Crystal structure of sphingosine kinase 1 with PF-543

J Wang, S Knapp, NJ Pyne, S Pyne…

Index: Baek, Dong Jae; MacRitchie, Neil; Anthony, Nahoum G.; MacKay, Simon P.; Pyne, Susan; Pyne, Nigel J.; Bittman, Robert Journal of Medicinal Chemistry, 2013 , vol. 56, # 22 p. 9310 - 9327

Full Text: HTML

Citation Number: 11

Abstract

The most potent inhibitor of Sphingosine Kinase 1 (SPHK1) so far identified is PF-543. The crystal structure of SPHK1 in complex with inhibitor PF-543 to 1.8 Å resolution reveals the inhibitor bound in a bent conformation analogous to that expected of a bound sphingosine