Target Information
Target General Infomation | |||||
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Target ID |
T14342
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Former ID |
TTDS00317
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Target Name |
HIV-1 reverse transcriptase
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Gene Name |
pol
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Synonyms |
HIV-1 RT; Human immunodeficiency virus type 1 reverse transcriptase; pol
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Target Type |
Successful
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Disease | Cancer [ICD9: 140-229; ICD10: C00-C96] | ||||
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26] | |||||
Hepacivirus infections [ICD9: 070.4, 070.5, 070.70; ICD10: B17.1, B18.2] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Viral infections [ICD9: 054.0, 054.1, 054.2, 054.3, 075, 771.2, 052, 053; ICD10: B01, B02, A60, B00, B27, G05.1, P35.2] | |||||
BioChemical Class |
Kinase
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Target Validation |
T14342
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UniProt ID | |||||
EC Number |
EC 2.7.7.49
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Sequence |
MEKEGKISKIGPENPYNTPVFAIKKKDSTRWRKLVDFRELNKRTQDFWEVQLGIPHPAGL
KKKKSVTV |
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Drugs and Mode of Action | |||||
Drug(s) | Rilpivirine | Drug Info | Approved | Human immunodeficiency virus infection | [531783] |
Sorivudine | Drug Info | Approved | Viral infections | [551871] | |
PT-304 | Drug Info | Phase 3 | Discovery agent | [522839] | |
Dideoxycytidine | Drug Info | Phase 2 | Discovery agent | [521414] | |
Dapivirine | Drug Info | Phase 1/2 | Human immunodeficiency virus infection | [536833] | |
TRICIRIBINE | Drug Info | Phase 1/2 | Solid tumours | [524080], [541208] | |
PT-112 | Drug Info | Phase 1 | Cancer | [524955] | |
PT-302 | Drug Info | Phase 1 | Discovery agent | [522768] | |
LY-73497 | Drug Info | Discontinued in Phase 1 | Discovery agent | [545326] | |
Inhibitor | 1-(1-Phenyl-propyl)-3-thiazol-2-yl-thiourea | Drug Info | [525991] | ||
1-(2-Furan-2-yl-ethyl)-3-thiazol-2-yl-thiourea | Drug Info | [534066] | |||
1-(2-Phenoxy-ethyl)-3-thiazol-2-yl-thiourea | Drug Info | [525991] | |||
1-(2-Phenyl-propyl)-3-thiazol-2-yl-thiourea | Drug Info | [534066] | |||
1-(2-Pyridin-2-yl-ethyl)-3-thiazol-2-yl-thiourea | Drug Info | [534066] | |||
1-(3-Phenyl-propyl)-3-thiazol-2-yl-thiourea | Drug Info | [534066] | |||
1-(4-Butyl-thiazol-2-yl)-3-phenethyl-thiourea | Drug Info | [534066] | |||
1-(4-Cyano-thiazol-2-yl)-3-phenethyl-thiourea | Drug Info | [534066] | |||
1-Adamantan-1-ylmethyl-3-thiazol-2-yl-thiourea | Drug Info | [525991] | |||
1-Benzenesulfonyl-2-nitro-benzene | Drug Info | [526074] | |||
1-Benzothiazol-2-yl-3-phenethyl-thiourea | Drug Info | [534066] | |||
1-Benzyl-3-thiazol-2-yl-thiourea | Drug Info | [534066] | |||
1-Furan-2-ylmethyl-3-thiazol-2-yl-thiourea | Drug Info | [525991] | |||
1-nitro-2-(2-nitrophenylsulfonyl)benzene | Drug Info | [526074] | |||
1-Phenethyl-3-[1,3,4]thiadiazol-2-yl-thiourea | Drug Info | [534066] | |||
1-Thiazol-2-yl-3-(2-o-tolyl-ethyl)-thiourea | Drug Info | [534066] | |||
1-Thiazol-2-yl-3-(2-p-tolyl-ethyl)-thiourea | Drug Info | [525991] | |||
10-Allyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [526794] | |||
10-Ethyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [526794] | |||
10-Isopropyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [526794] | |||
10-Propyl-10H-dibenzo[b,f][1,4]oxazepin-11-one | Drug Info | [526794] | |||
10-Propyl-10H-dibenzo[b,f][1,4]thiazepin-11-one | Drug Info | [526794] | |||
2',3'-Dideoxyadenosine Triphosphate (Ddatp) | Drug Info | [527497] | |||
2'-3'-dideoxy-7-deaza-guaninetriphosphate | Drug Info | [527497] | |||
2-Amino-6-(2-bromo-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-chloro-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-chloro-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-cyano-benzenesulfinyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-cyano-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-cyano-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-fluoro-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(2-methoxy-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-bromo-benzenesulfinyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-bromo-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-bromo-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-chloro-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-chloro-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-cyano-benzenesulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-cyano-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-fluoro-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(3-methoxy-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(4-chloro-phenylsulfanyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(naphthalene-1-sulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(naphthalene-2-sulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(toluene-2-sulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(toluene-3-sulfinyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(toluene-3-sulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-(toluene-4-sulfonyl)-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-benzenesulfonyl-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-m-tolylsulfanyl-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-p-tolylsulfanyl-benzonitrile | Drug Info | [526074] | |||
2-Amino-6-phenylsulfanyl-benzonitrile | Drug Info | [526074] | |||
2-Benzylsulfanyl-6-chloro-pyrimidin-4-ylamine | Drug Info | [534709] | |||
3'thiacytidine | Drug Info | [537934] | |||
3-Benzylamino-5-ethyl-6-methyl-1H-pyridin-2-one | Drug Info | [526635] | |||
6-Benzyl-2-cyclohexylsulfanyl-3H-pyrimidin-4-one | Drug Info | [533677] | |||
6-Benzyl-2-cyclopentylsulfanyl-3H-pyrimidin-4-one | Drug Info | [525430] | |||
6-Benzyl-2-isobutylsulfanyl-3H-pyrimidin-4-one | Drug Info | [533677] | |||
6-Benzyl-2-sec-butylsulfanyl-3H-pyrimidin-4-one | Drug Info | [525430] | |||
Benzimidazole 5-carboxamide | Drug Info | [536833] | |||
Benzothiadiazines | Drug Info | [536833] | |||
CORILAGIN | Drug Info | [551230] | |||
Cyclosporin A analogue | Drug Info | [526898] | |||
Dapivirine | Drug Info | [536833] | |||
DdC | Drug Info | [538143] | |||
DdI | Drug Info | [538143] | |||
Deoxyfluorothymidine | Drug Info | [537934] | |||
DEOXYTHYMIDINE_TRIPHOSPHATE | Drug Info | [527497] | |||
Dideoxycytidine | Drug Info | [537934] | |||
Dihydropyrone | Drug Info | [536833] | |||
EPIGALOCATECHIN GALLATE | Drug Info | [526160] | |||
Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Drug Info | [535055] | |||
Ethyl 1-[(1H-benzimidazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Drug Info | [535055] | |||
Ethyl 1-[(1H-benzotriazol-5(6)-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Drug Info | [535055] | |||
Fullerene Derivative | Drug Info | [527413] | |||
HEPT | Drug Info | [527080] | |||
HI-172 | Drug Info | [525526] | |||
HI-236 | Drug Info | [525677] | |||
HI-240 | Drug Info | [525664] | |||
HI-241 | Drug Info | [525677] | |||
HI-242 | Drug Info | [525677] | |||
HI-244 | Drug Info | [525991] | |||
HI-280 | Drug Info | [525526] | |||
HI-281 | Drug Info | [525526] | |||
HI-443 | Drug Info | [525664] | |||
HI-445 | Drug Info | [525526] | |||
Indole N -acetamide | Drug Info | [536833] | |||
ISODISPAR B | Drug Info | [527718] | |||
LY-73497 | Drug Info | [534066] | |||
NSC-380292 | Drug Info | [528078] | |||
PT-101 | Drug Info | [534066] | |||
PT-102 | Drug Info | [525677] | |||
PT-103 | Drug Info | [534066] | |||
PT-104 | Drug Info | [534243] | |||
PT-106 | Drug Info | [534066] | |||
PT-108 | Drug Info | [534066] | |||
PT-109 | Drug Info | [534243] | |||
PT-110 | Drug Info | [534243] | |||
PT-112 | Drug Info | [534243] | |||
PT-113 | Drug Info | [534243] | |||
PT-114 | Drug Info | [534243] | |||
PT-115 | Drug Info | [534243] | |||
PT-302 | Drug Info | [534066] | |||
PT-304 | Drug Info | [534066] | |||
PT-306 | Drug Info | [534066] | |||
PT-307 | Drug Info | [534066] | |||
PT-308 | Drug Info | [534066] | |||
PT-309 | Drug Info | [534066] | |||
PT-310 | Drug Info | [534066] | |||
PT-311 | Drug Info | [534066] | |||
PT-312 | Drug Info | [534066] | |||
PT-313 | Drug Info | [534066] | |||
PT-314 | Drug Info | [534066] | |||
PT-315 | Drug Info | [534066] | |||
PT-316 | Drug Info | [534066] | |||
PT-317 | Drug Info | [534066] | |||
PT-319 | Drug Info | [534066] | |||
PT-320 | Drug Info | [534066] | |||
PT-322 | Drug Info | [534066] | |||
R-87027 | Drug Info | [534775] | |||
Rilpivirine | Drug Info | [536833] | |||
RTI-20 | Drug Info | [528536] | |||
Tetrahydroimidazo[4,5,1-jk]-[1,4]benzodiazepin-2(1H)-one | Drug Info | [536329] | |||
TIBO | Drug Info | [534139] | |||
TRICIRIBINE | Drug Info | [527570] | |||
UK-129485 | Drug Info | [551232] | |||
[(40-OH) MeLeu]4-CsA derivatives | Drug Info | [526898] | |||
[(40-OH)MeLeu]4-Cyclosporin A | Drug Info | [526898] | |||
[(D)MeSer]3-[(40-OH) MeLeu]4-Cyclosporin A | Drug Info | [526898] | |||
Modulator | Sorivudine | Drug Info | [533923], [536361] | ||
References | |||||
Ref 521414 | ClinicalTrials.gov (NCT00000678) Dideoxycytidine ( Ro 24-2027 ) A Randomized, Open-Label, Comparative Study of Dideoxycytidine ( ddC ) Versus Zidovudine ( AZT ) in Patients With AIDS or Advanced ARC Who Have Received Long-Term AZT Therapy.. U.S. National Institutes of Health. | ||||
Ref 522768 | ClinicalTrials.gov (NCT00964262) A Study to Evaluate Safety and Pharmacokinetics/Pharmacodynamics of Sustained Release(SR) Exenatide. U.S. National Institutes of Health. | ||||
Ref 522839 | ClinicalTrials.gov (NCT01007890) Prediction of Response to Neoadjuvant Chemotherapy in Women With Operable Breast Cancer. U.S. National Institutes of Health. | ||||
Ref 524080 | ClinicalTrials.gov (NCT01697293) Triciribine Phosphate in Breast Cancer. U.S. National Institutes of Health. | ||||
Ref 524955 | ClinicalTrials.gov (NCT02266745) A Phase 1 Study of PT-112 Injection in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 541208 | (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: 5920). | ||||
Ref 525430 | J Med Chem. 1999 Feb 25;42(4):619-27.5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives. | ||||
Ref 525526 | Bioorg Med Chem Lett. 1999 Jun 7;9(11):1593-8.Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus. | ||||
Ref 525664 | Bioorg Med Chem Lett. 1999 Dec 20;9(24):3411-6.N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. | ||||
Ref 525677 | Bioorg Med Chem Lett. 2000 Jan 3;10(1):87-90.Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity. | ||||
Ref 525991 | Bioorg Med Chem Lett. 2001 Feb 26;11(4):523-8.Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. | ||||
Ref 526074 | J Med Chem. 2001 Jun 7;44(12):1866-82.2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. | ||||
Ref 526160 | Bioorg Med Chem Lett. 2001 Oct 22;11(20):2763-7.Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase. | ||||
Ref 526635 | J Med Chem. 1992 Oct 16;35(21):3792-802.Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one. | ||||
Ref 526794 | J Med Chem. 1992 May 15;35(10):1887-97.Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones. | ||||
Ref 526898 | Bioorg Med Chem Lett. 2003 Dec 15;13(24):4415-9.Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs. | ||||
Ref 527080 | Bioorg Med Chem Lett. 2004 Jun 21;14(12):3173-6.5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series. | ||||
Ref 527413 | Bioorg Med Chem Lett. 2005 Feb 15;15(4):1107-9.Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives. | ||||
Ref 527497 | J Med Chem. 2005 Apr 7;48(7):2695-700.Synthesis of 2',3'-dideoxynucleoside 5'-alpha-P-borano-beta,gamma-(difluoromethylene)triphosphates and their inhibition of HIV-1 reverse transcriptase. | ||||
Ref 527570 | J Med Chem. 2005 Jun 2;48(11):3840-51.Design, synthesis and antiviral activity of novel 4,5-disubstituted 7-(beta-D-ribofuranosyl)pyrrolo[2,3-d][1,2,3]triazines and the novel 3-amino-5-methyl-1-(beta-D-ribofuranosyl)- and 3-amino-5-methyl-1-(2-deoxy-beta-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,7,8-hexaazaacenaphthylene as analogues of triciribine. | ||||
Ref 527718 | Bioorg Med Chem Lett. 2005 Oct 15;15(20):4447-50.4-Phenylcoumarins as HIV transcription inhibitors. | ||||
Ref 528078 | Bioorg Med Chem Lett. 2006 Jun 1;16(11):3034-8. Epub 2006 Mar 9.New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity. | ||||
Ref 528536 | J Med Chem. 1991 Jul;34(7):2231-41.Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. | ||||
Ref 533677 | J Med Chem. 1995 Aug 18;38(17):3258-63.Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. | ||||
Ref 533923 | New antivirals with activity against varicella-zoster virus. Ann Neurol. 1994;35 Suppl:S69-72. | ||||
Ref 534066 | J Med Chem. 1995 Dec 8;38(25):4929-36.Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studiesof PETT analogs. | ||||
Ref 534139 | J Med Chem. 1996 May 24;39(11):2129-40.Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition. | ||||
Ref 534243 | J Med Chem. 1996 Oct 11;39(21):4261-74.Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs. | ||||
Ref 534709 | J Med Chem. 1998 Sep 24;41(20):3793-803.Pyrimidine thioethers: a novel class of HIV-1 reverse transcriptase inhibitors with activity against BHAP-resistant HIV. | ||||
Ref 534775 | J Med Chem. 1998 Dec 17;41(26):5272-86.Prediction of binding affinities for TIBO inhibitors of HIV-1 reverse transcriptase using Monte Carlo simulations in a linear response method. | ||||
Ref 535055 | Computer-assisted design, synthesis and biological evaluation of novel pyrrolyl heteroaryl sulfones targeted at HIV-1 reverse transcriptase as non-nucleoside inhibitors. Bioorg Med Chem. 2000 Sep;8(9):2305-9. | ||||
Ref 536329 | Chimeric human immunodeficiency virus type 1/type 2 reverse transcriptases display reversed sensitivity to nonnucleoside analog inhibitors. Proc Natl Acad Sci U S A. 1991 Nov 1;88(21):9878-82. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 538143 | A peptide inhibitor of HIV-1 reverse transcriptase using alpha,beta-dehydro residues: a structure-based computer model. J Biomol Struct Dyn. 1998 Oct;16(2):347-54. |
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