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Structure-based design of novel calcineurin (PP2B) inhibitors

…, RE Showalter, A Tempczyk, JE Villafranca

文献索引: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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被引用次数: 37

摘要

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.