Therapeutic Targets Database
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TTD Target ID: TTDS00317

Target Information
NameHIV-1 reverse transcriptase    
Type of targetSuccessful target    
SynonymsHIV-1 RT    
Human immunodeficiency virus type 1 reverse transcriptase    
DiseaseHuman immunodeficiency virus [HIV] disease
[ICD9: 279.3   ICD10: D84.9]
[1][2][3]
Drug(s)DelavirdineApprovedHIV infection[4]
EfavirenzApprovedHIV infection[5]
EmtricitabineApprovedHIV infection[6]
EtravirineApprovedHIV infections[7]
NevirapineApprovedHIV infection[8][9][10]
SorivudineApprovedAntiviral (Herpes simplex virus type I (HSV-1), Varicella zoster virus (VZV), Epstein-Barr virus (EBV))[11][12]
Tenofovir disoproxilApprovedHIV infection[13]
Abacavir/dolutegravir/lamivudinePhase IIIHIV infection therapy in treatment-naive patients
Dolutegravir + abacavir sulphate + lamivudinePhase IIIHIV infections
IDX899Phase IIHIV infections[14]
DapivirinePhase I/IIHIV infections[7]
BioChemical ClassRNA-directed DNA polymerase    
EC NumberEC 2.7.7.49
UniProt IDQ69617
SequenceMEKEGKISKIGPENPYNTPVFAIKKKDSTRWRKLVDFRELNKRTQDFWEVQLGIPHPAGL KKKKSVTV
Related US Patent6,492,423
6,492,515
6,569,897
6,610,714
6,673,791
6,759,533
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor1- (1-Phenyl-propyl)-3-thiazol-2-yl-thiourea[15]
1- (2-Furan-2-yl-ethyl)-3-thiazol-2-yl-thiourea[16]
1- (2-Phenoxy-ethyl)-3-thiazol-2-yl-thiourea[15]
1- (2-Phenyl-propyl)-3-thiazol-2-yl-thiourea[16]
1- (2-Pyridin-2-yl-ethyl)-3-thiazol-2-yl-thiourea[16]
1- (3-Phenyl-propyl)-3-thiazol-2-yl-thiourea[16]
1- (4-Butyl-thiazol-2-yl)-3-phenethyl-thiourea[16]
1- (4-Cyano-thiazol-2-yl)-3-phenethyl-thiourea[16]
1-Adamantan-1-ylmethyl-3-thiazol-2-yl-thiourea[15]
1-Benzenesulfonyl-2-nitro-benzene[17]
1-Benzothiazol-2-yl-3-phenethyl-thiourea[16]
1-Benzyl-3-thiazol-2-yl-thiourea[16]
1-Furan-2-ylmethyl-3-thiazol-2-yl-thiourea[15]
1-Phenethyl-3-[1,3,4]thiadiazol-2-yl-thiourea[16]
1-Thiazol-2-yl-3- (2-o-tolyl-ethyl)-thiourea[16]
1-Thiazol-2-yl-3- (2-p-tolyl-ethyl)-thiourea[15]
1-nitro-2- (2-nitrophenylsulfonyl)benzene[17]
10-Allyl-10H-dibenzo[b,f][1,4]oxazepin-11-one[18]
10-Ethyl-10H-dibenzo[b,f][1,4]oxazepin-11-one[18]
10-Isopropyl-10H-dibenzo[b,f][1,4]oxazepin-11-one[18]
10-Propyl-10H-dibenzo[b,f][1,4]oxazepin-11-one[18]
10-Propyl-10H-dibenzo[b,f][1,4]thiazepin-11-one[18]
2',3'-Dideoxyadenosine Triphosphate (Ddatp)[19]
2'-3'-dideoxy-7-deaza-guaninetriphosphate[19]
2-Amino-6- (2-bromo-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (2-chloro-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (2-chloro-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (2-cyano-benzenesulfinyl)-benzonitrile[17]
2-Amino-6- (2-cyano-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (2-cyano-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (2-fluoro-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (2-methoxy-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (3-bromo-benzenesulfinyl)-benzonitrile[17]
2-Amino-6- (3-bromo-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (3-bromo-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (3-chloro-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (3-chloro-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (3-cyano-benzenesulfonyl)-benzonitrile[17]
2-Amino-6- (3-cyano-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (3-fluoro-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (3-methoxy-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (4-chloro-phenylsulfanyl)-benzonitrile[17]
2-Amino-6- (naphthalene-1-sulfonyl)-benzonitrile[17]
2-Amino-6- (naphthalene-2-sulfonyl)-benzonitrile[17]
2-Amino-6- (toluene-2-sulfonyl)-benzonitrile[17]
2-Amino-6- (toluene-3-sulfinyl)-benzonitrile[17]
2-Amino-6- (toluene-3-sulfonyl)-benzonitrile[17]
2-Amino-6- (toluene-4-sulfonyl)-benzonitrile[17]
2-Amino-6-benzenesulfonyl-benzonitrile[17]
2-Amino-6-m-tolylsulfanyl-benzonitrile[17]
2-Amino-6-p-tolylsulfanyl-benzonitrile[17]
2-Amino-6-phenylsulfanyl-benzonitrile[17]
2-Benzylsulfanyl-6-chloro-pyrimidin-4-ylamine[20]
3'thiacytidine[21]
3-Benzylamino-5-ethyl-6-methyl-1H-pyridin-2-one[22]
6-Benzyl-2-cyclohexylsulfanyl-3H-pyrimidin-4-one[23]
6-Benzyl-2-cyclopentylsulfanyl-3H-pyrimidin-4-one[24]
6-Benzyl-2-isobutylsulfanyl-3H-pyrimidin-4-one[23]
6-Benzyl-2-sec-butylsulfanyl-3H-pyrimidin-4-one[24]
ATEVIRDINE[25]
ATEVIRDINE SULPHATE[26]
Alovudine[27]
Amdoxovir[28]
Apricitabine[7]
Benzimidazole 5-carboxamide[7]
Benzothiadiazines[7]
CORILAGIN[29]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
Cyclosporin A analogue[30]
DEOXYTHYMIDINE_TRIPHOSPHATE[19]
Dapivirine[7]
DdC[31]
DdI[31]
Delavirdine[4]
Deoxyfluorothymidine[21]
Dideoxycytidine[21]
Dihydropyrone[7]
EMIVIRINE[32]
EPIGALOCATECHIN GALLATE[33]
Efavirenz[5]
Elvucitabine[34]
Emtricitabine[6]
Ethyl 1-[ (1H-benzimidazol-2[35]
Ethyl 1-[ (1H-benzimidazol-5[35]
Ethyl 1-[ (1H-benzotriazol-5[35]
Etravirine[7]
Fullerene Derivative[36]
Fullerene Derivative[36]
Fullerene Derivative[36]
Fullerene Derivative[36]
Fullerene Derivative[36]
Fullerene Derivative[36]
Fullerene Derivative[36]
HEPT[37]
HI-172[38]
HI-236[39]
HI-240[32]
HI-241[39]
HI-242[39]
HI-244[15]
HI-280[38]
HI-281[38]
HI-443[32]
HI-445[38]
IDX899[14]
ISODISPAR B[40]
Indole N -acetamide[7]
L-697,661[41]
L-697661[42]
LY-73497[16]
NSC-380292[43]
Nevirapine[8][9][10]
Opaviraline[44]
PT-101[16]
PT-102[39]
PT-103[16]
PT-104[45]
PT-106[16]
PT-108[16]
PT-109[45]
PT-110[45]
PT-112[45]
PT-113[45]
PT-114[45]
PT-115[45]
PT-302[16]
PT-304[16]
PT-306[16]
PT-307[16]
PT-308[16]
PT-309[16]
PT-310[16]
PT-311[16]
PT-312[16]
PT-313[16]
PT-314[16]
PT-315[16]
PT-316[16]
PT-317[16]
PT-319[16]
PT-320[16]
PT-322[16]
R-82150[46]
R-82913[16]
R-87027[47]
RTI-20[48]
Rilpivirine[7]
TIBO[49]
TRICIRIBINE[50]
TROVIRDINE[38]
TROVIRDINE[42]
TROVIRDINE HYDROCHLORIDE[51]
Tenofovir disoproxil[13]
Tetrahydroimidazo[4,5,1-jk]-[1,4]benzodiazepin-2 (1H)-one[52]
UK-129485[53]
ZIDOVUDINE TRIPHOSPHATE[19]
[ (40-OH) MeLeu]4-CsA derivatives[30]
[ (40-OH) MeLeu]4-CsA derivatives[30]
[ (40-OH) MeLeu]4-CsA derivatives[30]
[ (40-OH) MeLeu]4-CsA derivatives[30]
[ (40-OH) MeLeu]4-CsA derivatives[30]
[ (40-OH)MeLeu]4-Cyclosporin A[30]
[ (D)MeSer]3-[[30]
AptamerLigand 1.1[54]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
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Ref 2Nevirapine: a review of its use in the prevention and treatment of paediatric HIV infection. Paediatr Drugs. 2000 Sep-Oct;2(5):373-407. To Reference
Ref 3Strategies for antiviral therapy in AIDS. Nature. 1987 Feb 26-Mar 4;325(6107):773-8. To Reference
Ref 4Probing nonnucleoside inhibitor-induced active-site distortion in HIV-1 reverse transcriptase by transient kinetic analyses. Protein Sci. 2007 Aug;16(8):1728-37. To Reference
Ref 5Characterization of HIV-1 enzyme reverse transcriptase inhibition by the compound 6-chloro-1,4-dihydro-4-oxo-1-(beta-D-ribofuranosyl) quinoline-3-carboxylic acid through kinetic and in silico studies. Curr HIV Res. 2009 May;7(3):327-35. To Reference
Ref 6The simultaneous assay of tenofovir and emtricitabine in plasma using LC/MS/MS and isotopically labeled internal standards. J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Jul 1;877(20-21):1907-14. Epub 2009 May 21. To Reference
Ref 7Emerging antiviral drugs. Expert Opin Emerg Drugs. 2008 Sep;13(3):393-416. To Reference
Ref 8The human immunodeficiency virus type 1 nonnucleoside reverse transcriptase inhibitor resistance mutation I132M confers hypersensitivity to nucleoside analogs. J Virol. 2009 Apr;83(8):3826-33. Epub 2009 Feb 4. To Reference
Ref 9Nevirapine Increases High-Density Lipoprotein Cholesterol Concentration by Stimulation of Apolipoprotein A-I Production. Arterioscler Thromb Vasc Biol. 2009 Aug 10. [Epub ahead of print] To Reference
Ref 10Mini Rev Med Chem. 2007 Nov;7(11):1108-19.Privileged structures: a useful concept for the rational design of new lead drug candidates. To Reference
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Ref 13Effect of mobile phase pH and organic content on LC-MS analysis of nucleoside and nucleotide HIV reverse transcriptase inhibitors. J Chromatogr Sci. 2009 May-Jun;47(5):365-72. To Reference
Ref 14GSK. Product Development Pipeline. February 2009. To Reference
Ref 15Bioorg Med Chem Lett. 2001 Feb 26;11(4):523-8.Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. To Reference
Ref 16J 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 studies of PETT analogs. To Reference
Ref 17J Med Chem. 2001 Jun 7;44(12):1866-82.2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. To Reference
Ref 18J Med Chem. 1992 May 15;35(10):1887-97.Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 2. Tricyclic pyridobenzoxazepinones and dibenzoxazepinones. To Reference
Ref 19J 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. To Reference
Ref 20J 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. To Reference
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Ref 22J 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. To Reference
Ref 23J Med Chem. 1995 Aug 18;38(17):3258-63.Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. To Reference
Ref 24J 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. To Reference
Ref 25J Med Chem. 1993 May 14;36(10):1505-8.Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a second-generation clinical candidate. To Reference
Ref 26J Med Chem. 1996 Sep 13;39(19):3769-89.Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors. To Reference
Ref 27Emerging drugs for treatment of overactive bladder and detrusor overactivity. Expert Opin Emerg Drugs. 2008 Sep;13(3):431-46. To Reference
Ref 28Agents in development for the treatment of diabetic nephropathy. Expert Opin Emerg Drugs. 2008 Sep;13(3):447-63. To Reference
Ref 29Bioorg. Med. Chem. Lett. 2(12):1529-1534 (1992) To Reference
Ref 30Bioorg 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. To Reference
Ref 31A 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. To Reference
Ref 32Bioorg 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. To Reference
Ref 33Bioorg Med Chem Lett. 2001 Oct 22;11(20):2763-7.Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase. To Reference
Ref 34The development of the direct renin inhibitor aliskiren: treating hypertension and beyond. Expert Opin Emerg Drugs. 2008 Sep;13(3):417-30. To Reference
Ref 35Computer-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. To Reference
Ref 36Bioorg 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. To Reference
Ref 37Bioorg 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. To Reference
Ref 38Bioorg 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. To Reference
Ref 39Bioorg Med Chem Lett. 2000 Jan 3;10(1):87-90.Antioxidant function of phenethyl-5-bromo-pyridyl thiourea compounds with potent anti-HIV activity. To Reference
Ref 40Bioorg Med Chem Lett. 2005 Oct 15;15(20):4447-50.4-Phenylcoumarins as HIV transcription inhibitors. To Reference
Ref 41Clinical experience with non-nucleoside reverse transcriptase inhibitors: L-697,661 and nevirapine. Adv Exp Med Biol. 1996;394:291-8. To Reference
Ref 42Bioorg Med Chem Lett. 1998 Jun 16;8(12):1511-6.Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors. To Reference
Ref 43Bioorg 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. To Reference
Ref 44Bioorg Med Chem Lett. 2000 Aug 7;10(15):1729-31.Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors. To Reference
Ref 45J 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. To Reference
Ref 46J Med Chem. 1993 Jan 22;36(2):249-55.Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one. To Reference
Ref 47J 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. To Reference
Ref 48J Med Chem. 1991 Jul;34(7):2231-41.Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. To Reference
Ref 49J Med Chem. 1996 May 24;39(11):2129-40.Comparative molecular moment analysis (CoMMA): 3D-QSAR without molecular superposition. To Reference
Ref 50J 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. To Reference
Ref 51J Med Chem. 2005 Jun 2;48(11):3858-73.Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives. To Reference
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