Journal article icon

Journal article

Crystal Structure of Sphingosine Kinase 1 with PF-543.

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.
Publication status:
Published

Actions


Access Document


Publisher copy:
10.1021/ml5004074

Authors


More by this author
Institution:
University of Oxford
Department:
Oxford, MSD, Clinical Medicine, Structural Genomics Consortium
Role:
Author
Publisher:
American Chemical Society
Journal:
ACS medicinal chemistry letters
Volume:
5
Issue:
12
Pages:
1329-1333
Publication date:
2014-12-05
DOI:
EISSN:
1948-5875
ISSN:
1948-5875
URN:
uuid:41340312-7b29-4265-9ddd-e2d1cb984583
Source identifiers:
499830
Local pid:
pubs:499830
Language:
English
Keywords:

Terms of use


Metrics


Views and Downloads






If you are the owner of this record, you can report an update to it here: Report update to this record

TO TOP