Crystal structure of sphingosine kinase 1 with PF-543

Jing Wang, Stefan Knapp, Nigel Pyne, Susan Pyne, Jonathan Elkins

Research output: Contribution to journalArticle

50 Citations (Scopus)
90 Downloads (Pure)

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 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 languageEnglish
Pages (from-to)1329-1333
Number of pages5
JournalMedicinal Chemistry Letters
Volume5
Issue number12
Early online date27 Oct 2014
DOIs
Publication statusPublished - 27 Dec 2014

Keywords

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

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