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Covalent Allosteric Inactivation of Protein Tyrosine Phosphatase 1B (PTP1B) by an Inhibitor-Electrophile Conjugate.

Biochemistry - 11 Apr 2017

Punthasee Puminan, Laciak Adrian R, Cummings Andrea H, Ruddraraju Kasi Viswanatharaju, Lewis Sarah M, Hillebrand Roman, Singh Harkewal, Tanner John J, Gates Kent S

Abstract excerpt

Protein tyrosine phosphatase 1B (PTP1B) is a validated drug target, but it has proven difficult to develop medicinally useful, reversible inhibitors of this enzyme. Here we explored covalent strategies for the inactivation of PTP1B using a conjugate composed of an active site-directed 5-aryl-1,2,5-thiadiazolidin-3-one 1,1-dioxide inhibitor connected via a short linker to an electrophilic α-bromoacetamide moiety....

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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PMID: 28345882
DOI: 10.1021/acs.biochem.7b00151

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