|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
2
|
|
pubmed:dateCreated |
2010-2-3
|
|
pubmed:abstractText |
2,3,5-Trisubstituted pyridines have been designed as potent AKT inhibitors that are selective against ROCK1 based on the comparison between AKT and ROCK1 structures. Substitution at the 2-position of the core pyridine is the key element to provide selectivity against ROCK1. An X-ray co-crystal structure of 9p in PKA supports the proposed rationale of ROCK1 selectivity.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jan
|
|
pubmed:issn |
1464-3405
|
|
pubmed:author |
pubmed-author:ChoudhryAnthony EAE,
pubmed-author:ConchaNestor ONO,
pubmed-author:ElkinsPatricia APA,
pubmed-author:HeerdingDirk ADA,
pubmed-author:KnickVictoria BVB,
pubmed-author:LaiZhihongZ,
pubmed-author:LinHongH,
pubmed-author:LuengoJuan IJI,
pubmed-author:MinthornElisabeth AEA,
pubmed-author:NidarmarthySirishkumarS,
pubmed-author:RhodesNelsonN,
pubmed-author:StrumSusan LSL,
pubmed-author:WangWenyongW,
pubmed-author:WoodEdgar RER,
pubmed-author:XieRenR,
pubmed-author:YamashitaDennis SDS,
pubmed-author:ZengJinJ
|
|
pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
|
|
pubmed:issnType |
Electronic
|
|
pubmed:day |
15
|
|
pubmed:volume |
20
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
673-8
|
|
pubmed:meshHeading |
|
|
pubmed:year |
2010
|
|
pubmed:articleTitle |
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.
|
|
pubmed:affiliation |
Oncology Medicinal Chemistry, GlaxoSmithKline, 1250 S. Collegeville, Rd., Collegeville, PA 19426, United States. hong.2.lin@gsk.com
|
|
pubmed:publicationType |
Journal Article
|
