Tag: STAT5

Stafib-1 is the First Selective Inhibitor of the STAT5b SH2 Domain

The transcription factor STAT5A/B controls leukemic cell survival and disease progression. Especially, STAT5B as major STAT5 isoform driving BCR/ABL+ leukemia. Besides, STAT5B enables transformation by suppressing IFN-α/γ, thereby facilitating leukemogenesis. STAT5b might serve as an anticancer target in ductal pancreatic adenocarcinoma. Stafib-1 acts as the first selective inhibitor of...

SIAIS178 is a Potent and Selective PROTAC-Based BCR-ABL Degrader

Proteolysis targeting chimeras (PROTACs) work by inducing selective intracellular proteolysis rather than acting as a conventional enzyme inhibitor. Besides, PROTACs consists of two covalently linked protein-binding molecules. One can engage an E3 ubiquitin ligase, and another binds to a target protein meant for degradation. Moreover, PROTACs need only to...