| Literature DB >> 17948981 |
Richard D Carpenter1, Mirela Andrei, Edmond Y Lau, Felice C Lightstone, Ruiwu Liu, Kit S Lam, Mark J Kurth.
Abstract
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.Entities:
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Year: 2007 PMID： 17948981 DOI： 10.1021/jm070790o
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446