Analysis Biomolecular Interactions of DS003 to gp120 by BLI (CAT#: STEM-MB-0115-CJ)

Introduction

A major target for potential HIV pre-exposure prophylaxis (PrEP) intervention is the binding of viral gp120 to CD4+. Inhibiting this step can be achieved by blocking the CD4+-binding site within gp120. Small proteins mimicking CD4+ have shown high potency against HIV-1 in-vitro and in animal studies. An alternative to inhibit effective gp120-CD4+ binding is for a drug to bind to gp120 and block the conformational change in gp120 induced by CD4+. DS003 (BMS-599793) is another related compound with a similar mechanism of action, developed for topical PrEP as a microbicide candidate by the International Partnership for Microbicides (IPM). DS003 has been advanced to a Phase I clinical trial, IPM042, as a vaginal tablet showing a good safety profile and achieving concentrations in the female genital tract that were capable of inhibiting ex-vivo HIV-1 infection of cervical biopsies.