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Volumn 51, Issue 18, 2008, Pages 5490-5493

Discovery of potent and selective small-molecule PAR-2 agonists

Author keywords

[No Author keywords available]

Indexed keywords

AC 264613; AC 55541; AC 98170; PROTEINASE ACTIVATED RECEPTOR 2; PROTEINASE ACTIVATED RECEPTOR 2 AGONIST; PROTEINASE ACTIVATED RECEPTOR 2 ANTAGONIST; UNCLASSIFIED DRUG;

EID: 52449126200     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm800754r     Document Type: Article
Times cited : (39)

References (19)
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  • 6
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    • A low potency small molecule PAR-2 antagonist was recently reported. Kelso, E. B.; Lockhart, J. C.; Hembrough, T.; Dunning, L.; Plevin, R.; Hollenberg, M. D.; Sommerhoff, C. P.; McLean, J. S.; Ferrell, W. R. Therapeutic promise of proteinase-activated receptor-2 antagonism in joint inflammation. J. Pharmacol. Exp. Ther. 2006, 316 (3), 1017-1024.
    • A low potency small molecule PAR-2 antagonist was recently reported. Kelso, E. B.; Lockhart, J. C.; Hembrough, T.; Dunning, L.; Plevin, R.; Hollenberg, M. D.; Sommerhoff, C. P.; McLean, J. S.; Ferrell, W. R. Therapeutic promise of proteinase-activated receptor-2 antagonism in joint inflammation. J. Pharmacol. Exp. Ther. 2006, 316 (3), 1017-1024.
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    • Unpublished results
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    • Molecular Operating Environment, Version 2004.03, Chemical Computing Group Inc, 1010 Sherbrooke Street West, Suite 910, Montreal, Canada H3A 2R7. A number of conformations were generated for each of these two molecules using a stochastic search algorithm and the MMFF94 force field. These conformations were then superimposed in 3D to ensure the maximum overlap of their van der Waals and pharmacophore features, like hydrogen bond donors and acceptors, aromatic rings, and lipophilic moieties. Each resulting alignment was assigned a score which quantified both feature overlap and internal strain energy
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    • Unpublished results.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.