AI Article Synopsis
- - The alpha 4 beta 1 integrin receptor, which is constantly active in lymphoma, can be targeted using a special drug known as LLP2A.
- - Concerns about LLP2A's initial pharmacokinetic properties led researchers to modify its structure, changing it from a bisaryl urea to a 2-arylaminobenzimidazole compound.
- - This new compound offers better solubility while still being highly effective, suggesting it could enhance the diagnosis and treatment of lymphoma.
Article 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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jm070790o | DOI Listing |
Publication Analysis
Top Keywords
alpha beta
8
beta integrin
8
bisaryl urea
8
highly potent
4
potent water
4
water soluble
4
soluble benzimidazole
4
benzimidazole antagonist
4
antagonist activated
4
activated alpha
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!