| pubmed-article:20800479 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C0332307 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C0205147 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C0001480 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C0031727 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C1167622 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C2587213 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C1707719 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C1706053 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C0457406 | lld:lifeskim |
| pubmed-article:20800479 | lifeskim:mentions | umls-concept:C1546856 | lld:lifeskim |
| pubmed-article:20800479 | pubmed:issue | 19 | lld:pubmed |
| pubmed-article:20800479 | pubmed:dateCreated | 2010-9-13 | lld:pubmed |
| pubmed-article:20800479 | pubmed:abstractText | Switch control pocket inhibitors of p38-alpha kinase are described. Durable type II inhibitors were designed which bind to arginines (Arg67 or Arg70) that function as key residues for mediating phospho-threonine 180 dependant conformational fluxing of p38-alpha from an inactive type II state to an active type I state. Binding to Arg70 in particular led to potent inhibitors, exemplified by DP-802, which also exhibited high kinase selectivity. Binding to Arg70 obviated the requirement for binding into the ATP Hinge region. X-ray crystallography revealed that DP-802 and analogs induce an enhanced type II conformation upon binding to either the unphosphorylated or the doubly phosphorylated form of p38-alpha kinase. | lld:pubmed |
| pubmed-article:20800479 | pubmed:language | eng | lld:pubmed |
| pubmed-article:20800479 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20800479 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:20800479 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20800479 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20800479 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20800479 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20800479 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:20800479 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:20800479 | pubmed:month | Oct | lld:pubmed |
| pubmed-article:20800479 | pubmed:issn | 1464-3405 | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:ClarkRobinR | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:StewartLanceL | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:ClareMichaelM | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:FlynnDaniel... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:VogetiLakshmi... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:AbendrothJanJ | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:AhnYu MiYM | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:SmithBryan... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:LuWei-PingWP | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:KaufmanMichae... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:EnsingerCarol... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:PattWilliam... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:MillerDavid... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:PetilloPeter... | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:WiseScott CSC | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:KimHidongH | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:HoodMolly MMM | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:LordJohn WJW | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:ChunLawrenceL | lld:pubmed |
| pubmed-article:20800479 | pubmed:author | pubmed-author:FeeseMichaelM | lld:pubmed |
| pubmed-article:20800479 | pubmed:copyrightInfo | Copyright © 2010 Elsevier Ltd. All rights reserved. | lld:pubmed |
| pubmed-article:20800479 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:20800479 | pubmed:day | 1 | lld:pubmed |
| pubmed-article:20800479 | pubmed:volume | 20 | lld:pubmed |
| pubmed-article:20800479 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:20800479 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:20800479 | pubmed:pagination | 5793-8 | lld:pubmed |
| pubmed-article:20800479 | pubmed:meshHeading | pubmed-meshheading:20800479... | lld:pubmed |
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| pubmed-article:20800479 | pubmed:meshHeading | pubmed-meshheading:20800479... | lld:pubmed |
| pubmed-article:20800479 | pubmed:year | 2010 | lld:pubmed |
| pubmed-article:20800479 | pubmed:articleTitle | Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region. | lld:pubmed |
| pubmed-article:20800479 | pubmed:affiliation | Deciphera Pharmaceuticals LLC, 643 Massachusetts St, Lawrence, KS 66044, USA. | lld:pubmed |
| pubmed-article:20800479 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:20800479 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:20800479 | lld:chembl |
