The inhibition of human immunodeficiency virus type 1 in vitro by a non-nucleoside reverse transcriptase inhibitor MKC-442, alone and in combination with other anti-HIV compounds

Antiviral Research

Volumn 26, Issue 2, 1995, Pages 173-187

  Brennan, Tara M ^a   Taylor, Debra L ^a   Bridges, C Gordon ^a   Leyda, James P ^b   Tyms, A Stanley ^a  

^a MEDICAL RESEARCH COUNCIL   (United Kingdom)

^b Merrell Dow Research Institute   (United States)

Author keywords

Drug combination, Non nucleoside RT inhibitor; Human immunodeficiency virus

Indexed keywords

CASTANOSPERMINE 6 BUTYRATE; DIDANOSINE; EMIVIRINE; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; ZALCITABINE; ZIDOVUDINE;

ARTICLE; CONTROLLED STUDY; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; IN VITRO STUDY; PRIORITY JOURNAL; VIRUS INHIBITION;

ANTIVIRAL AGENTS; CELLS, CULTURED; CYTOTOXICITY TESTS, IMMUNOLOGIC; DIDANOSINE; DRUG INTERACTIONS; HIV-1; HIV-1 REVERSE TRANSCRIPTASE; HUMAN; INDOLIZINES; ISOQUINOLINES; LEUKOCYTES, MONONUCLEAR; MOLECULAR STRUCTURE; NEVIRAPINE; PYRIDINES; QUINOLINES; REVERSE TRANSCRIPTASE INHIBITORS; SAQUINAVIR; URACIL; ZALCITABINE; ZIDOVUDINE;

HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 0028919933     PISSN: 01663542     EISSN: None     Source Type: Journal    
DOI: 10.1016/0166-3542(94)00074-I     Document Type: Article

References (46)

1. Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative
2. Potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by 5-ethyl-6-phenylthiouracil derivatives through their interaction with the HIV-1 reverse transcriptase
3. Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro
4. 2′,5′-Bis-O-(tert-butyldimethylsilyl)-3′-spiro-5″-(4″-amino-1″,2″-oxathiole-2″,2″dioxide) pyrimidine (TSAO) nucleoside analogues: highly selective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase
5. Treatment of human immunodeficiency virus type-1 (HIV-1)-infected cells with combinations of HIV-1 specific inhibitors results in a different resistant pattern than does treatment with single-drug therapy
6. What is synergy?
7. Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors
8. Use of evolutionary limitations of HIV-1 multidrug resistance to optimize therapy
9. Characterisation of the binding site for nevirapine (BI-RG-587), a non-nucleoside inhibitor of human immunodeficiency virus type 1 reverse transcriptase
10. In vitro resistance to an inhibitor of HIV proteinase (Ro-31-8959) relative to inhibitors of reverse transcriptase (AZT and TIBO)
11. In vitro selection of human immunodeficiency virus type 1 resistant to Ro-31-8959 proteinase inhibitor
12. The binding of a novel bis(heteroaryl)piperazine mediates inhibition of human immunodeficiency virus type 1 reverse transcriptase
13. Phenotypic and genotypic characterisation of HIV-1 variants selected during treatment with the protease inhibitor L-735,524
14. The same mutation that encodes low-level human immunodeficiency virus type-1 resistance to 2′,3′-dideoxyinosine and 2′,3′-dideoxycytidine confers high level resistance to the (−) enantiomer of 2′,3′dideoxy-3′-thiacytidine
15. Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity
16. Novel mutation in the human immunodeficiency virus type 1 reverse transcriptase gene that encodes cross-resistance to 2′,3′-dideoxyinosine and 2′,3′-dideoxycytidine
17. Antiviral activity of nevirapine at 400 mg in p24 antigen positive patients
18. Genotypic characterisation of HIV-1 from patients after prolonged treatment with proteinase inhibitor saquinavir
19. HIV with reduced sensitivity to zidovudine (AZT) isolated during prolonged therapy
20. 3′-Azido-3′-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors
21. Synthesis of potent anti-HIV agents: esters of castanospermine
22. In vitro selection and molecular characterisation of human immunodeficiency virus-1 resistant to non-nucleoside inhibitors of reverse transcriptase
23. Inhibition of HIV replication by a non-nucleoside reverse transcriptase inhibitor
24. A novel lead for specific anti-HIV 1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine
25. Dissociation of gp120 from HIV-1 virions induced by soluble CD4
26. Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors
27. In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C2 symmetrical inhibitors of HIV type 1 protease
28. Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds
29. Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives
30. Potent and highly selective HIV-1 inhibition by a new series of α-anilino phenyl acetamide (α-APA) derivatives targeted at HIV-1 reverse transcriptase
31. Human immunodeficiency virus type 1 mutants to nonnucleoside inhibitors of reverse transcriptase in tissue culture
32. The emergence of nevirapine resistance in clinical trials
33. Rational design of peptide-based HIV proteinase inhibitors
34. Nonnucleoside reverse transcriptase inhibitors that potently and specifically block human immunodeficiency virus type 1 replication
35. A short-term clinical evaluation of L-697,661, a non-nucleoside inhibitor of HIV-1 reverse transcriptase
36. Mutations in HIV-1 reverse transcriptase and protease associated with drug resistance
37. Isolation and characterisation of human immunodeficiency virus type 1 mutants resistant to nonnucleoside reverse transcriptase inhibitor, MKC-442
38. Resistance to ddI and sensitivity to AZT induced by a mutation in HIV-1 reverse transcriptase
39. Evaluation of synergism or antagonism for the combined action of antiviral agents
40. A new class of HIV-1 specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)
41. 6-O-Butanoyl castanospermine (MDL 28,574) inhibits glycoprotein processing and the growth of HIVs
42. Inhibition of α-glucosidase 1 of the glycoprotein processing enzymes by 6-O-butanoyl castanospermine (MDL 28,574) and its consequences in HIV-infected T-cells
43. Synergistic inhibition of human immunodeficiency virus type 1 in vitro by 6-O-butanoyl castanospermine (MDL 28,574), in combination with inhibitors of the virus encoded reverse transcriptase and proteinase
44. Rapid in vitro selection of human immunodeficiency virus type 1 resistant to 3′-thiacytidine inhibitors due to a mutation in the YMDD region of reverse transcriptase
45. Selective and synergistic inhibition of human immunodeficiency virus type 1 reverse transcriptase by a non-nucleoside inhibitor, MKC-422