Lamivudine (3TC) resistance in HIV-1 reverse transcriptase involves steric hindrance with β-branched amino acids

SG Sarafianos, K Das, AD Clark Jr… - Proceedings of the …, 1999 - National Acad Sciences
An important component of triple-drug anti-AIDS therapy is 2′, 3′-dideoxy-3′-thiacytidine
(3TC, lamivudine). Single mutations at residue 184 of the reverse transcriptase (RT) in HIV …

Structure of HIV-1 RT/TIBO R 86183 complex reveals similarity in the binding of diverse nonnucleoside inhibitors

J Ding, K Das, H Moereels, L Koymans… - Nature structural …, 1995 - nature.com
We report the structure of HIV-1 reverse transcriptase (RT) complexed with the
nonnucleoside inhibitor TIBO R 86183 at 3.0 Å resolution. Comparing this structure with …

[PDF][PDF] Comparative quantitative structure− activity relationship studies on anti-HIV drugs

R Garg, SP Gupta, H Gao, MS Babu… - Chemical …, 1999 - researchgate.net
In the present era, acquired immunodeficiency syndrome (AIDS) is the most fatal disorder for
which no completely successful chemotherapy has been developed so far. The pandemic …

Hormonal control of T-cell development in health and disease

W Savino, DA Mendes-da-Cruz, A Lepletier… - Nature Reviews …, 2016 - nature.com
The physiology of the thymus, the primary lymphoid organ in which T cells are generated, is
controlled by hormones. Data from animal models indicate that several peptide and …

[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 …

K Das, PJ Lewi, SH Hughes, E Arnold - Progress in biophysics and …, 2005 - Elsevier
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 …

Structure of HIV-2 reverse transcriptase at 2.35-Å resolution and the mechanism of resistance to non-nucleoside inhibitors

J Ren, LE Bird, PP Chamberlain… - Proceedings of the …, 2002 - National Acad Sciences
The HIV-2 serotype of HIV is a cause of disease in parts of the West African population, and
there is evidence for its spread to Europe and Asia. HIV-2 reverse transcriptase (RT) …

Crystal structures of 8-Cl and 9-Cl TIBO complexed with wild-type HIV-1 RT and 8-Cl TIBO complexed with the Tyr181Cys HIV-1 RT drug-resistant mutant

K Das, J Ding, Y Hsiou, AD Clark Jr, H Moereels… - Journal of molecular …, 1996 - Elsevier
Human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) is an important
target for chemotherapeutic agents used in the treatment of AIDS; the TIBO compounds are …

Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis (heteroaryl) piperazine (BHAP) U-90152 explain resistance mutations …

RM Esnouf, J Ren, AL Hopkins… - Proceedings of the …, 1997 - National Acad Sciences
The viral reverse transcriptase (RT) provides an attractive target in the search for anti-HIV
therapies. The nonnucleoside inhibitors (NNIs) are a diverse set of compounds (usually HIV …

The HIV‐1 reverse transcription (RT) process as target for RT inhibitors

H Jonckheere, J Anné… - Medicinal research reviews, 2000 - Wiley Online Library
Abstract Since the Human Immunodeficiency Virus Type 1 (HIV‐1) was identified as the
etiologic agent of the Acquired Immune Deficiency Syndrome (AIDS), the HIV‐1 reverse …

Conformational changes in HIV-1 reverse transcriptase induced by nonnucleoside reverse transcriptase inhibitor binding

N Sluis-Cremer, NA Temiz, I Bahar - Current HIV research, 2004 - ingentaconnect.com
Nonnucleoside reverse transcriptase inhibitors (NNRTI) are a group of small hydrophobic
compounds with diverse structures that specifically inhibit HIV-1 reverse transcriptase (RT) …