molecules of the year


long-acting HIV capsid PPI-based inhibitor

in Ph. II/III for resistant HIV (SC once/6 mo.)

from HTS for binders, SBDD + opt. for funct.

Nature, Aug. 27, 2020 issue

Gilead Sciences, Foster City, CA

1 min read

August’s molecule, the Gilead HIV capsid inhibitor GS-6207, is an HIV-1 inhibitor that took over 12 years to develop due to its challenging mode of action. It acts on the capsid protein monomer (p24), which normally self-assembles in the HIV virion to form the capsid core that is essential for virus infectivity. GS-6207 targets a protein-protein interaction between the small (24 kDa) p24 monomers, binding in a glue-like fashion to two separate monomers, and is able to overcome the high concentration of p24 in a virion (~4 mM!) to inhibit HIV activity with sub-nanomolar potency in cells (20-500 pM). Since the HIV capsid protein is highly conserved among HIV-1 variants, GS-6207 shows high synergy and no cross-resistance with approved anti-HIV…

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