title: The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues.
abstract: Here we identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor.
authors.affiliation: Department of Internal Medicine and Molecular Biology, Division of Translational Research, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390-9185, USA.
authors.forename: D Gomika
authors.initials: DG
authors.lastname: Udugamasooriya
authors.forename: Geoff
authors.initials: G
authors.lastname: Dunham
authors.forename: Caroline
authors.initials: C
authors.lastname: Ritchie
authors.forename: Rolf A
authors.initials: RA
authors.lastname: Brekken
authors.forename: Thomas
authors.initials: T
authors.lastname: Kodadek
mesh_terms: D015394:Molecular Structure; D034444:Peptoids / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: C533385:GU40C compound; D034444:Peptoids; D040301:Vascular Endothelial Growth Factor Receptor-2