Aurantiamide-related dipeptide derivatives are formyl peptide receptor 1 antagonists.

ABSTRACT: Formyl peptide receptor 1 (FPR1) is expressed on a variety of immune system cells and is a key regulator of the inflammatory environment. Therefore, the development of FPR1 antagonists may represent a novel approach for modulating innate immunity and treating inflammatory diseases. Starting from a dipeptide scaffold that is structurally related to the natural product aurantiamide, we investigated the structure-activity relationships of the dipeptide (2R,2'S)-6, which was reported as an FPR1 antagonist. We found that the absolute configuration 2R,2'S was preferred to obtain potent and selective FPR1 antagonists. The structural modifications performed on the terminal fragments of the molecule suggest that the size of the substituents can greatly influence the interaction with FPR1. These com

SUBMITTER: Mastromarino M 

PROVIDER: S-EPMC7069519 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature