title: Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.
abstract: We report the discovery of potent agonists for the human formyl-peptide-like 1 receptor (hFPRL1). These compounds did not act at a closely related receptor denoted human formyl peptide receptor (hFPR) up to 10 microM concentration. Recent studies have indicated that agonizing this receptor may promote resolution of inflammation. In an exploratory study, a novel hFPRL1 agonist showed efficacy in a mouse ear inflammation model following oral administration.
authors.affiliation: Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. rburli@amgen.com
authors.forename: Roland W
authors.initials: RW
authors.lastname: Bürli
authors.forename: Han
authors.initials: H
authors.lastname: Xu
authors.forename: Xiaoming
authors.initials: X
authors.lastname: Zou
authors.forename: Kristine
authors.initials: K
authors.lastname: Muller
authors.forename: Jennifer
authors.initials: J
authors.lastname: Golden
authors.forename: Mike
authors.initials: M
authors.lastname: Frohn
authors.forename: Matthew
authors.initials: M
authors.lastname: Adlam
authors.forename: Matthew H
authors.initials: MH
authors.lastname: Plant
authors.forename: Min
authors.initials: M
authors.lastname: Wong
authors.forename: Michele
authors.initials: M
authors.lastname: McElvain
authors.forename: Kelly
authors.initials: K
authors.lastname: Regal
authors.forename: Vellarkad N
authors.initials: VN
authors.lastname: Viswanadhan
authors.forename: Philip
authors.initials: P
authors.lastname: Tagari
authors.forename: Randall
authors.initials: R
authors.lastname: Hungate
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use*; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007249:Inflammation / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D044042:Receptors, Formyl Peptide / Q000819:agonists*; D044067:Receptors, Lipoxin / Q000819:agonists*
chemical_list: D000893:Anti-Inflammatory Agents; C105101:FPR2 protein, human; D044042:Receptors, Formyl Peptide; D044067:Receptors, Lipoxin