JNS 1-40 is a potent and selective cysteine-reactive covalent ligand of regulatory subunit PPP2R1A of the tumor-suppressor protein phosphatase 2A (PP2A) that activate PP2A in vitro and in vivo. JNS 1-40 targets C377 of PPP2R1A and inhibits breast cancer proliferation, and in vivo tumor growth.
cysteine-reactive covalent ligand of regulatory subunit PPP2R1A of the PP2A that activate PP2A
Cell chemical biology, 24(11), 1368-1376 (2017-09-19)
Many natural products that show therapeutic activities are often difficult to synthesize or isolate and have unknown targets, hindering their development as drugs. Identifying druggable hotspots targeted by covalently acting anti-cancer natural products can enable pharmacological interrogation of these sites
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