Source:http://linkedlifedata.com/resource/pubmed/id/17948981
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
23
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| pubmed:dateCreated |
2007-11-8
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| pubmed:abstractText |
The cell surface receptor alpha 4 beta 1 integrin, activated constitutively in lymphoma, can be targeted with the bisaryl urea peptidomimetic antagonist 1 (LLP2A). However, concerns on its preliminary pharmacokinetic (PK) profile provided an impetus to change the pharmacophore from a bisaryl urea to a 2-arylaminobenzimidazole moiety, resulting in improved solubility while maintaining picomolar potency [5 (KLCA4); IC50 = 305 pM]. With exceptional solubility, this finding has the potential for improving PK to help diagnose and treat lymphomas.
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Nov
|
| pubmed:issn |
0022-2623
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
15
|
| pubmed:volume |
50
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
5863-7
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| pubmed:meshHeading |
pubmed-meshheading:17948981-Benzimidazoles,
pubmed-meshheading:17948981-Cell Adhesion,
pubmed-meshheading:17948981-Cell Line, Tumor,
pubmed-meshheading:17948981-Humans,
pubmed-meshheading:17948981-Integrin alpha4beta1,
pubmed-meshheading:17948981-Solubility,
pubmed-meshheading:17948981-Structure-Activity Relationship
|
| pubmed:year |
2007
|
| pubmed:articleTitle |
Highly potent, water soluble benzimidazole antagonist for activated alpha 4 beta 1 integrin.
|
| pubmed:affiliation |
Department of Chemistry, University of California, Davis, Davis, CA 95616, USA.
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| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
|