Open AccessThe entry inhibitor DS003 (BMS-599793): a BMS-806 analogue, provides superior activity as a pre-exposure prophylaxis candidate
Author(s) -
Carolina Herrera,
Sarah Harman,
Yoann Aldon,
P. S. Z. Rogers,
Naomi Armanasco,
Paul Ziprin,
Daniel J. Stieh,
Jeremy Nuttall,
Robin J. Shattock
Publication year - 2021
Publication title -
aids
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.195
H-Index - 216
eISSN - 1473-5571
pISSN - 0269-9370
DOI - 10.1097/qad.0000000000002974
Subject(s) - in vivo , flow cytometry , in vitro , pharmacology , ex vivo , mechanism of action , entry inhibitor , chemistry , viral entry , epitope , binding site , antibody , medicine , biology , immunology , viral replication , virus , biochemistry , microbiology and biotechnology
Small molecule inhibitors able to bind to gp120 and prevent CD4+-induced HIV-1 envelope conformational change provide an important class of inhibitors. Currently, only Fostemsavir is approved for HAART, which makes this class of inhibitors attractive candidates for prevention. We assessed the activity of DS003 (BMS-599793), an analogue of BMS-378806, in different mucosal tissues and elucidated its mechanism of action.