Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.
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.
Bürli
Roland W
RW
Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. rburli@amgen.com
Xu
Han
H
Zou
Xiaoming
X
Muller
Kristine
K
Golden
Jennifer
J
Frohn
Mike
M
Adlam
Matthew
M
Plant
Matthew H
MH
Wong
Min
M
McElvain
Michele
M
Regal
Kelly
K
Viswanadhan
Vellarkad N
VN
Tagari
Philip
P
Hungate
Randall
R
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*
D000893:Anti-Inflammatory Agents; C105101:FPR2 protein, human; D044042:Receptors, Formyl Peptide; D044067:Receptors, Lipoxin