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@article{Harman:2012,
author = {Harman, SJ and Herrera, C and Armanasco, N and Nuttall, J and Shattock, RJ},
journal = {Antimicrobial Agents and Chemotherapy},
title = {Pre-clinical evaluation of the HIV-1 fusion inhibitor L'644 as a potential candidate microbicide.},
year = {2012}
}
TY - JOUR
AB - Topical blockade of the gp41 fusogenic protein of HIV-1 is one possible strategy by which microbicides could prevent HIV transmission, working early against infection, by inhibiting viral entry into host cells. In this study we examined the potential of gp41 fusion inhibitors (FIs) as candidate anti-HIV microbicides. Preclinical evaluation of four FIs, C34, T20, T1249 and L'644, was performed using cellular and ex vivo genital and colorectal tissue explant models. Increased and sustained activity was detected for L'644, a cholesterol derivatized version of C34 relative to the other FIs. The higher potency of L'644 was further increased with sustained exposure of cells or tissue to the compound. The activity of L'644 was not affected by biological fluids and the compound was still active when tissue explants where treated after viral exposure. L'644 was also more active than other FIs against a viral escape mutant resistant to reverse transcriptase inhibitors (RTIs), demonstrating the potential of L'644 to be included as part of a multi-active ARV-combination based microbicide. These data support further development of L'644 for microbicide application.
AU - Harman,SJ
AU - Herrera,C
AU - Armanasco,N
AU - Nuttall,J
AU - Shattock,RJ
PY - 2012///
TI - Pre-clinical evaluation of the HIV-1 fusion inhibitor L'644 as a potential candidate microbicide.
T2 - Antimicrobial Agents and Chemotherapy
ER -