title: Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
abstract: Herein we report the first disclosure of biphenyl azoles that are nanomolar binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized.
authors.affiliation: Department of Metabolic Disease Chemistry, Bristol Myers-Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. sulskyr@bms.com
authors.forename: Richard
authors.initials: R
authors.lastname: Sulsky
authors.forename: David R
authors.initials: DR
authors.lastname: Magnin
authors.forename: Yanting
authors.initials: Y
authors.lastname: Huang
authors.forename: Ligaya
authors.initials: L
authors.lastname: Simpkins
authors.forename: Prakash
authors.initials: P
authors.lastname: Taunk
authors.forename: Manorama
authors.initials: M
authors.lastname: Patel
authors.forename: Yeheng
authors.initials: Y
authors.lastname: Zhu
authors.forename: Terry R
authors.initials: TR
authors.lastname: Stouch
authors.forename: Donna
authors.initials: D
authors.lastname: Bassolino-Klimas
authors.forename: Rex
authors.initials: R
authors.lastname: Parker
authors.forename: Thomas
authors.initials: T
authors.lastname: Harrity
authors.forename: Robert
authors.initials: R
authors.lastname: Stoffel
authors.forename: David S
authors.initials: DS
authors.lastname: Taylor
authors.forename: Thomas B
authors.initials: TB
authors.lastname: Lavoie
authors.forename: Kevin
authors.initials: K
authors.lastname: Kish
authors.forename: Bruce L
authors.initials: BL
authors.lastname: Jacobson
authors.forename: Steven
authors.initials: S
authors.lastname: Sheriff
authors.forename: Leonard P
authors.initials: LP
authors.lastname: Adam
authors.forename: William R
authors.initials: WR
authors.lastname: Ewing
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Robl
mesh_terms: D017667:Adipocytes / Q000187:drug effects* / Q000378:metabolism; D000818:Animals; D001393:Azoles / Q000037:antagonists & inhibitors*; D001665:Binding Sites; D001713:Biphenyl Compounds / Q000037:antagonists & inhibitors*; D004195:Disease Models, Animal; D004817:Epidermis / Q000378:metabolism; D050556:Fatty Acid-Binding Proteins / Q000037:antagonists & inhibitors*; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D051379:Mice; D008956:Models, Chemical; D011869:Radioligand Assay
chemical_list: D001393:Azoles; D001713:Biphenyl Compounds; D050556:Fatty Acid-Binding Proteins; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; C010574:biphenyl