Search

Your search keyword '"Klon AE"' showing total 1 results
Start Over Author "Klon AE" Publisher elsevier science ltd

Refine your results

1 results on '"Klon AE"'

1. The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.

Author

Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, and Klon AE

Subjects
Drug Design, Humans, Models, Molecular, Phosphorylation, Structure-Activity Relationship, AMP-Activated Protein Kinases antagonists & inhibitors, Protein Kinase Inhibitors chemistry, Protein Kinase Inhibitors pharmacology
Abstract

We have designed and synthesized analogues of compound C, a non-specific inhibitor of 5'-AMP-activated protein kinase (AMPK), using a computational fragment-based drug design (FBDD) approach. Synthesizing only twenty-seven analogues yielded a compound that was equipotent to compound C in the inhibition of the human AMPK (hAMPK) α2 subunit in the heterotrimeric complex in vitro, exhibited significantly improved selectivity against a subset of relevant kinases, and demonstrated enhanced cellular inhibition of AMPK., (Copyright © 2010 Elsevier Ltd. All rights reserved.)

Published
2010
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results