title: Discovery of small molecule human FPR1 receptor antagonists.
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.
authors.affiliation: AstraZeneca R&D Charnwood, Bioscience, Bakewell Road, Loughborough LE11 5RH, UK.
authors.forename: John
authors.initials: J
authors.lastname: Unitt
authors.forename: Malbinder
authors.initials: M
authors.lastname: Fagura
authors.forename: Tim
authors.initials: T
authors.lastname: Phillips
authors.forename: Sarah
authors.initials: S
authors.lastname: King
authors.forename: Matthew
authors.initials: M
authors.lastname: Perry
authors.forename: Andrew
authors.initials: A
authors.lastname: Morley
authors.forename: Cathy
authors.initials: C
authors.lastname: MacDonald
authors.forename: Richard
authors.initials: R
authors.lastname: Weaver
authors.forename: Jadeen
authors.initials: J
authors.lastname: Christie
authors.forename: Simon
authors.initials: S
authors.lastname: Barber
authors.forename: Rukhsana
authors.initials: R
authors.lastname: Mohammed
authors.forename: Melanie
authors.initials: M
authors.lastname: Paul
authors.forename: Andrew
authors.initials: A
authors.lastname: Cook
authors.forename: Andrew
authors.initials: A
authors.lastname: Baxter
mesh_terms: D055808:Drug Discovery; D006801:Humans; D015394:Molecular Structure; D044042:Receptors, Formyl Peptide / Q000037:antagonists & inhibitors* / Q000737:chemistry*
chemical_list: C469986:FPR1 protein, human; D044042:Receptors, Formyl Peptide