Target Information

Target General Infomation
Target ID
T14342
Former ID
TTDS00317
Target Name
HIV-1 reverse transcriptase
Gene Name
pol
Synonyms
HIV-1 RT; Human immunodeficiency virus type 1 reverse transcriptase; pol
Target Type
Successful
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
Target Validation
T14342
UniProt ID
Q69617
EC Number
EC 2.7.7.49
Sequence
MEKEGKISKIGPENPYNTPVFAIKKKDSTRWRKLVDFRELNKRTQDFWEVQLGIPHPAGL
KKKKSVTV
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 521414ClinicalTrials.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 522768ClinicalTrials.gov (NCT00964262) A Study to Evaluate Safety and Pharmacokinetics/Pharmacodynamics of Sustained Release(SR) Exenatide. U.S. National Institutes of Health.
Ref 522839ClinicalTrials.gov (NCT01007890) Prediction of Response to Neoadjuvant Chemotherapy in Women With Operable Breast Cancer. U.S. National Institutes of Health.
Ref 524080ClinicalTrials.gov (NCT01697293) Triciribine Phosphate in Breast Cancer. U.S. National Institutes of Health.
Ref 524955ClinicalTrials.gov (NCT02266745) A Phase 1 Study of PT-112 Injection in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 536833Emerging antiviral drugs. Expert Opin Emerg Drugs. 2008 Sep;13(3):393-416.
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 545326Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002844)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525430J 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 525526Bioorg 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 525664Bioorg 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 525677Bioorg 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 525991Bioorg Med Chem Lett. 2001 Feb 26;11(4):523-8.Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
Ref 526074J Med Chem. 2001 Jun 7;44(12):1866-82.2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
Ref 526160Bioorg Med Chem Lett. 2001 Oct 22;11(20):2763-7.Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase.
Ref 526635J 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 526794J Med Chem. 1992 May 15;35(10):1887-97.Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones.
Ref 526898Bioorg 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 527080Bioorg 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 527413Bioorg 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 527497J 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 527570J 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 527718Bioorg Med Chem Lett. 2005 Oct 15;15(20):4447-50.4-Phenylcoumarins as HIV transcription inhibitors.
Ref 528078Bioorg 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 528536J Med Chem. 1991 Jul;34(7):2231-41.Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
Ref 533677J Med Chem. 1995 Aug 18;38(17):3258-63.Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.
Ref 533923New antivirals with activity against varicella-zoster virus. Ann Neurol. 1994;35 Suppl:S69-72.
Ref 534066J 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 534139J Med Chem. 1996 May 24;39(11):2129-40.Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition.
Ref 534243J 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 534709J 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 534775J 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 535055Computer-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 536329Chimeric 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 536361Natural 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 536833Emerging antiviral drugs. Expert Opin Emerg Drugs. 2008 Sep;13(3):393-416.
Ref 537934Current use of anti-HIV drugs in AIDS. J Antimicrob Chemother. 1993 Jul;32 Suppl A:133-8.
Ref 538143A 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.
Ref 551230HIV and reverse transcriptase inhibition by tanninsOriginal Research. Bioorg. Med. Chem. Lett. 2(12):1529-1534 (1992).
Ref 551232Imidazo[2??3??:6,5]dipyrido[3,2-b:2??3??e]-1,4-diazepines: non-nucleoside HIV-1 reverse transcriptase inhibitors with greater enzyme affinity than nevirapine, Bioorg. Med. Chem. Lett. 2(12):1745-1750(1992).

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