通过文库合成与筛选得到的新型α4β1整合素受体相互作用抑制剂
Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.
作者信息
Souers A J, Virgilio A A, Schürer S S, Ellman J A, Kogan T P, West H E, Ankener W, Vanderslice P
机构信息
Department of Chemistry, University of California, Berkeley 94720, USA.
出版信息
Bioorg Med Chem Lett. 1998 Sep 8;8(17):2297-302. doi: 10.1016/s0960-894x(98)00416-8.
A library of 2302 small molecule beta-turn mimetics was screened for inhibition of the alpha 4 beta 1 integrin-CS1 splice variant binding interaction. Preliminary data revealed several active ligands, and validation with purified material culminated in the identification of some of the first small molecule ligands (1, IC50 = 5 microM, and 2, IC50 = 8 microM) to be reported for this class of integrins.
对一个包含2302个小分子β-转角模拟物的文库进行筛选，以检测其对α4β1整合素-CS1剪接变体结合相互作用的抑制作用。初步数据显示了几种活性配体，使用纯化材料进行的验证最终确定了一些首批针对此类整合素报道的小分子配体（1，IC50 = 5 microM；2，IC50 = 8 microM）。
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