Impact of Residues in the Nonnucleoside Reverse Transcriptase Inhibitor Binding Pocket on HIV-1 Reverse Transcriptase Heterodimer Stability

Anna Figueiredo; Shannon Zelina; Nicolas Sluis-Cremer; Gilda Tachedjian

doi:10.2174/157016208783885065

Impact of Residues in the Nonnucleoside Reverse Transcriptase Inhibitor Binding Pocket on HIV-1 Reverse Transcriptase Heterodimer Stability

Current HIV Research ◽

10.2174/157016208783885065 ◽

2008 ◽

Vol 6 (2) ◽

pp. 130-137 ◽

Cited By ~ 16

Author(s):

Anna Figueiredo ◽

Shannon Zelina ◽

Nicolas Sluis-Cremer ◽

Gilda Tachedjian

Keyword(s):

Reverse Transcriptase ◽

Binding Pocket ◽

Transcriptase Inhibitor ◽

Inhibitor Binding ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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Conformational Changes in HIV-1 Reverse Transcriptase Induced by Nonnucleoside Reverse Transcriptase Inhibitor Binding

Current HIV Research ◽

10.2174/1570162043351093 ◽

2004 ◽

Vol 2 (4) ◽

pp. 323-332 ◽

Cited By ~ 87

Author(s):

Nicolas Sluis-Cremer ◽

N. Temiz ◽

Ivet Bahar

Keyword(s):

Reverse Transcriptase ◽

Conformational Changes ◽

Transcriptase Inhibitor ◽

Inhibitor Binding ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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Recent progress in HIV-1 inhibitors targeting the entrance channel of HIV-1 non-nucleoside reverse transcriptase inhibitor binding pocket

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2019.04.054 ◽

2019 ◽

Vol 174 ◽

pp. 277-291 ◽

Cited By ~ 4

Author(s):

Shuang-Xi Gu ◽

Ting Xiao ◽

Yuan-Yuan Zhu ◽

Gen-Yan Liu ◽

Fen-Er Chen

Keyword(s):

Reverse Transcriptase ◽

Nucleoside Reverse Transcriptase Inhibitor ◽

Recent Progress ◽

Binding Pocket ◽

Transcriptase Inhibitor ◽

Entrance Channel ◽

Inhibitor Binding ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2020.113051 ◽

2020 ◽

pp. 113051

Author(s):

Xiangyi Jiang ◽

Boshi Huang ◽

Fisayo A. Olotu ◽

Jing Li ◽

Dongwei Kang ◽

...

Keyword(s):

Reverse Transcriptase ◽

Nucleoside Reverse Transcriptase Inhibitor ◽

Binding Pocket ◽

Transcriptase Inhibitor ◽

Region I ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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HIV-1 drug resistance mutations in children after failure of first-line nonnucleoside reverse transcriptase inhibitor-based antiretroviral therapy

HIV Medicine ◽

10.1111/j.1468-1293.2010.00828.x ◽

2010 ◽

Vol 11 (9) ◽

pp. 565-572 ◽

Cited By ~ 19

Author(s):

T Puthanakit ◽

G Jourdain ◽

S Hongsiriwon ◽

P Suntarattiwong ◽

K Chokephaibulkit ◽

...

Keyword(s):

Drug Resistance ◽

Antiretroviral Therapy ◽

Reverse Transcriptase ◽

Transcriptase Inhibitor ◽

Resistance Mutations ◽

First Line ◽

Drug Resistance Mutations ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor

Science ◽

10.1126/science.1701568 ◽

1990 ◽

Vol 250 (4986) ◽

pp. 1411-1413 ◽

Cited By ~ 507

Author(s):

V. Merluzzi ◽

K. Hargrave ◽

M Labadia ◽

K Grozinger ◽

M Skoog ◽

...

Keyword(s):

Reverse Transcriptase ◽

Transcriptase Inhibitor ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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Three Nonnucleoside Reverse Transcriptase Inhibitor–Sparing Antiretroviral Regimens for Treatment-Naive Volunteers Infected With HIV-1

Annals of Internal Medicine ◽

10.7326/l15-5066-2 ◽

2015 ◽

Vol 162 (6) ◽

pp. 461

Author(s):

Giuseppe Lapadula ◽

Andrea Gori

Keyword(s):

Reverse Transcriptase ◽

Transcriptase Inhibitor ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Treatment Naïve ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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Selection of nonnucleoside reverse transcriptase inhibitor-associated mutations in HIV-1 subtype C: evidence of etravirine cross-resistance

AIDS ◽

10.1097/qad.0b013e328346269f ◽

2011 ◽

Vol 25 (8) ◽

pp. 1123-1126 ◽

Cited By ~ 13

Author(s):

Ujjwal Neogi ◽

Anita Shet ◽

Ranjani Shamsundar ◽

Maria L Ekstrand

Keyword(s):

Reverse Transcriptase ◽

Transcriptase Inhibitor ◽

Cross Resistance ◽

Subtype C ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1 ◽

Selection Of

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Early Archiving and Predominance of Nonnucleoside Reverse Transcriptase Inhibitor–Resistant HIV‐1 among Recently Infected Infants Born in the United States

The Journal of Infectious Diseases ◽

10.1086/513871 ◽

2007 ◽

Vol 195 (10) ◽

pp. 1402-1410 ◽

Cited By ~ 41

Author(s):

Deborah Persaud ◽

Paul Palumbo ◽

Carrie Ziemniak ◽

Jie Chen ◽

Stuart C. Ray ◽

...

Keyword(s):

United States ◽

Reverse Transcriptase ◽

The United States ◽

Transcriptase Inhibitor ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

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94 Combination therapy with AZT prevents selection of HIV-1 variants that are highly resistant to the nonnucleoside reverse transcriptase inhibitor L-697, 661

Antiviral Research ◽

10.1016/0166-3542(93)90472-u ◽

1993 ◽

Vol 20 ◽

pp. 94 ◽

Cited By ~ 1

Keyword(s):

Combination Therapy ◽

Reverse Transcriptase ◽

Transcriptase Inhibitor ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1 ◽

Selection Of

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In Vitro Cross-Resistance Profiles of Rilpivirine, Dapivirine, and MIV-150, Nonnucleoside Reverse Transcriptase Inhibitor Microbicides in Clinical Development for the Prevention of HIV-1 Infection

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00277-17 ◽

2017 ◽

Vol 61 (7) ◽

Cited By ~ 9

Author(s):

Nicholas S. Giacobbi ◽

Nicolas Sluis-Cremer

Keyword(s):

Reverse Transcriptase ◽

Genital Tract ◽

Transcriptase Inhibitor ◽

Cross Resistance ◽

Nonnucleoside Reverse Transcriptase Inhibitor ◽

Immunodeficiency Virus ◽

Reverse Transcriptase Inhibitor ◽

Hiv 1

ABSTRACT Rilpivirine (RPV), dapivirine (DPV), and MIV-150 are in development as microbicides. It is not known whether they will block infection of circulating nonnucleoside reverse transcriptase inhibitor (NNRTI)-resistant human immunodeficiency virus type 1 (HIV-1) variants. Here, we demonstrate that the activity of DPV and MIV-150 is compromised by many resistant viruses containing single or double substitutions. High DPV genital tract concentrations from DPV ring use may block replication of resistant viruses. However, MIV-150 genital tract concentrations may be insufficient to inhibit many resistant viruses, including those harboring K103N or Y181C.

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