Literature DB >> 14693562

In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides.

Yven Van Herrewege1, Jo Michiels, Jens Van Roey, Katrien Fransen, Luc Kestens, Jan Balzarini, Paul Lewi, Guido Vanham, Paul Janssen.   

Abstract

The nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 (Dapivirine) effectively prevented human immunodeficiency virus (HIV) infection in cocultures of monocyte-derived dendritic cells and T cells, representing primary targets in sexual transmission. Both drugs had a favorable therapeutic index. A 24-h treatment with 1,000 nM UC-781 or 100 nM TMC120-R147681 prevented cell-free HIV infection, whereas 10-fold-higher concentrations blocked cell-associated HIV.

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Year:  2004        PMID： 14693562      PMCID： PMC310190          DOI： 10.1128/AAC.48.1.337-339.2004

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  22 in total

1.  PCR-Based assay to quantify human immunodeficiency virus type 1 DNA in peripheral blood mononuclear cells.

Authors:  C Christopherson; Y Kidane; B Conway; J Krowka; H Sheppard; S Kwok
Journal:  J Clin Microbiol       Date:  2000-02       Impact factor: 5.948

2.  Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T).

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Journal:  J Biol Chem       Date:  1992-06-15       Impact factor: 5.157

Review 3.  Considerations and development of topical microbicides to inhibit the sexual transmission of HIV.

Authors:  Jim A Turpin
Journal:  Expert Opin Investig Drugs       Date:  2002-08       Impact factor: 6.206

4.  HIV prevention: the need for methods women can use.

Authors:  Z A Stein
Journal:  Am J Public Health       Date:  1990-04       Impact factor: 9.308

Review 5.  Challenges for the development of female-controlled vaginal microbicides.

Authors:  C J Elias; L L Heise
Journal:  AIDS       Date:  1994-01       Impact factor: 4.177

6.  Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.

Authors:  D W Ludovici; B L De Corte; M J Kukla; H Ye; C Y Ho; M A Lichtenstein; R W Kavash; K Andries; M P de Béthune; H Azijn; R Pauwels; P J Lewi; J Heeres; L M Koymans; M R de Jonge; K J Van Aken; F F Daeyaert; K Das; E Arnold; P A Janssen
Journal:  Bioorg Med Chem Lett       Date:  2001-09-03       Impact factor: 2.823

7.  Attenuated infectivity of HIV type 1 from epithelial cells pretreated with a tight-binding nonnucleoside reverse transcriptase inhibitor.

Authors:  Gadi Borkow; Horacio Salomon; Mark A Wainberg; Michael A Parniak
Journal:  AIDS Res Hum Retroviruses       Date:  2002-07-01       Impact factor: 2.205

8.  Inhibition of vaginal transmission of HIV-1 in hu-SCID mice by the non-nucleoside reverse transcriptase inhibitor TMC120 in a gel formulation.

Authors:  Simonetta Di Fabio; Jens Van Roey; Giacomo Giannini; Guy van den Mooter; Massimo Spada; Andrea Binelli; Maria F Pirillo; Elena Germinario; Filippo Belardelli; Marie-Pierre de Bethune; Stefano Vella
Journal:  AIDS       Date:  2003-07-25       Impact factor: 4.177

9.  Mechanisms of HIV/SIV mucosal transmission.

Authors:  G Milman; O Sharma
Journal:  AIDS Res Hum Retroviruses       Date:  1994-10       Impact factor: 2.205

10.  Activity of reverse transcriptase inhibitors in monocyte-derived dendritic cells: a possible in vitro model for postexposure prophylaxis of sexual HIV transmission.

Authors:  Yven Van Herrewege; Lieve Penne; Chris Vereecken; Katrien Fransen; Guido van der Groen; Luc Kestens; Jan Balzarini; Guido Vanham
Journal:  AIDS Res Hum Retroviruses       Date:  2002-10-10       Impact factor: 2.205
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  43 in total

1.  Polymeric nanoparticles affect the intracellular delivery, antiretroviral activity and cytotoxicity of the microbicide drug candidate dapivirine.

Authors:  José das Neves; Johan Michiels; Kevin K Ariën; Guido Vanham; Mansoor Amiji; Maria Fernanda Bahia; Bruno Sarmento
Journal:  Pharm Res       Date:  2011-11-10       Impact factor: 4.200

Review 2.  Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.

Authors:  Fraser F Fleming; Lihua Yao; P C Ravikumar; Lee Funk; Brian C Shook
Journal:  J Med Chem       Date:  2010-08-30       Impact factor: 7.446

3.  Search for non-nucleoside inhibitors of HIV-1 reverse transcriptase using chemical similarity, molecular docking, and MM-GB/SA scoring.

Authors:  Gabriela Barreiro; Cristiano R W Guimarães; Ivan Tubert-Brohman; Theresa M Lyons; Julian Tirado-Rives; William L Jorgensen
Journal:  J Chem Inf Model       Date:  2007-10-20       Impact factor: 4.956

Review 4.  Vaginal drug delivery systems for HIV prevention.

Authors:  Lisa Cencia Rohan; Alexandra B Sassi
Journal:  AAPS J       Date:  2009-02-05       Impact factor: 4.009

5.  Human immunodeficiency virus type 1 resistance or cross-resistance to nonnucleoside reverse transcriptase inhibitors currently under development as microbicides.

Authors:  Philippe Selhorst; Ana C Vazquez; Katty Terrazas-Aranda; Johan Michiels; Katleen Vereecken; Leo Heyndrickx; Jan Weber; Miguel E Quiñones-Mateu; Kevin K Ariën; Guido Vanham
Journal:  Antimicrob Agents Chemother       Date:  2011-01-31       Impact factor: 5.191

6.  Preclinical evaluation of UC781 microbicide vaginal drug delivery.

Authors:  Meredith R Clark; Timothy J McCormick; Gustavo F Doncel; David R Friend
Journal:  Drug Deliv Transl Res       Date:  2011-04       Impact factor: 4.617

7.  The nonnucleoside reverse transcriptase inhibitor UC-781 inhibits human immunodeficiency virus type 1 infection of human cervical tissue and dissemination by migratory cells.

Authors:  Patricia Fletcher; Yana Kiselyeva; Greg Wallace; Joseph Romano; George Griffin; Leonid Margolis; Robin Shattock
Journal:  J Virol       Date:  2005-09       Impact factor: 5.103

Review 8.  Vaginal microbicides and the prevention of HIV transmission.

Authors:  Blayne Cutler; Jessica Justman
Journal:  Lancet Infect Dis       Date:  2008-11       Impact factor: 25.071

9.  A series of diaryltriazines and diarylpyrimidines are highly potent nonnucleoside reverse transcriptase inhibitors with possible applications as microbicides.

Authors:  Yven Van Herrewege; Guido Vanham; Jo Michiels; Katrien Fransen; Luc Kestens; Koen Andries; Paul Janssen; Paul Lewi
Journal:  Antimicrob Agents Chemother       Date:  2004-10       Impact factor: 5.191

10.  RT-SHIV, an infectious CCR5-tropic chimeric virus suitable for evaluating HIV reverse transcriptase inhibitors in macaque models.

Authors:  Yonghou Jiang; Baoping Tian; Mohammed Saifuddin; Michael B Agy; Peter Emau; J Scott Cairns; Che-Chung Tsai
Journal:  AIDS Res Ther       Date:  2009-11-05       Impact factor: 2.250
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