Crystal Structure of Sphingosine Kinase 1 with PF-543 | Zendy

Jing Wang | Zendy; Stefan Knapp | Zendy; Nigel J. Pyne | Zendy; Susan Pyne | Zendy; Jonathan M. Elkins | Zendy

AI Assistant Blog Pricing

Home ZAIA Blog

Open Access

Crystal Structure of Sphingosine Kinase 1 with PF-543

Author(s) -

Jing Wang,

Stefan Knapp,

Nigel J. Pyne,

Susan Pyne,

Jonathan M. Elkins

Publication year - 2014

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml5004074

Subject(s) - sphingosine , sphingosine kinase 1 , sphingosine kinase , substrate (aquarium) , kinase , chemistry , biochemistry , biology , sphingosine 1 phosphate , receptor , ecology

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.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research