نتایج جستجو برای: integrase inhibitors

تعداد نتایج: 191203  

2016
Lenard S. Vranckx Jonas Demeulemeester Suha Saleh Annegret Boll Gerlinde Vansant Rik Schrijvers Caroline Weydert Emilie Battivelli Eric Verdin Anna Cereseto Frauke Christ Rik Gijsbers Zeger Debyser

Persistence of latent, replication-competent Human Immunodeficiency Virus type 1 (HIV-1) provirus is the main impediment towards a cure for HIV/AIDS (Acquired Immune Deficiency Syndrome). Therefore, different therapeutic strategies to eliminate the viral reservoirs are currently being explored. We here propose a novel strategy to reduce the replicating HIV reservoir during primary HIV infection...

2012
Rei Ohmori Tatsuaki Tsuruyama

Integration into the host genome is an essential step in the HIV-1 life cycle. However, the host genome sequence that is favored by HIV-1 during integration has never been documented. Here, we report that CD27, a T cell activation gene, includes a sequence that is a target for in vitro HIV-1 cDNA integration. This sequence has a high affinity for integrase, and the target nucleotides responsibl...

Journal: :Bioorganic & medicinal chemistry letters 2005
Mark W Embrey John S Wai Timothy W Funk Carl F Homnick Debbie S Perlow Steven D Young Joseph P Vacca Daria J Hazuda Peter J Felock Kara A Stillmock Marc V Witmer Gregory Moyer William A Schleif Lori J Gabryelski Lixia Jin I-Wu Chen Joan D Ellis Bradley K Wong Jiunn H Lin Yvonne M Leonard Nancy N Tsou Linghang Zhuang

Introduction of a 5,6-dihydrouracil functionality in the 5-position of N-(4-fluorobenzyl)-8-hydroxy-[1,6]naphthyridine-7-carboxamide 1 led to a series of highly active HIV-1 integrase inhibitors. These compounds displayed low nanomolar activity in inhibiting both the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 11 is a 150-fold more potent antiviral agent ...

2014
Karolin Meixenberger Kaveh Pouran Yousef Sybille Somogyi Stefan Fiedler Barbara Bartmeyer Max von Kleist Claudia Kücherer

INTRODUCTION The aim of our study was to analyze the occurrence and evolution of HIV-1 integrase polymorphisms during the HIV-1 epidemic in Germany prior to the introduction of the first integrase inhibitor raltegravir in 2007. MATERIALS AND METHODS Plasma samples from drug-naïve HIV-1 infected individuals newly diagnosed between 1986 and 2006 were used to determine PCR-based population seque...

Journal: :Proceedings of the National Academy of Sciences 1996

Journal: :Topics in HIV medicine : a publication of the International AIDS Society, USA 2009
Raphael J Landovitz

Data supporting the efficacy of HIV postexposure prophylaxis (PEP) come largely from a small number of older studies and case reports in health care workers, studies of transmission from infected mothers to their infants, and animal studies. These data also provide support for the current recommendations regarding duration of PEP and the window of time within which PEP should be started. Althou...

2012
Hao Wang Kellie A. Jurado Xiaolin Wu Ming-Chieh Shun Xiang Li Andrea L. Ferris Steven J. Smith Pratiq A. Patel James R. Fuchs Peter Cherepanov Mamuka Kvaratskhelia Stephen H. Hughes Alan Engelman

The binding of integrase (IN) to lens epithelium-derived growth factor (LEDGF)/p75 in large part determines the efficiency and specificity of HIV-1 integration. However, a significant residual preference for integration into active genes persists in Psip1 (the gene that encodes for LEDGF/p75) knockout (KO) cells. One other cellular protein, HRP2, harbors both the PWWP and IN-binding domains tha...

2011
R Satpathy S Ghosh

Elvitegravir is a new-generation drug which acts as an integrase inhibitor of the HIV virus. The potential inhibition has been tested from the clinical trial data. Here the work basically deals with the quantitative structure-activity relationship (QSAR) analysis by considering some of the physiochemical descriptors like molecular weight, logP, molar volume, and structural descriptors like Wine...

Journal: :Chemical biology & drug design 2012
Pawan Gupta Prabha Garg Nilanjan Roy

The objective of this study is to identify novel HIV-1 integrase (IN) inhibitors. Here, shape-based screening and QSAR have been successfully implemented to identify the novel inhibitors for HIV-1 IN, and in silico validation is performed by docking studies. The 2D QSAR model of benzodithiazine derivatives was built using genetic function approximation (GFA) method with good internal (cross-val...

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