Target Information
Target General Infomation | |||||
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Target ID |
T25258
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Former ID |
TTDR00007
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Target Name |
Multidrug resistance protein 1
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Gene Name |
ABCB1
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Synonyms |
CD243 antigen; P-glycoprotein 1; ABCB1
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Target Type |
Successful
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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.
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BioChemical Class |
Acid anhydrides hydrolase
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Target Validation |
T25258
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UniProt ID | |||||
EC Number |
EC 3.6.3.44
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Sequence |
MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAII
HGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSG IGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVS KINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFT DKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIG AAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARG AAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSG QTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLF ATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIA IARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAG FDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRS SLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAII NGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKA GEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNI ANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEA IENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFG AYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDS YSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVV QLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVV SQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLD EATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQL LAQKGIYFSMVSVQAGTKRQ |
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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 521968 | ClinicalTrials.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 536248 | Pharmacological strategies for overcoming multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):861-79. | ||||
Ref 545232 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002537) | ||||
Ref 545874 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005159) | ||||
Ref 546769 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010214) | ||||
Ref 546965 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011621) | ||||
Ref 527635 | A 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 528198 | J 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 529220 | Bioorg 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 529846 | J 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 531954 | Mechanisms 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. |
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