Discovery and pharmacological characterization of JNJ-42756493 (Erdafitinib), a functionally selective small-molecule FGFR family inhibitor

TPS Perera, E Jovcheva, L Mevellec, J Vialard… - Molecular cancer …, 2017 - AACR
Fibroblast growth factor (FGF) signaling plays critical roles in key biological processes
ranging from embryogenesis to wound healing and has strong links to several hallmarks of …

A successful collaboration between academia, biotech and pharma led to discovery of erdafitinib, a selective FGFR inhibitor recently approved by the FDA

CW Murray, DR Newell, P Angibaud - MedChemComm, 2019 - pubs.rsc.org
Fibroblast growth factor receptors (FGFR) belong to a family of 4 receptor tyrosine kinases
(FGFR1–4) which dimerise and auto-phosphorylate upon binding to one of the multiple FGF …

[HTML][HTML] Fibroblast growth factor receptors (FGFRs): structures and small molecule inhibitors

S Dai, Z Zhou, Z Chen, G Xu, Y Chen - Cells, 2019 - mdpi.com
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases
expressed on the cell membrane that play crucial roles in both developmental and adult …

AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family

PR Gavine, L Mooney, E Kilgour, AP Thomas… - Cancer research, 2012 - AACR
The fibroblast growth factor (FGF) signaling axis is increasingly implicated in tumorigenesis
and chemoresistance. Several small-molecule FGF receptor (FGFR) kinase inhibitors are …

[HTML][HTML] INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor …

PCC Liu, H Koblish, L Wu, K Bowman, S Diamond… - PLoS …, 2020 - journals.plos.org
Alterations in fibroblast growth factor receptor (FGFR) genes have been identified as
potential driver oncogenes. Pharmacological targeting of FGFRs may therefore provide …

A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models

G Zhao, W Li, D Chen, JR Henry, HY Li, Z Chen… - Molecular cancer …, 2011 - AACR
The fibroblast growth factor receptors (FGFR) are tyrosine kinases that are present in many
types of endothelial and tumor cells and play an important role in tumor cell growth, survival …

The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor

Y Nakanishi, N Akiyama, T Tsukaguchi, T Fujii… - Molecular cancer …, 2014 - AACR
The FGF receptors (FGFR) are tyrosine kinases that are constitutively activated in a subset of
tumors by genetic alterations such as gene amplifications, point mutations, or chromosomal …

Fibroblast growth factor receptor inhibitors as a cancer treatment: from a biologic rationale to medical perspectives

MV Dieci, M Arnedos, F Andre, JC Soria - Cancer discovery, 2013 - AACR
The fibroblast growth factor/fibroblast growth factor receptor (FGF/FGFR) signaling pathway
plays a fundamental role in many physiologic processes, including embryogenesis, adult …

Anticancer molecules targeting fibroblast growth factor receptors

G Liang, Z Liu, J Wu, Y Cai, X Li - Trends in pharmacological sciences, 2012 - cell.com
The fibroblast growth factor receptor (FGFR) family includes four highly conserved receptor
tyrosine kinases: FGFR1–4. Upon ligand binding, FGFRs activate an array of downstream …

[HTML][HTML] Signaling pathway and small-molecule drug discovery of FGFR: A comprehensive review

J Zheng, W Zhang, L Li, Y He, Y Wei, Y Dang… - Frontiers in …, 2022 - frontiersin.org
Targeted therapy is a groundbreaking innovation for cancer treatment. Among the receptor
tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered substantial …