The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues.
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.
Udugamasooriya
D Gomika
DG
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.
Dunham
Geoff
G
Ritchie
Caroline
C
Brekken
Rolf A
RA
Kodadek
Thomas
T
D015394:Molecular Structure; D034444:Peptoids / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
C533385:GU40C compound; D034444:Peptoids; D040301:Vascular Endothelial Growth Factor Receptor-2