Target Information

Target General Infomation
Target ID
T15352
Former ID
TTDS00318
Target Name
HIV reverse transcriptase
Gene Name
gag-pol
Synonyms
gag-pol
Target Type
Successful
Disease Breast cancer [ICD9: 174, 175; ICD10: C50]
Cytomegalovirus infection [ICD10: B25]
Herpes simplex virus infection [ICD9: 54; ICD10: B00]
HBV infection [ICD9: 070.2-070.3; ICD10: B16, B18.0, B18.1]
HIV infection; Chronic hepatitis b [ICD9: 042, 070.2-070.3; ICD10: B16, B18.0, B18.1, B20]
Hepatitis virus infection; Human immunodeficiency virus infection [ICD9:573.3, 279.3; ICD10: K75.9, B20-B26]
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26]
HIV-1 infection [ICD9: 001-139, 042; ICD10: B20-B24]
Mycobacterium tuberculosis infection [ICD10: A15-A19]
Sexually transmitted infection [ICD10: A64]
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]
Unspecified [ICD code not available]
Function
Integrase: Catalyzes viral DNA integration into the host chromosome, by performing a series of DNA cutting and joining reactions. This enzyme activity takes place after virion entry into a cell and reverse transcription of the RNA genome in dsDNA. The first step in the integration process is 3' processing. This step requires a complex comprising the viral genome, matrix protein, Vpr and integrase. This complex is called the pre- integration complex (PIC). The integrase protein removes 2 nucleotides from each 3' end of the viral DNA, leaving recessed CA OH's atthe 3' ends. In the second step, the PIC enters cell nucleus. This process is mediated through integrase and Vpr proteins, and allows the virus to infect a non dividing cell. This ability to enter the nucleus is specific of lentiviruses, other retroviruses cannot and rely on cell division to access cell chromosomes. In the third step, termed strand transfer, the integrase protein joins the previously processed 3' ends to the 5' ends of strands of target cellular DNA at the site of integration. The 5'-ends are produced by integrase-catalyzed staggered cuts, 5 bp apart. A Y-shaped, gapped, recombination intermediate results, with the 5'-ends of the viral DNA strands and the 3' ends of target DNA strands remaining unjoined, flanking a gap of 5 bp. The last step is viral DNA integration into host chromosome. This involves host DNA repair synthesis in which the 5 bp gaps between the unjoined strands are filled in and then ligated. Since this process occurs at both cuts flanking the HIV genome, a 5 bp duplication of host DNA is produced at the ends of HIV-1 integration. Alternatively, Integrase may catalyze the excision of viral DNA just after strand transfer, this is termed disintegration.
Target Validation
T15352
UniProt ID
P03366 (600-1159)
Sequence
PISPIETVPVKLKPGMDGPKVKQWPLTEEKIKALVEICTEMEKEGKISKIGPENPYNTPV
FAIKKKDSTKWRKLVDFRELNKRTQDFWEVQLGIPHPAGLKKKKSVTVLDVGDAYFSVPL
DEDFRKYTAFTIPSINNETPGIRYQYNVLPQGWKGSPAIFQSSMTKILEPFKKQNPDIVI
YQYMDDLYVGSDLEIGQHRTKIEELRQHLLRWGLTTPDKKHQKEPPFLWMGYELHPDKWT
VQPIVLPEKDSWTVNDIQKLVGKLNWASQIYPGIKVRQLCKLLRGTKALTEVIPLTEEAE
LELAENREILKEPVHGVYYDPSKDLIAEIQKQGQGQWTYQIYQEPFKNLKTGKYARMRGA
HTNDVKQLTEAVQKITTESIVIWGKTPKFKLPIQKETWETWWTEYWQATWIPEWEFVNTP
PLVKLWYQLEKEPIVGAETFYVDGAANRETKLGKAGYVTNKGRQKVVPLTNTTNQKTELQ
AIYLALQDSGLEVNIVTDSQYALGIIQAQPDKSESELVNQIIEQLIKKEKVYLAWVPAHK
GIGGNEQVDKLVSAGIRKIL
Drugs and Mode of Action
Drug(s) Abacavir Drug Info Approved Human immunodeficiency virus infection [1]
Adefovir Dipivoxil Drug Info Approved HBV infection [2]
Delavirdine Drug Info Approved Human immunodeficiency virus infection [3]
Didanosine Drug Info Approved Human immunodeficiency virus infection [4], [5]
Efavirenz Drug Info Approved Human immunodeficiency virus infection [3]
Emtricitabine Drug Info Approved Hepatitis virus infection; Human immunodeficiency virus infection [6], [7], [5]
Etravirine Drug Info Approved HIV-1 infection [8], [9]
Lamivudine Drug Info Approved HIV infection; Chronic hepatitis b [5]
Nevirapine Drug Info Approved Human immunodeficiency virus infection [3]
Stavudine Drug Info Approved Human immunodeficiency virus infection [5]
Tenofovir Drug Info Approved Human immunodeficiency virus infection [10]
Tenofovir disoproxil fumarate Drug Info Approved Unspecified [11]
Zalcitabine Drug Info Approved Human immunodeficiency virus infection [12], [5]
Zidovudine Drug Info Approved Human immunodeficiency virus infection [13], [5]
Apricitabine Drug Info Phase 3 Human immunodeficiency virus infection [14]
Emtricitabine Drug Info Phase 3 HBV infection [15]
Glyminox Drug Info Phase 3 Sexually transmitted infection [16]
MK-1439 Drug Info Phase 3 Human immunodeficiency virus infection [17]
VM-1500 Drug Info Phase 2/3 Human immunodeficiency virus infection [18]
Alovudine Drug Info Phase 2 Breast cancer [19]
Amdoxovir Drug Info Phase 2 HBV infection [20]
BILR-355 Drug Info Phase 2 Human immunodeficiency virus infection [21]
EMIVIRINE Drug Info Phase 2 Human immunodeficiency virus infection [22]
F4co vaccine Drug Info Phase 2 Human immunodeficiency virus infection [23], [24]
GS-7340 Drug Info Phase 2 Human immunodeficiency virus infection [25]
IDX899 Drug Info Phase 2 Human immunodeficiency virus infection [26]
L-697,661 Drug Info Phase 2 Human immunodeficiency virus infection [27]
Lersivirine Drug Info Phase 2 Human immunodeficiency virus infection [28]
NRT inhibitor Drug Info Phase 2 Human immunodeficiency virus infection [29]
OBP-601 Drug Info Phase 2 HIV-1 infection [30]
RALURIDINE Drug Info Phase 2 Human immunodeficiency virus infection [31], [32]
Ad35-GRIN Drug Info Phase 1/2 Human immunodeficiency virus infection [33]
Ad35-GRIN/ENV Drug Info Phase 1 Human immunodeficiency virus infection [34]
AIC-292 Drug Info Phase 1 Human immunodeficiency virus infection [35]
ATEVIRDINE Drug Info Phase 1 Human immunodeficiency virus infection [36]
CALANOLIDE A Drug Info Phase 1 Mycobacterium tuberculosis infection [37]
Capravirine Drug Info Phase 1 Human immunodeficiency virus infection [38]
CMX-157 Drug Info Phase 1 Human immunodeficiency virus infection [39]
GW-695634 Drug Info Phase 1 Human immunodeficiency virus infection [40]
KM-023 Drug Info Phase 1 Human immunodeficiency virus infection [41]
MK-6186 Drug Info Phase 1 Human immunodeficiency virus infection [42]
MSH-372 Drug Info Phase 1 Human immunodeficiency virus infection [43]
TROVIRDINE HYDROCHLORIDE Drug Info Phase 1 Human immunodeficiency virus infection [44]
UC-781 Drug Info Phase 1 Human immunodeficiency virus infection [45], [46]
Lobucavir Drug Info Discontinued in Phase 3 Viral infections [47]
AZT-P-DDI Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [48]
DMP-961 Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [49]
Elvucitabine Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [50]
FOZIVUDINE TIDOXIL Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [51]
L-696229 Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [52]
Lodenosine Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [53]
Loviride Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [54]
Opaviraline Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [55]
R-18893 Drug Info Discontinued in Phase 2 Human immunodeficiency virus infection [56]
DPC-082 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [57]
L-697639 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [58]
PNU-142721 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [59]
R-82150 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [60]
R-82913 Drug Info Discontinued in Phase 1 Human immunodeficiency virus infection [61]
A-79296 Drug Info Terminated Herpes simplex virus infection [62]
ANX-201 Drug Info Terminated Cytomegalovirus infection [63]
BAY-Z-4305 Drug Info Terminated HIV-1 infection [64]
BEA-005 Drug Info Terminated Cytomegalovirus infection [65]
C-AFG Drug Info Terminated Viral infections [66]
DMP-963 Drug Info Terminated Human immunodeficiency virus infection [67]
DPC-A78277 Drug Info Terminated Human immunodeficiency virus infection [68]
GS-9148 Drug Info Terminated Human immunodeficiency virus infection [69]
ISIS-1082 Drug Info Terminated Viral infections [70]
MEN-10690 Drug Info Terminated HIV-1 infection [71]
MEN-10880 Drug Info Terminated HIV-1 infection [72]
MEN-10979 Drug Info Terminated HIV-1 infection [73]
MIV-170 Drug Info Terminated Human immunodeficiency virus infection [74]
MSC-204 Drug Info Terminated Human immunodeficiency virus infection [75]
Navuridine Drug Info Terminated Human immunodeficiency virus infection [76]
RDEA-427 Drug Info Terminated Human immunodeficiency virus infection [77]
RDEA-640 Drug Info Terminated Human immunodeficiency virus infection [77]
SPD-756 Drug Info Terminated Human immunodeficiency virus infection [78]
UC-38 Drug Info Terminated Human immunodeficiency virus infection [79]
UC-84 Drug Info Terminated Human immunodeficiency virus infection [80]
Adefovir Dipivoxil Drug Info Investigative Discovery agent [81]
Modulator A-79296 Drug Info [82]
Adefovir Dipivoxil Drug Info [83]
Alovudine Drug Info
Amdoxovir Drug Info
ANX-201 Drug Info
Apricitabine Drug Info
ATEVIRDINE Drug Info [84]
AZT nucleotide mimics Drug Info
BEA-005 Drug Info [85]
C-AFG Drug Info [86]
Delavirdine Drug Info [83]
E-EBU-dM Drug Info
Efavirenz Drug Info [83]
Elvucitabine Drug Info
EMIVIRINE Drug Info
Emtricitabine Drug Info [6], [7]
Etravirine Drug Info [8]
IDX899 Drug Info
ISIS-1082 Drug Info [87]
L-697,661 Drug Info
Lamivudine Drug Info [83]
Lobucavir Drug Info
MEN-10690 Drug Info [88]
MEN-10880 Drug Info [88]
MEN-10979 Drug Info [89]
MSC-204 Drug Info [90]
Nevirapine Drug Info
Opaviraline Drug Info [91]
R-18893 Drug Info [92]
R-82150 Drug Info
R-82913 Drug Info
Tenofovir disoproxil fumarate Drug Info [93], [7]
TNK-651 Drug Info
TROVIRDINE HYDROCHLORIDE Drug Info
UC-38 Drug Info [94]
UC-84 Drug Info [95]
Inhibitor Abacavir Drug Info [96]
AIC-292 Drug Info [97]
AZT-P-DDI Drug Info [98], [11]
BAY-Z-4305 Drug Info [99]
BILR-355 Drug Info [100], [11]
CALANOLIDE A Drug Info [101]
Capravirine Drug Info [102]
CMX-157 Drug Info [103]
Didanosine Drug Info [104]
DMP-961 Drug Info [105], [11]
DMP-963 Drug Info [105], [11]
DPC-082 Drug Info [106], [11]
DPC-A78277 Drug Info [107]
FOZIVUDINE TIDOXIL Drug Info [108], [11]
Glyminox Drug Info [109]
GS-7340 Drug Info [110]
GS-9148 Drug Info [111]
GW-695634 Drug Info [112]
KM-023 Drug Info [113]
L-696229 Drug Info [114], [11]
L-697639 Drug Info [115]
Lersivirine Drug Info [116]
Lodenosine Drug Info [117]
Loviride Drug Info [118]
MIV-170 Drug Info [119]
MK-1439 Drug Info [120]
MK-6186 Drug Info [121]
MSH-372 Drug Info [90]
Navuridine Drug Info [122]
NRT inhibitor Drug Info [123]
NSC-625487 Drug Info [124], [11]
OBP-601 Drug Info [125]
PNU-142721 Drug Info [126]
RALURIDINE Drug Info [127], [11]
RDEA-427 Drug Info [128]
RDEA-640 Drug Info [129]
SPD-756 Drug Info [130]
Stavudine Drug Info [131]
Tenofovir Drug Info [132]
UC-781 Drug Info [133]
VM-1500 Drug Info [134]
Zalcitabine Drug Info [131]
Zidovudine Drug Info [132]
References
REF 1Abacavir (marketed as Ziagen) and Abacavir-containing Medications. FDA. 2008.
REF 2Telbivudine: a new option for the treatment of chronic hepatitis B. Expert Opin Biol Ther. 2007 May;7(5):751-61.
REF 3Approved antiretroviral drugs. Antiretroviral Drugs. Company report of AVERT. 2009.
REF 4(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: 4833).
REF 5Natural 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 6Emtricitabine: a novel nucleoside reverse transcriptase inhibitor. Drugs Today (Barc). 2005 Apr;41(4):241-52.
REF 7Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 82008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
REF 9Emerging antiviral drugs. Expert Opin Emerg Drugs. 2008 Sep;13(3):393-416.
REF 10Anti-hepatitis B virus activity in vitro of combinations of tenofovir with nucleoside/nucleotide analogues. Antivir Chem Chemother. 2009;19(4):165-76.
REF 11Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 12(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: 4828).
REF 13(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: 4825).
REF 14ClinicalTrials.gov (NCT00686270) A Long Term Safety Study of Apricitabine in HIV-infected Patients. U.S. National Institutes of Health.
REF 15Clinical pipeline report, company report or official report of Gilead (2011).
REF 16ClinicalTrials.gov (NCT00129532) Trial of SAVVY and HIV in Ghana. U.S. National Institutes of Health.
REF 17ClinicalTrials.gov (NCT02403674) Comparison of MK-1439A and ATRIPLA in Treatment-Naive Human Immunodeficiency Virus (HIV)-Infected Participants (MK-1439A-021). U.S. National Institutes of Health.
REF 18ClinicalTrials.gov (NCT02489461) Efficacy, Safety and Optimal Dose Selection VM-1500 in Comparison to Efavirenz When Added to Standard-of-care Antiretroviral Therapy.
REF 19ClinicalTrials.gov (NCT02232581) Study to Determine the Antiviral Activity and Safety of Alovudine in Nucleoside-experienced HIV-infected Subjects Experiencing Virologic Failure. U.S. National Institutes of Health.
REF 20ClinicalTrials.gov (NCT01738555) A Safety and Efficacy Study of Amdoxovir in HIV-1 Treatment-experienced Subjects. U.S. National Institutes of Health.
REF 21ClinicalTrials.gov (NCT00294372) Phase II Study on the Antiviral Activity and Safety of BILR 355 BS in HIV-1 Infected, NNRTI-treated Patients. U.S. National Institutes of Health.
REF 22ClinicalTrials.gov (NCT00002413) A Study of MKC-442 in HIV-Positive Patients. U.S. National Institutes of Health.
REF 23ClinicalTrials.gov (NCT01218113) Efficacy and Safety of GSK Biologicals HIV Vaccine in Antiretroviral Therapy (ART)-naive HIV-1 Infected Persons. U.S. National Institutes of Health.
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027409)
REF 25ClinicalTrials.gov (NCT01565850) Safety and Efficacy of Darunavir/Cobicistat/Emtricitabine/GS-7340 Single Tablet Regimen Versus Cobicistat-boosted Darunavir Plus Emtricitabine/Tenofovir Disoproxil Fumarate Fixed Dose Combination in HIV-1 Infected, Antiretroviral Treatment Naive Adults. U.S. National Institutes of Health.
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027243)
REF 27A short-term clinical evaluation of L-697,661, a non-nucleoside inhibitor of HIV-1 reverse transcriptase. L-697,661 Working Group. N Engl J Med. 1993 Oct 7;329(15):1065-72.
REF 28ClinicalTrials.gov (NCT01254656) A Long Term Safety Study Of Lersivirine For The Treatment Of HIV-1 Infection In Subjects Who Have Completed Treatment With Lersivirine In Studies A5271015 And A5271022. U.S. National Institutes of Health.
REF 29Pipeline report of Bristol-Myers Squibb in August 2013.
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024698)
REF 31ClinicalTrials.gov (NCT00002338) The Safety and Effectiveness of 935U83 in HIV-Infected Patients. U.S. National Institutes of Health.
REF 32Safety and pharmacokinetics of 5-chloro-2',3'-dideoxy-3'-fluorouridine (935U83) following oral administration of escalating single doses in human immunodeficiency virus-infected adults. Antimicrob Agents Chemother. 1996 Dec;40(12):2842-7.
REF 33ClinicalTrials.gov (NCT02099994) Safety & Immunogenicity of HIV Vaccines in Healthy Kenyan Adults. U.S. National Institutes of Health.
REF 34ClinicalTrials.gov (NCT01496989) Safety and Immunogenicity Study of HIV-MAG Vaccine +/- IL-12 and Ad35-GRIN/ENV in HIV-uninfected Volunteers. U.S. National Institutes of Health.
REF 35Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032413)
REF 36ClinicalTrials.gov (NCT00000753) A Phase I Concentration-Targeted Multidose Study of Atevirdine Mesylate ( U-87201E ), AZT, and ddI or ddC. U.S. National Institutes of Health.
REF 37ClinicalTrials.gov (NCT00005120) The Safety and Effectiveness of (+)-Calanolide A in HIV-Infected Patients Who Have Never Taken Anti-HIV Drugs. U.S. National Institutes of Health.
REF 38ClinicalTrials.gov (NCT00002214) Phase I Trial of S-1153 in Patients With HIV Infection. U.S. National Institutes of Health.
REF 39ClinicalTrials.gov (NCT01080820) A Safety, Tolerability and Pharmacokinetic Study of a Single Dose of CMX157 in Healthy Volunteers. U.S. National Institutes of Health.
REF 40ClinicalTrials.gov (NCT00090077) Monotherapy Versus Placebo Over 7 Days-Non-Nucleoside Reverse Transcriptase Inhibitor-Experienced HIV1 Infected Adults. U.S. National Institutes of Health.
REF 41ClinicalTrials.gov (NCT01348516) Single Ascending Dose (SAD)/Multiple Ascending Dose(MAD) Safety/Pharmacokinetic (PK) Study of KM-023. U.S. National Institutes of Health.
REF 42ClinicalTrials.gov (NCT01152255) MK6186 in HIV-1 Infected Patients (MK-6186-007 AM2). U.S. National Institutes of Health.
REF 43ClinicalTrials.gov (NCT02033109) Safety, Pharmacokinetics and Acceptability of PC-1005 for Vaginal Use. U.S. National Institutes of Health.
REF 44Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002628)
REF 45ClinicalTrials.gov (NCT00441909) Phase I Study of Safety and Persistence of UC-781 Vaginal Microbicide. U.S. National Institutes of Health.
REF 46First phase 1 double-blind, placebo-controlled, randomized rectal microbicide trial using UC781 gel with a novel index of ex vivo efficacy. PLoS One. 2011;6(9):e23243.
REF 47Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002213)
REF 48Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005869)
REF 49Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011150)
REF 50Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007421)
REF 51Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007452)
REF 52Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001460)
REF 53Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005453)
REF 54Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002631)
REF 55Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011603)
REF 56Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002204)
REF 57Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014106)
REF 58Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002199)
REF 59Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010327)
REF 60Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002478)
REF 61Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001064)
REF 62Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003585)
REF 63Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014324)
REF 64Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012173)
REF 65Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008999)
REF 66Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003394)
REF 67Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011151)
REF 68Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800020281)
REF 69Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016343)
REF 70Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001244)
REF 71Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008240)
REF 72[Abstract Book Vol. 2, International Conference on AIDS (10th: 1994: Yokohama, Japan)], International AIDS Society, 1994.
REF 73Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008234)
REF 74Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019379)
REF 75Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009440)
REF 76Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001006)
REF 77Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024208)
REF 78Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013016)
REF 79Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005073)
REF 80Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005397)
REF 81The ChEMBL database in 2017.
REF 82US patent application no. 5,830,759, Unique associated kaposi's sarcoma virus sequences and uses thereof.
REF 83Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 84J 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 reversetranscriptase inhibitors.
REF 85Efficacy of Postexposure Prophylaxis after Intravaginal Exposure of Pig-Tailed Macaques to a Human-Derived Retrovirus (Human Immunodeficiency Virus Type 2). J Virol. 2000 October; 74(20): 9771-9775.
REF 86Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003394)
REF 87Comparison of the toxicity profiles of ISIS 1082 and ISIS 2105, phosphorothioate oligonucleotides, following subacute intradermal administration in Sprague-Dawley rats. Toxicology. 1997 Jan 15;116(1-3):77-88.
REF 88US patent application no. 2004,0023,290, Novel therapeutic agents that modulate enzymatic processes.
REF 89New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase. Antiviral Res. 1996 May;30(2-3):109-24.
REF 90WO patent application no. 2004,0290,42, Pyrazole derivatives as reverse transcriptase inhibitors.
REF 91Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 92EP patent application no. 0767664, Combination therapy for hiv infection.
REF 93Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48.
REF 94Biological and biochemical anti-human immunodeficiency virus activity of UC 38, a new non-nucleoside reverse transcriptase inhibitor. J Pharmacol Exp Ther. 1996 Jan;276(1):298-305.
REF 95Crystal structures of HIV-1 reverse transcriptase in complex with carboxanilide derivatives. Biochemistry. 1998 Oct 13;37(41):14394-403.
REF 96Quadruple nucleos(t)ide reverse transcriptase inhibitors-only regimen of tenofovir plus zidovudine/lamivudine/abacavir in heavily pre-treated HIV-1 infected patients: salvage therapy or backbone only? Curr HIV Res. 2009 May;7(3):320-6.
REF 97In vitro and in vivo activities of AIC292, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2013 Nov;57(11):5320-9.
REF 98Antiviral activities of nucleotide heterodimers against human immunodeficiency virus type 1 in vitro. Antiviral Res. 1996 Jun;31(1-2):115-20.
REF 99US patent application no. 2008,0161,324, Compositions and methods for treatment of viral diseases.
REF 100Evaluation of steady-state pharmacokinetic interactions between ritonavir-boosted BILR 355, a non-nucleoside reverse transcriptase inhibitor, and lamivudine/zidovudine in healthy subjects. J Clin Pharm Ther. 2012 Feb;37(1):81-8.
REF 101Calanolide A: a natural non-nucleoside reverse transcriptase inhibitor. BETA. 1999 Apr;12(2):8-9.
REF 102Metabolism and excretion of capravirine, a new non-nucleoside reverse transcriptase inhibitor, alone and in combination with ritonavir in healthy volunteers. Drug Metab Dispos. 2004 Jul;32(7):689-98.
REF 103Practical Considerations For Developing Nucleoside Reverse Transcriptase Inhibitors. Drug Discov Today Technol. 2012 Autumn; 9(3): e183-e193.
REF 104The effect of individual antiretroviral drugs on body composition in HIV-infected persons initiating highly active antiretroviral therapy. J Acquir Immune Defic Syndr. 2009 Jul 1;51(3):298-304.
REF 105Effect of drug substance particle size on the characteristics of granulation manufactured in a high-shear mixer. AAPS PharmSciTech. 2000 December; 1(4): 55-61.
REF 106Expanded-spectrum nonnucleoside reverse transcriptase inhibitors inhibit clinically relevant mutant variants of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 1999 Dec;43(12):2893-7.
REF 107The chimpanzee (Pan troglodytes) as a pharmacokinetic model for selection of drug candidates: model characterization and application. Drug Metab Dispos. 2004 Dec;32(12):1359-69. Epub 2004 Aug 27.
REF 108Fozivudine tidoxil as single-agent therapy decreases plasma and cell-associated viremia during acute feline immunodeficiency virus infection. J Vet Intern Med. 2011 May-Jun;25(3):413-8.
REF 109Glyminox Biosyn. Curr Opin Investig Drugs. 2004 Feb;5(2):222-31.
REF 110Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue. Antimicrob Agents Chemother. 2005 May;49(5):1898-906.
REF 111Novel nucleotide human immunodeficiency virus reverse transcriptase inhibitor GS-9148 with a low nephrotoxic potential: characterization of renal transport and accumulation. Antimicrob Agents Chemother. 2009 Jan;53(1):150-6.
REF 112Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors. Curr Opin Investig Drugs. 2006 Feb;7(2):128-35.
REF 113Pharmacokinetics and tolerability of the new second-generation nonnucleoside reverse- transcriptase inhibitor KM-023 in healthy subjects. Drug Des Devel Ther. 2014 Sep 26;8:1613-9.
REF 114L-696,229 specifically inhibits human immunodeficiency virus type 1 reverse transcriptase and possesses antiviral activity in vitro.. Antimicrob Agents Chemother. 1992 May; 36(5): 1019-1023.
REF 115Human pharmacokinetics and tolerability of L-697,639, a non-nucleoside HIV-1 reverse transcriptase inhibitor. Int J Clin Pharmacol Res. 1994;14(2):45-50.
REF 116Safety and tolerability of lersivirine, a nonnucleoside reverse transcriptase inhibitor, during a 28-day, randomized, placebo-controlled, Phase I clinical study in healthy male volunteers. Clin Ther.2010 Oct;32(11):1889-95.
REF 1172?,3?-Dialdehyde of ATP, ADP, and adenosine inhibit HIV-1 reverse transcriptase and HIV-1 replication. Curr HIV Res. 2014;12(5):347-58.
REF 118Nucleoside reverse transcriptase inhibitor resistance mutations associated with first-line stavudine-containing antiretroviral therapy: programmatic implications for countries phasing out stavudine. J Infect Dis. 2013 Jun 15;207 Suppl 2:S70-7.
REF 119Inhibition of HIV-1 by non-nucleoside reverse transcriptase inhibitors via an induced fit mechanism-Importance of slow dissociation and relaxation rates for antiviral efficacy. Biochem Pharmacol. 2010 Oct 15;80(8):1133-40.
REF 120Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses. Bioorg Med Chem Lett. 2014 Feb 1;24(3):917-22.
REF 121Antiviral activity and in vitro mutation development pathways of MK-6186, a novel nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2012 Jun;56(6):3324-35.
REF 122Synthesis and anti-human immunodeficiency virus (HIV-1) activity of 3'-deoxy-3'-(triazol-1-yl)thymidines and 2',3'-dideoxy-3'-(triazol-1-yl)uridines and inhibition of reverse transcriptase by their 5'-triphosphates. Chem Pharm Bull (Tokyo). 1990 Sep;38(9):2597-601.
REF 123Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor. J Biol Chem. 2009 Dec 18;284(51):35681-91.
REF 124Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors. Antivir Chem Chemother. 1999 Jul;10(4):211-7.
REF 125Antiviral drug resistance and the need for development of new HIV-1 reverse transcriptase inhibitors. Antimicrob Agents Chemother. 2012 Oct;56(10):5000-8.
REF 126Activation of the human nuclear xenobiotic receptor PXR by the reverse transcriptase-targeted anti-HIV drug PNU-142721. Protein Sci. 2011 Oct;20(10):1713-9.
REF 1275-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile. Antimicrob Agents Chemother. 1994 Jul;38(7):1590-603.
REF 128CN patent application no. 103360398, Triazolopyrimidine hiv-1 retrovirus inhibitor and its preparation method and application thereof.
REF 129WO patent application no. 2008,0165,22, Novel hiv reverse transcriptase inhibitors.
REF 130Single dose pharmacokinetics of SPD-756 in healthy adult volunteers, P F Smith, Poster Exhibition: The XIV International AIDS Conference: Abstract no. WePeB6050.
REF 131Primer unblocking by HIV-1 reverse transcriptase and resistance to nucleoside RT inhibitors (NRTIs). Int J Biochem Cell Biol. 2004 Sep;36(9):1687-705.
REF 132Antiviral drugs in current clinical use. J Clin Virol. 2004 Jun;30(2):115-33.
REF 133The nonnucleoside reverse transcriptase inhibitor UC-781 inhibits human immunodeficiency virus type 1 infection of human cervical tissue and dissemination by migratory cells. J Virol. 2005 Sep;79(17):11179-86.
REF 134127??afety, pharmokinetics and efficacy of VM-1500, a novel reverse transcriptase inhibitor, In healthy volunteers and HIV-infected patients. J Acquir Immune Defic Syndr. 2014 April; 65(Suppl 2): 52.

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