cyclophilin subtype selective inhibitor / SCYNEXIS, Cypralis - LARVOL DELTA

Discovery and molecular basis of subtype-selective cyclophilin inhibitors. (PubMed, Nat Chem Biol) - "We further exploited S2 pocket interactions to develop the first cyclophilin E (CypE)-selective inhibitor, which forms a reversible covalent bond with a CypE S2 pocket lysine, and exhibits 30- to >4,000-fold selectivity over other cyclophilins. These findings reveal a strategy to generate isoform-selective small-molecule cyclophilin modulators, advancing their suitability as targets for biological investigation and therapeutic development."

Journal • PPIF