Structural basis for the resilience of efavirenz (DMP-266) to drug resistance mutations in HIV-1 reverse transcriptase

Structure

Volumn 8, Issue 10, 2000, Pages 1089-1094

  Ren, Jingshan ^a   Milton, John ^b   Weaver, Kurt L ^c   Short, Steven A ^c   Stuart, David I ^a,d   Stammers, David K ^a,d  

^a UNIVERSITY OF OXFORD   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GLAXOSMITHKLINE   (United States)

^d UNIVERSITY OF OXFORD   (United Kingdom)

Author keywords

Drug resistance; Efavirenz; HIV 1; Nevirapine; Reverse transcriptase

Indexed keywords

ANILIDE; BENZOXAZINE DERIVATIVE; EFAVIRENZ; N [4 CHLORO 3 (3 METHYL 2 BUTENYLOXY)PHENYL] 2 METHYL 3 FURANCARBOTHIOAMIDE; NEVIRAPINE; QUINOXALINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ARTICLE; CONFORMATIONAL TRANSITION; CRYSTAL STRUCTURE; DRUG BINDING; DRUG BINDING SITE; DRUG EFFECT; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; PRIORITY JOURNAL; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

AMINO ACID SUBSTITUTION; ANTI-HIV AGENTS; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; DRUG RESISTANCE, MICROBIAL; HIV-1; HIV-1 REVERSE TRANSCRIPTASE; HUMANS; MODELS, MOLECULAR; MUTATION; NEVIRAPINE; OXAZINES; PROTEIN BINDING; PROTEIN CONFORMATION; REVERSE TRANSCRIPTASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034435564     PISSN: 09692126     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-2126(00)00513-X     Document Type: Article

References (30)

1. Combination therapy for HIV: The effect on inpatient activity, morbidity and mortality of a cohort of patients
2. Changing patterns of mortality across Europe in patients infected with HIV-1
3. Multidrug-resistant human immunodeficiency virus type 1 strains resulting from combination antiretroviral therapy
4. A family of insertion mutations between codons 67 and 70 of human immunodeficiency virus type 1 reverse transcriptase confer multinucleoside analog resistance
5. Structure of a covalently trapped catalytic complex of HIV-1 reverse transcriptase: Implications for drug resistance
6. Crystal structure at 3.5 Å resolution of HIV-1 reverse transcriptase complexed with an inhibitor
7. High resolution structures of HIV-1 RT from four RT-inhibitor complexes
8. Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors
9. Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors
10. Mechanism of inhibition of HIV-1 reverse transcriptase by nonnucleoside inhibitors
11. Crystal structures of HIV-1 reverse transcriptase in complex with carboxanilide derivatives
12. Crystallographic analysis of the binding modes of thiozolo-isoindolinone non-nucleoside inhibitors to HIV-1 reverse transcriptase and comparison with modelling studies
13. Phenylethylthiazolylthiourea (PETT) non-nucleoside inhibitors of HIV-1 and HIV-2 reverse transcriptases: Structural and biochemical analyses
14. Mutations in retroviral genes associated with drug resistance
15. L-743, 726 (DMP-266): A novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase
16. Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication
17. Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication
18. Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors
19. Design of MKC-442 (Emivirine) analogues with improved activity against drug resistant HIV mutants
20. Binding of the second generation non-nucleoside inhibitor S-1153 to HIV-1 RT involves extensive main chain hydrogen bonding
21. Crystals of HIV-1 reverse transcriptase diffracting to 2.2 Å resolution
22. 3′-azido-3′-deoxythymidine drug resistance mutations in HIV-1 reverse transcriptase can induce long range conformational changes
23. X-ray diffraction data collection system for modern protein crystallography with a Weissenberg camera and an imaging plate using synchrotron radiation
24. Processing of X-ray diffraction data collected in oscillation mode
25. The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: Lessons for inhibitor design
26. Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine U-90152 explain resistance mutations for this non-nucleoside inhibitor
27. Crystallography and NMR system: A new software suite for macromolecular structure determination
28. Interactive computer graphics: FRODO
29. Continuous and discontinuous changes in the unit cell of HIV-1 reverse transcriptase crystals on dehydration