Avoiding drug resistance in HIV reverse transcriptase

ME Cilento, KA Kirby, SG Sarafianos - Chemical reviews, 2021 - ACS Publications
HIV reverse transcriptase (RT) is an enzyme that plays a major role in the replication cycle of
HIV and has been a key target of anti-HIV drug development efforts. Because of the high …

[HTML][HTML] Integrase strand transfer inhibitors are effective anti-HIV drugs

SJ Smith, XZ Zhao, DO Passos, D Lyumkis, TR Burke Jr… - Viruses, 2021 - mdpi.com
Integrase strand transfer inhibitors (INSTIs) are currently recommended for the first line
treatment of human immunodeficiency virus type one (HIV-1) infection. The first-generation …

[HTML][HTML] Drug discovery of nucleos (t) ide antiviral agents: dedicated to Prof. Dr. Erik De Clercq on occasion of his 80th birthday

G Li, T Yue, P Zhang, W Gu, LJ Gao, L Tan - Molecules, 2021 - mdpi.com
Nucleoside and nucleotide analogues are essential antivirals in the treatment of infectious
diseases such as human immunodeficiency virus (HIV), hepatitis B virus (HBV), hepatitis C …

[HTML][HTML] An overview of human immunodeficiency virus-1 antiretroviral drugs: general principles and current status

YH Shin, CM Park, CH Yoon - Infection & Chemotherapy, 2021 - ncbi.nlm.nih.gov
Abstract Treatment with highly active antiretroviral therapy (HAART) can prolong a patient's
life-span by disrupting pivotal steps in the replication cycle of the human immunodeficiency …

[HTML][HTML] Genetic diversity of SARS-CoV-2 over a one-year period of the COVID-19 pandemic: a global perspective

M Miao, ED Clercq, G Li - Biomedicines, 2021 - mdpi.com
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) caused a global pandemic
of coronavirus disease in 2019 (COVID-19). Genome surveillance is a key method to track …

Druggability modification strategies of the diarylpyrimidine‐type non‐nucleoside reverse transcriptase inhibitors

L Ding, C Zhuang, F Chen - Medicinal Research Reviews, 2021 - Wiley Online Library
Drug discovery of human immunodeficiency virus (HIV) is a hot field in medicinal chemistry
community for many years. The diarylpyrimidines (DAPYs) are the second‐generation non …

Covalent inhibition of wild-type HIV-1 reverse transcriptase using a fluorosulfate warhead

JA Ippolito, H Niu, N Bertoletti, ZJ Carter… - ACS Medicinal …, 2021 - ACS Publications
Covalent inhibitors of wild-type HIV-1 reverse transcriptase (CRTIs) are reported. Three
compounds derived from catechol diether non-nucleoside inhibitors (NNRTIs) with addition …

Design, synthesis, and evaluation of “dual-site”-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase

D Feng, X Zuo, L Jing, CH Chen, FA Olotu, H Lin… - European Journal of …, 2021 - Elsevier
Inspired by our previous efforts to improve the drug-resistance profiles of HIV-1 non-
nucleoside reverse transcriptase inhibitors (NNRTIs), a novel series of “dual-site” binding …

[HTML][HTML] Epidemiology and transmitted HIV-1 drug resistance among treatment-naive individuals in Israel, 2010–2018

T Wagner, NS Zuckerman, T Halperin, D Chemtob… - Viruses, 2021 - mdpi.com
Despite the low prevalence of HIV-1 in Israel, continuous waves of immigration may have
impacted the local epidemic. We characterized all people diagnosed with HIV-1 in Israel in …

Cell culture selections reveal favourable drug resistance profiles for doravirine and islatravir

BG Brenner, M Oliveira, RI Ibanescu… - Journal of …, 2021 - academic.oup.com
Abstract Background The newer generation NNRTIs, including doravirine and rilpivirine,
were designed to show high potency and overcome K103N, Y181C and G190A resistance …