title: Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
abstract: The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States. Electronic address: steven.m.sparks@gsk.com.
authors.forename: Steven M
authors.initials: SM
authors.lastname: Sparks
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Grace
authors.initials: G
authors.lastname: Chen
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Jon L
authors.initials: JL
authors.lastname: Collins
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Dana
authors.initials: D
authors.lastname: Danger
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Steven T
authors.initials: ST
authors.lastname: Dock
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Channa
authors.initials: C
authors.lastname: Jayawickreme
authors.affiliation: Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Stephen
authors.initials: S
authors.lastname: Jenkinson
authors.affiliation: Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Christopher
authors.initials: C
authors.lastname: Laudeman
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: M Anthony
authors.initials: MA
authors.lastname: Leesnitzer
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Xi
authors.initials: X
authors.lastname: Liang
authors.affiliation: Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Patrick
authors.initials: P
authors.lastname: Maloney
authors.affiliation: Metabolic Center for Excellence in Drug Discovery, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: David C
authors.initials: DC
authors.lastname: McCoy
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: David
authors.initials: D
authors.lastname: Moncol
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Vincent
authors.initials: V
authors.lastname: Rash
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Thomas
authors.initials: T
authors.lastname: Rimele
authors.affiliation: Platform Technology & Science, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Padmaja
authors.initials: P
authors.lastname: Vulimiri
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: James M
authors.initials: JM
authors.lastname: Way
authors.affiliation: Enteroendocrine Discovery Performance Unit, GlaxoSmithKline, PO Box 13398, Research Triangle Park, NC 27705, United States.
authors.forename: Sean
authors.initials: S
authors.lastname: Ross
mesh_terms: D000818:Animals; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D007328:Insulin / Q000819:agonists; D051379:Mice; D015394:Molecular Structure; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C519853:FFAR4 protein, human; D007328:Insulin; D043562:Receptors, G-Protein-Coupled; D013449:Sulfonamides
keywords: FFA4; Free fatty acid receptor 4; Free fatty acid receptor 4 agonist; Free fatty acid receptor 4 antagonist; GPR120