PDE3A-targeted degrader

PDE3A-targeted degrader is an experimental therapeutic agent designed to selectively induce the degradation of Phosphodiesterase 3A (PDE3A). In triple-negative breast cancer (TNBC), PDE3A expression in cancer-associated fibroblasts (CAFs) is a key driver of immunotherapy resistance. The degrader works by disrupting a non-enzymatic signaling role of PDE3A, where it inhibits the negative regulator Cbl-b, leading to IGF-1R lipid raft translocation and STAT3 activation. This pathway promotes the secretion of CXCL12 and the recruitment of myeloid-derived suppressor cells (MDSCs), creating an immunosuppressive tumor microenvironment. By eliminating PDE3A, the degrader reverses this process, enhancing T cell infiltration and activity, and sensitizing tumors to immune checkpoint inhibitors.

Other names

PDE3A degraderPDE-3A degraderPDE 3A degrader