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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 substrate but with a rotated head group. The structural data presented will aid in the design of SPHK1 and SPHK2 inhibitors with improved properties.

Original publication

DOI

10.1021/ml5004074

Type

Journal article

Journal

ACS Med Chem Lett

Publication Date

11/12/2014

Volume

5

Pages

1329 - 1333

Keywords

PF-543, S1P, SPHK1, SPHK2, lipid, sphingosine