期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 12, 页码 1329-1333出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml5004074
关键词
SPHK1; PF-543; SPHK2; sphingosine; lipid; S1P
资金
- Structural Genomics Consortium [1097737]
- AbbVie
- Bayer
- Boehringer Ingelheim
- Canada Foundation for Innovation
- Canadian Institutes for Health Research
- Genome Canada
- GlaxoSmithKline
- Janssen
- Lilly Canada
- Novartis Research Foundation
- Ontario Ministry of Economic Development and Innovation
- Pfizer
- Takeda
- Wellcome Trust [092809/Z/10/Z]
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 angstrom 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.
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