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- W4236056208 abstract "While stimulation of formyl peptide receptors (FPRs) on the surface of human neutrophils induces several immune responses, under conditions of continuous activation of the receptor by agonists such as formyl-Met-Leu-Phe-OH (fMLP), neutrophil-dependent tissue damage ensues. Thus, FPR antagonists could be anticipated as drugs for FPR-related disease. In this study, Boc-Phe-d-Leu-Phe-d-Leu-Phe-OH (Boc-FlFlF), one of several FPR subtype selective antagonists, was chosen and the positions at the Phe residues were optimized. We found that substitution with unnatural amino acids resulted in an improvement of two orders of magnitude. The most potent antagonist indicated FPR subtype selectivity at 1 μM. In addition to finding a potent antagonist, the structure–activity trends observed in this study should be valuable in designing a new type of FPR subtype selective antagonist." @default.
- W4236056208 created "2022-05-12" @default.
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- W4236056208 date "2004-08-01" @default.
- W4236056208 modified "2023-09-27" @default.
- W4236056208 title "PRIMO 12" @default.
- W4236056208 doi "https://doi.org/10.1016/j.marenvres.2004.03.007" @default.
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