Basic Information
ID: ALA5046306
Journal: ACS Med Chem Lett
Title: Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Authors: Alcock LJ, Chang Y, Jarusiewicz JA, Actis M, Nithianantham S, Mayasundari A, Min J, Maxwell D, Hunt J, Smart B, Yang JJ, Nishiguchi G, Fischer M, Mullighan CG, Rankovic Z.
Abstract: Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ10542 displayed high selectivity over GSPT1 and other members of the JAK family and potency in patient-derived ALL cells containing both JAK2 fusions and CRLF2 rearrangements.
CiteXplore: 35300081
DOI: 10.1021/acsmedchemlett.1c00650
Patent ID: ┄
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