HIV protease inhibitors: a review of molecular selectivity and toxicity
Zhengtong Lv,Yuan Chu,Yong Wang +2 more
TLDR
From the chemical structures of HIV protease inhibitors and their possible off-target molecules, hints for optimizing the molecular selectivity of the inhibitors are obtained to provide help in the design of new compounds with enhanced bioavailability and reduced side effects.Abstract:
Highly active antiretroviral therapy (HAART) is recognized as the most effective treatment method for AIDS, and protease inhibitors play a very important role in HAART. However, poor bioavailability and unbearable toxicity are their common disadvantages. Thus, the development of safer and potentially promising protease inhibitors is eagerly needed. In this review, we introduced the chemical characteristics and associated side effects of HIV protease inhibitors, as well as the possible off-target mechanisms causing the side effects. From the chemical structures of HIV protease inhibitors and their possible off-target molecules, we could obtain hints for optimizing the molecular selectivity of the inhibitors, to provide help in the design of new compounds with enhanced bioavailability and reduced side effects.read more
Citations
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Computational studies of drug repurposing and synergism of lopinavir, oseltamivir and ritonavir binding with SARS-CoV-2 protease against COVID-19.
TL;DR: The combination of three known drugs, lopinavir, oseltamivir and ritonavir has been proposed to control the virulence to a great extent in COVID-19 affected patients within 48 hours and showed a better binding energy than that of individual drugs.
Journal ArticleDOI
Recent Progress in the Development of HIV-1 Protease Inhibitors for the Treatment of HIV/AIDS.
TL;DR: Current drug design and medicinal chemistry efforts toward the development of next-generation protease inhibitors beyond the currently approved drugs are outlined.
Journal ArticleDOI
Efficacy, safety, and tolerability of dolutegravir-rilpivirine for the maintenance of virological suppression in adults with HIV-1: phase 3, randomised, non-inferiority SWORD-1 and SWORD-2 studies
Josep M. Llibre,Chien-Ching Hung,Cynthia Brinson,Francesco Castelli,Pierre-Marie Girard,Lesley P Kahl,Elizabeth A. Blair,Kostas Angelis,Brian Wynne,Kati Vandermeulen,Mark R. Underwood,Kim Smith,Martin Gartland,Michael Aboud +13 more
TL;DR: Dolutegravir-rilpivirine was non-inferior to CAR over 48 weeks in participants with HIV suppression and showed a safety profile consistent with its components, which supports the use of this two-drug regimen to maintain HIV suppression.
Journal ArticleDOI
Dolutegravir plus lamivudine versus dolutegravir plus tenofovir disoproxil fumarate and emtricitabine in antiretroviral-naive adults with HIV-1 infection (GEMINI-1 and GEMINI-2): week 48 results from two multicentre, double-blind, randomised, non-inferiority, phase 3 trials
TL;DR: The proportion of participants with HIV-1 RNA of less than 50 copies per mL at week 48 in the GEMINI-1 intention-to-treat-exposed population, using the Snapshot algorithm and a non-inferiority margin of -10%.
Journal ArticleDOI
Ageing and inflammation in patients with HIV infection
Milena Nasi,S. De Biasi,Lara Gibellini,Elena Bianchini,Simone Pecorini,V Bacca,Giovanni Guaraldi,Cristina Mussini,Marcello Pinti,Andrea Cossarizza +9 more
TL;DR: The role of inflammation and immune activation on the most important non‐AIDS‐related complications of chronic HIV infection, and the contribution of aging per se to this scenario are discussed.
References
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The Department of Health and Human Services.
TL;DR: This letter is in response to your two Citizen Petitions, requesting that the Food and Drug Administration (FDA or the Agency) require a cancer warning on cosmetic talc products.
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Jae Bum Kim,Pasha Sarraf,Margaret E. Wright,Kwok M. Yao,Elisabetta Mueller,Gemma Solanes,Bradford B. Lowell,Bruce M. Spiegelman +7 more
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Class-Sparing Regimens for Initial Treatment of HIV-1 Infection
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TL;DR: The virologic efficacy of the NRTI-sparing regimen was similar to that of the efavirenz regimen but was more likely to be associated with drug resistance.
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