug resistance may relate to down-regulation of multidrug resistance associated protein 7 expression. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2012 Jun;20(3):558-63.
Ref 532939In vitro activities of the novel bicyclolides modithromycin (EDP-420, EP-013420, S-013420) and EDP-322 against MDR clinical Neisseria gonorrhoeae isolates and international reference strains. J Antimicrob Chemother. 2015 Jan;70(1):173-7.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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