AstraZeneca R&D Charnwood, Bioscience, Bakewell Road, Loughborough LE11 5RH, UK.
Bioorg Med Chem Lett. 2011 May 15;21(10):2991-7. doi: 10.1016/j.bmcl.2011.03.049. Epub 2011 Mar 21.
The identification of two novel series of formyl peptide receptor 1 (FPR1) antagonists are reported, represented by methionine benzimidazole 6 and diamide 7. Both series specifically inhibited the binding of labelled fMLF to hrFPR1 and selectively antagonized FPR1 function in human neutrophils, making them useful in vitro validation tools for the target.
报道了两种新型的甲酰肽受体 1（FPR1）拮抗剂，分别由苯并咪唑 6 和二酰胺 7 代表。这两个系列都特异性地抑制了标记的 fMLF 与 hrFPR1 的结合，并选择性地拮抗了人中性粒细胞中的 FPR1 功能，使它们成为该靶标的有用的体外验证工具。
