ChemBioChem

Dynamic Substrate Enhancement for the Identification of Specific, Second??Site??Binding Fragments Targeting a Set of Protein Tyrosine Phosphatases

MF Schmidt, MR Groves, J Rademann

Index: Schmidt, Marco F.; Groves, Matthew R.; Rademann, Joerg ChemBioChem, 2011 , vol. 12, # 17 p. 2640 - 2646

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Citation Number: 16

Abstract

Abstract Protein tyrosine phosphatases (PTPs) are key regulators in living systems and thus are attractive drug targets. The development of potent, selective PTP inhibitors has been a difficult challenge mainly due to the high homology of the phosphotyrosine substrate pockets. Here, a strategy of dynamic substrate enhancement is described targeting the secondary binding sites of PTPs. By screening four different PTPs from bacterial (MptpA) ...