Issue 6, 2016

Identification of novel peptoid agonists of fibroblast growth factor receptors 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 106 was designed and synthesized. Microarray-based screening led to the identification of four hit sequences 1–4 as FGFR1α ligands, which were further confirmed using both solution-phase and solid-phase binding assays. Western blot results indicated that peptoids 2–4 activated 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.

Graphical abstract: Identification of novel peptoid agonists of fibroblast growth factor receptors using microarray-based screening

Supplementary files

Article information

Article type
Research Article
Submitted
29 Feb 2016
Accepted
13 Apr 2016
First published
14 Apr 2016

Med. Chem. Commun., 2016,7, 1183-1189

Author version available

Identification of novel peptoid agonists of fibroblast growth factor receptors using microarray-based screening

J. Fu, A. Xia and X. Qi, Med. Chem. Commun., 2016, 7, 1183 DOI: 10.1039/C6MD00121A

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Spotlight

Advertisements