title: Identification of novel peptoid agonists of fibroblast growth factor receptor using microarray-based screening.
abstract: Drug development targeting fibroblast growth factor receptors (FGFRs) represents an emerging theme in the field of medicinal chemistry. Considering the fact that most of the currently identified FGFR agonists are long chain peptides with limited stability, the discovery of novel non-peptide FGFR ligands is still highly demanded. A linear one-bead-one-compound peptoid (oligomers of N-substituted glycine units) library with a theoretical diversity of 106was designed and synthesized. Microarray-based screening led to the identification of four hit sequences1-4as FGFR1α ligands, which were further confirmed using both solution-phase and solid-phase binding assays. Western blot results indicated that peptoids2-4activated FGFR signaling pathways, resulting in increased levels of p-Akt and p-ERK in different cell lines. Our work discovered novel peptoid ligands as FGFR agonists, shedding new light on FGFR-based drug discovery.
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, 32610.
authors.forename: Junjie
authors.initials: J
authors.lastname: Fu
authors.affiliation: Columbia University, New York, NY 10027.
authors.forename: Amy
authors.initials: A
authors.lastname: Xia
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL, 32610.
authors.forename: Xin
authors.initials: X
authors.lastname: Qi