VAV1 molecular glue degrader

VAV1 molecular glue degraders represent an emerging class of targeted protein degraders (TPDs) designed to selectively target and eliminate VAV1 (Vav guanine nucleotide exchange factor 1). VAV1 is a critical intracellular signaling protein restricted to hematological and immune cells, playing a central role downstream of both T-cell and B-cell receptors to regulate lymphocyte activation, proliferation, and cytokine production. Because VAV1 lacks a classic small-molecule binding pocket, it has historically been considered undruggable. Molecular glue degraders overcome this by inducing a ternary complex between VAV1 and the E3 ubiquitin ligase cereblon (CRBN), leading to VAV1 ubiquitination and subsequent proteasomal degradation. This therapeutic platform is being actively developed for a wide range of systemic and neurological autoimmune and inflammatory disorders. Key clinical-stage candidates in this class include Monte Rosa Therapeutics and Novartis's MRT-6160 (DDY391), InnoCare's ICP-538, and Haisco's HSK56630.

Other names

VAV1 MGDVAV-1 MGDVAV 1 MGDVAV1 MGDsVAV-1 MGDsVAV 1 MGDsVAV1 degraderVAV-1 degraderVAV 1 degraderVAV1 degradersVAV-1 degradersVAV 1 degradersVAV1 molecular glue degradersVAV-1 molecular glue degradersVAV 1 molecular glue degraders