New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation

Mike Frohn; Han Xu; Xiaoming Zou; Catherine Chang; Michele McElvaine; Matthew H Plant; Min Wong; Philip Tagari; Randall Hungate; Roland W Bürli

doi:10.1016/j.bmcl.2007.09.043

New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6633-7. doi: 10.1016/j.bmcl.2007.09.043. Epub 2007 Sep 15.

Authors

Mike Frohn¹, Han Xu, Xiaoming Zou, Catherine Chang, Michele McElvaine, Matthew H Plant, Min Wong, Philip Tagari, Randall Hungate, Roland W Bürli

Affiliation

¹ Chemistry Research and Discovery, Amgen, Inc., One Amgen Center Drive, Thousand Oaks, CA 91320, USA. [email protected]

PMID: 17920884
DOI: 10.1016/j.bmcl.2007.09.043

Abstract

We report the development of the novel N-substituted benzimidazole 11 as a potent and selective human formyl peptide receptor-like 1 (hFPRL1) agonist. This compound and its less active enantiomer 12 were identified as useful tools for studying receptor function in vitro.

Publication types

Comparative Study

MeSH terms

Animals
Benzimidazoles / agonists
Benzimidazoles / chemical synthesis
Benzimidazoles / pharmacology
CHO Cells
Cell Migration Inhibition
Chemotaxis, Leukocyte / physiology
Cricetinae
Cricetulus
Humans
Inflammation Mediators / agonists
Inflammation Mediators / physiology*
Interleukin-6 / metabolism
Molecular Probes / analysis*
Molecular Probes / chemical synthesis*
Neutrophils / cytology
Neutrophils / drug effects
Neutrophils / metabolism
Receptors, Formyl Peptide / agonists
Receptors, Formyl Peptide / blood
Receptors, Formyl Peptide / physiology*
Receptors, Lipoxin / agonists
Receptors, Lipoxin / blood
Receptors, Lipoxin / physiology*

Substances

Benzimidazoles
FPR2 protein, human
Inflammation Mediators
Interleukin-6
Molecular Probes
Receptors, Formyl Peptide
Receptors, Lipoxin
benzimidazolone