نتایج جستجو برای: integrase inhibitors

تعداد نتایج: 191203  

Journal: :The Journal of antimicrobial chemotherapy 2014
Thibault Mesplède Nathan Osman Melissa Wares Peter K Quashie Said Hassounah Kaitlin Anstett Yingshan Han Diane N Singhroy Mark A Wainberg

BACKGROUND The results of several clinical trials suggest that the integrase inhibitor dolutegravir may be less prone than other drugs to the emergence of HIV drug resistance mutations in treatment-naive patients. We have shown that the R263K mutation commonly emerged during tissue culture selection studies with dolutegravir and conferred low levels of resistance to this drug while simultaneous...

2016
Pawel Bonczkowski Marie-Angélique De Scheerder Eva Malatinkova Alexandra Borch Zora Melkova Renate Koenig Ward De Spiegelaere Linos Vandekerckhove

To understand the persistence of latently HIV-1 infected cells in virally suppressed infected patients, a number of in vitro models of HIV latency have been developed. In an attempt to mimic the in vivo situation as closely as possible, several models use primary cells and replication-competent viruses in combination with antiretroviral compounds to prevent ongoing replication. Latency is subse...

Journal: :Current Opinion in Hiv and Aids 2021

Purpose of review Increased total body fat with truncal redistribution is common in antiretroviral therapy (ART)-controlled persons living HIV(PLWH), leading to insulin resistance, prediabetes/diabetes and dyslipidaemia. We address these topics here. Recent findings Most antiretrovirals are associated gain trunk fat, including visceral adipose tissue (VAT). Protease-inhibitors could inhibit whi...

2012
Xiaoju Ni Safwat Abdel-Azeim Elodie Laine Rohit Arora Osamuede Osemwota Anne-Geneviève Marcelin Vincent Calvez Jean-François Mouscadet Luba Tchertanov

Most antiretroviral medical treatments were developed and tested principally on HIV-1 B nonrecombinant strain, which represents less than 10% of the worldwide HIV-1-infected population. HIV-1 circulating recombinant form CRF02_AG is prevalent in West Africa and is becoming more frequent in other countries. Previous studies suggested that the HIV-1 polymorphisms might be associated to variable s...

Journal: :AIDS research and human retroviruses 2014
Pamela Tau Alessandro Mancon Davide Mileto Silvia Di Nardo Stuppino Giulia Bottani Maria Rita Gismondo Massimo Galli Valeria Micheli Stefano Rusconi

HIV drug resistance still represents a crucial problem in antiretroviral therapy. We report a case of a naive patient, harboring a CRF11-cpx virus, which showed drug resistance mutations in the reverse transcriptase. A drug resistance genotyping test was performed for the pol (protease, reverse transcriptase, and integrase) and V3 regions. The initial clinical parameter results showed a 4 log l...

2014
Manuel Battegay

Current international and national treatment guidelines such as EACS, BHIVA, DHHS or IAS update regularly recommendations on the choice of initial combination antiretroviral treatment (cART) regimens. Preferred cART regimens include a backbone with two nucleoside (nucleotide) reverse transcriptase inhibitors combined either with one non-nucleoside reverse transcriptase inhibitor or one ritonavi...

Journal: :Journal of medicinal chemistry 2007
Zhengqiang Wang Eric M Bennett Daniel J Wilson Christine Salomon Robert Vince

Bifunctional inhibitors were designed and synthesized based on 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)a1 non-nucleoside reverse transcriptase (RT) inhibitors and diketoacid (DKA) integrase (IN) inhibitors. Biochemical studies revealed activity against RT and IN at low nanomolar and low micromolar concentrations, respectively. Exceptionally low IC50 values from a cell-based assa...

Journal: :Proceedings of the National Academy of Sciences 2001

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