Target Information
| Target General Information | Top | |||||
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| Target ID |
T16422
(Former ID: TTDS00255)
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| Target Name |
Multidrug resistance protein (MDR)
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| Synonyms |
P-glycoprotein
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Nausea/vomiting [ICD-11: MD90] | |||||
| BioChemical Class |
ABC transporter
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Benzquinamide | Drug Info | Approved | Nausea | [2], [3], [4] | |
| Clinical Trial Drug(s) | [+] 3 Clinical Trial Drugs | + | ||||
| 1 | Curcumin | Drug Info | Phase 3 | Solid tumour/cancer | [5], [6] | |
| 2 | MM36 | Drug Info | Phase 2 | Atopic dermatitis | [7] | |
| 3 | Ortataxel | Drug Info | Phase 2 | Solid tumour/cancer | [8] | |
| Discontinued Drug(s) | [+] 1 Discontinued Drugs | + | ||||
| 1 | Valspodar | Drug Info | Discontinued in Phase 3 | Acute myeloid leukaemia | [9] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | Benzquinamide | Drug Info | [1] | |||
| 2 | Curcumin | Drug Info | [10] | |||
| 3 | MM36 | Drug Info | [10] | |||
| 4 | Chemosensitizers | Drug Info | [14] | |||
| 5 | KP772 | Drug Info | [10] | |||
| 6 | WK-X-34 | Drug Info | [10] | |||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Ortataxel | Drug Info | [11], [12] | |||
| 2 | Valspodar | Drug Info | [13] | |||
| Drug Property Profile of Target | Top | |
|---|---|---|
| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| References | Top | |||||
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| REF 1 | Benzquinamide inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells. Oncol Res. 1992;4(8-9):359-65. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7124). | |||||
| REF 3 | Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21. | |||||
| REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7000). | |||||
| REF 6 | Nanocurcumin: a promising therapeutic advancement over native curcumin. Crit Rev Ther Drug Carrier Syst. 2013;30(4):331-68. | |||||
| REF 7 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
| REF 8 | Broad-spectrum modulation of ATP-binding cassette transport proteins by the taxane derivatives ortataxel (IDN-5109, BAY 59-8862) and tRA96023. Cancer Chemother Pharmacol. 2004 May;53(5):363-9. | |||||
| REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001281) | |||||
| REF 10 | Thiazolides: a new class of antiviral drugs. Expert Opin Drug Metab Toxicol. 2009 Jun;5(6):667-74. | |||||
| REF 11 | Clinical pipeline report, company report or official report of Spectrum Phamaceuticals (2009). | |||||
| REF 12 | Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer. 2008 Nov 18;99(10):1579-85. | |||||
| REF 13 | Intracellular levels of two cyclosporin derivatives valspodar (PSC 833) and cyclosporin a closely associated with multidrug resistance-modulating activity in sublines of human colorectal adenocarcinoma HCT-15. Jpn J Cancer Res. 2001 Oct;92(10):1116-26. | |||||
| REF 14 | P-glycoprotein as a drug target in the treatment of multidrug resistant cancer. Curr Drug Targets. 2000 Jul;1(1):85-99. | |||||
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