Discovery of small molecule human FPR1 receptor antagonists

John Unitt; Malbinder Fagura; Tim Phillips; Sarah King; Matthew Perry; Andrew Morley; Cathy MacDonald; Richard Weaver; Jadeen Christie; Simon Barber; Rukhsana Mohammed; Melanie Paul; Andrew Cook; Andrew Baxter

doi:10.1016/j.bmcl.2011.03.049

Discovery of small molecule human FPR1 receptor antagonists

Bioorg Med Chem Lett. 2011 May 15;21(10):2991-7. doi: 10.1016/j.bmcl.2011.03.049. Epub 2011 Mar 21.

Authors

John Unitt¹, Malbinder Fagura, Tim Phillips, Sarah King, Matthew Perry, Andrew Morley, Cathy MacDonald, Richard Weaver, Jadeen Christie, Simon Barber, Rukhsana Mohammed, Melanie Paul, Andrew Cook, Andrew Baxter

Affiliation

¹ AstraZeneca R&D Charnwood, Bioscience, Bakewell Road, Loughborough LE11 5RH, UK.

PMID: 21486695
DOI: 10.1016/j.bmcl.2011.03.049

Abstract

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.

MeSH terms

Drug Discovery*
Humans
Molecular Structure
Receptors, Formyl Peptide / antagonists & inhibitors*
Receptors, Formyl Peptide / chemistry*

Substances

FPR1 protein, human
Receptors, Formyl Peptide