Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase …
K Das, AD Clark, PJ Lewi, J Heeres… - Journal of medicinal …, 2004 - ACS Publications
Anti-AIDS drug candidate and non-nucleoside reverse transcriptase inhibitor (NNRTI)
TMC125-R165335 (etravirine) caused an initial drop in viral load similar to that observed …
TMC125-R165335 (etravirine) caused an initial drop in viral load similar to that observed …
Crystal structures of HIV-1 reverse transcriptase with etravirine (TMC125) and rilpivirine (TMC278): implications for drug design
EB Lansdon, KM Brendza, M Hung… - Journal of medicinal …, 2010 - ACS Publications
Diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitors (NNRTIs) have
inherent flexibility, helping to maintain activity against a wide range of resistance mutations …
inherent flexibility, helping to maintain activity against a wide range of resistance mutations …
[HTML][HTML] Crystallography and the design of anti-AIDS drugs: conformational flexibility and positional adaptability are important in the design of non-nucleoside HIV-1 …
Drug resistance is a key cause of failure for treatment of HIV infection. The efficacy of non-
nucleoside reverse transcriptase inhibiting (NNRTI) drugs is impaired by rapid emergence of …
nucleoside reverse transcriptase inhibiting (NNRTI) drugs is impaired by rapid emergence of …
High-resolution structures of HIV-1 reverse transcriptase/TMC278 complexes: strategic flexibility explains potency against resistance mutations
TMC278 is a diarylpyrimidine (DAPY) nonnucleoside reverse transcriptase inhibitor (NNRTI)
that is highly effective in treating wild-type and drug-resistant HIV-1 infections in clinical trials …
that is highly effective in treating wild-type and drug-resistant HIV-1 infections in clinical trials …
Validation of a model for the complex of HIV-1 reverse transcriptase with nonnucleoside inhibitor TMC125
M Udier-Blagović, J Tirado-Rives… - Journal of the American …, 2003 - ACS Publications
The structure for the complex of nonnucleoside inhibitor TMC125 and HIV-1 reverse
transcriptase has been determined and validated through computation of resistance profiles …
transcriptase has been determined and validated through computation of resistance profiles …
Crystal engineering of HIV-1 reverse transcriptase for structure-based drug design
Abstract HIV-1 reverse transcriptase (RT) is a primary target for anti-AIDS drugs. Structures
of HIV-1 RT, usually determined at∼ 2.5–3.0 Å resolution, are important for understanding …
of HIV-1 RT, usually determined at∼ 2.5–3.0 Å resolution, are important for understanding …
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms
D Li, P Zhan, E De Clercq, X Liu - Journal of medicinal chemistry, 2012 - ACS Publications
Currently, five NNRTIs have been approved by US Food and Drug Administration (US FDA)
for the clinical treatment of AIDS, ie, nevirapine, delavirdine, efavirenz, etravirine, and …
for the clinical treatment of AIDS, ie, nevirapine, delavirdine, efavirenz, etravirine, and …
Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIV reverse transcriptase
J Ren, DK Stammers - Virus research, 2008 - Elsevier
The selection of drug resistant virus is a significant obstacle to the continued successful
treatment of HIV infection. Reverse transcriptase is the target for numerous approved anti …
treatment of HIV infection. Reverse transcriptase is the target for numerous approved anti …
Design strategies of novel NNRTIs to overcome drug resistance
P Zhan, X Liu, Z Li, C Pannecouque… - Current medicinal …, 2009 - ingentaconnect.com
Nonnucleoside reverse transcriptase inhibitors (NNRTIs) are very potent and most
promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT) …
promising anti-AIDS drugs that specifically inhibit HIV-1 reverse transcriptase (RT) …
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors
Owing to the emergence of resistant virus, next generation non-nucleoside HIV reverse
transcriptase inhibitors (NNRTIs) with improved drug resistance profiles have been …
transcriptase inhibitors (NNRTIs) with improved drug resistance profiles have been …
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