Source:http://linkedlifedata.com/resource/pubmed/id/20870405
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
22
|
| pubmed:dateCreated |
2010-10-19
|
| pubmed:abstractText |
The Bcl-2 family of proteins plays a major role in the regulation of apoptosis, or programmed cell death. Overexpression of the anti-apoptotic members of this family (Bcl-2, Bcl-x(L), and Mcl-1) can render cancer cells resistant to chemotherapeutic agents and therefore these proteins are important targets for the development of new anti-cancer agents. Here we describe the discovery of a potent, highly selective, Bcl-2 inhibitor using SAR by NMR and structure-based drug design which could serve as a starting point for the development of a Bcl-2 selective anti-cancer agent. Such an agent would potentially overcome the Bcl-x(L) mediated thrombocytopenia observed with ABT-263.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Nov
|
| pubmed:issn |
1464-3405
|
| pubmed:author |
pubmed-author:DingHongH,
pubmed-author:DorwinSarahS,
pubmed-author:ElmoreSteven WSW,
pubmed-author:FesikStephen WSW,
pubmed-author:GramlingEmilyE,
pubmed-author:HajdukPhilip JPJ,
pubmed-author:HuthJeffrey RJR,
pubmed-author:LadrorUriU,
pubmed-author:MackJameyJ,
pubmed-author:MendozaRenaldoR,
pubmed-author:NimmerPaulP,
pubmed-author:OostThorstenT,
pubmed-author:ParkCheol-MinCM,
pubmed-author:PetrosAndrew MAM,
pubmed-author:RosenbergSaul HSH,
pubmed-author:SunChaohongC,
pubmed-author:WalterKarlK,
pubmed-author:WangXiluX,
pubmed-author:ZhangHaichaoH
|
| pubmed:copyrightInfo |
Copyright © 2010 Elsevier Ltd. All rights reserved.
|
| pubmed:issnType |
Electronic
|
| pubmed:day |
15
|
| pubmed:volume |
20
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
6587-91
|
| pubmed:meshHeading | |
| pubmed:year |
2010
|
| pubmed:articleTitle |
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
|
| pubmed:affiliation |
Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, United States.
|
| pubmed:publicationType |
Journal Article
|