molecules of the month

“Compound 20”

long-acting RIPK2 degrader (SC admin.)

in vivo degradation of RIPK2 over 60 days

IAP binder linked to RIPK2 binder

Journal of Medicinal Chemistry

GlaxoSmithKline, Stevenage, UK

compound 20
1 min read

The GSK RIPK2 PROTAC, “compound 20”, demonstrates in vivo degradation of RIPK2 over 60 days after a single compound dose when administered SC in slow-release PLGA microparticles. This degrader was previously highlighted as a Molecule of the Month, voted by our readers as a final contender for Molecule of the Year in 2020 thanks to its remarkable in vivo PD. This article shares more details about the optimization campaign and identification of the molecule, as well as proof-of-concept on the use of the slow-release matrix, and is worth a read for all interested in targeted protein degradation.

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