Roles of Conformational and Positional Adaptability in Structure-Based Design of TMC125-R165335 (Etravirine) and Related Non-nucleoside Reverse Transcriptase Inhibitors That Are Highly Potent and Effective against Wild-Type and Drug-Resistant HIV-1 Variants

Journal of Medicinal Chemistry

Volumn 47, Issue 10, 2004, Pages 2550-2560

  Das, Kalyan ^a   Clark Jr , Arthur D ^a   Lewi, Paul J ^b   Heeres, Jan ^b   De Jonge, Marc R ^b   Koymans, Lucien M H ^b   Vinkers, H Maarten ^b   Daeyaert, Frederik ^b   Ludovici, Donald W ^c   Kukla, Michael J ^c   De Corte, Bart ^c   Kavash, Robert W ^c   Ho, Chih Y ^c   Ye, Hong ^c   Lichtenstein, Mark A ^c   Andries, Koen ^d   Pauwels, Rudi ^d   De Béthune, Marie Pierre ^d   Boyer, Paul L ^e   Clark, Patrick ^e   Hughes, Stephen H ^e   Janssen, Paul A J ^b   Arnold, Eddy ^a,f   more..

^a RUTGERS UNIVERSITY   (United States)

^b Center for Molecular Design   (Belgium)

^c JANSSEN RESEARCH AND DEVELOPMENT   (United States)

^d Virco BVBA   (Belgium)

^e NATIONAL CANCER INSTITUTE   (United States)

^f RUTGERS UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ETRAVIRINE; PYRIMIDINE DERIVATIVE; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ACQUIRED IMMUNE DEFICIENCY SYNDROME; ANTIVIRAL ACTIVITY; ARTICLE; CHEMICAL BINDING; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG BINDING; DRUG CONFORMATION; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; NONHUMAN; STRUCTURE ACTIVITY RELATION; VIRUS MUTATION; VIRUS RESISTANCE;

ANTI-HIV AGENTS; CRYSTALLOGRAPHY, X-RAY; DRUG RESISTANCE, VIRAL; HIV-1 REVERSE TRANSCRIPTASE; MODELS, MOLECULAR; MUTATION; PROTEIN CONFORMATION; PYRIDAZINES; PYRIMIDINES; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 2342620790     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm030558s     Document Type: Article

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