Structure-based design of novel calcineurin (PP2B) inhibitors

…, RE Showalter, A Tempczyk, JE Villafranca

Index: Tatlock, John H.; Linton, M. Angelica; Hou, Xinjun J.; Kissinger, Charles R.; Pelletier, Laura A.; Showalter, Richard E.; Tempczyk, Anna; Villafranca, J. Ernest Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 8 p. 1007 - 1012

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Citation Number: 37

Abstract

The design, synthesis, and evaluation of small molecule, in vitro, inhibitors of human calcineurin is described. These ligands were derived from the known nonspecific phosphatase inhibitor endothall, and were modified to enhance binding and selectivity toward calcineurin using protein crystal structure information.