Selective PTP1B inhibition by A-1331852: Uncompetitive kinetics and computational evidence for C-terminal engagement.
Repurposing the clinical-stage Bcl-xL BH3 mimetic A-1331852 is identified as a potent PTP1B inhibitor demonstrating a selectivity margin of at least 50-fold over TCPTP, highlighting A-1331852 as a promising starting point for developing PTP1B inhibitors designed to exploit transient, substrate-induced binding states.
Nathaly Vasquez-Martínez, Alejandro Sosa-Peinado, Francisco Cortés-Benítez et al.
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