Rogaratinib: A potent and selective pan‐FGFR inhibitor with broad antitumor activity in FGFR‐overexpressing preclinical cancer models

S Grünewald, O Politz, S Bender… - … journal of cancer, 2019 - Wiley Online Library
Aberrant activation in fibroblast growth factor signaling has been implicated in the
development of various cancers, including squamous cell lung cancer, squamous cell head …

ErbB-3 mediates phosphoinositide 3-kinase activity in gefitinib-sensitive non-small cell lung cancer cell lines

JA Engelman, PA Jänne, C Mermel… - Proceedings of the …, 2005 - National Acad Sciences
Therapies that target the EGF receptor (EGFR), such as gefitinib (IRESSA), are effective in a
subset of patients with advanced non-small cell lung cancer (NSCLC). The differences in …

FGFR blockade inhibits targeted therapy-tolerant persister in basal FGFR1-and FGF2-high cancers with driver oncogenes

K Furugaki, T Fujimura, H Mizuta, T Yoshimoto… - NPJ Precision …, 2023 - nature.com
Cancer cell resistance arises when tyrosine kinase inhibitor (TKI)-targeted therapies induce
a drug-tolerant persister (DTP) state with growth via genetic aberrations, making DTP cells …

A systems mechanism for KRAS mutant allele–specific responses to targeted therapy

T McFall, JK Diedrich, M Mengistu, SL Littlechild… - Science …, 2019 - science.org
Cancer treatment decisions are increasingly guided by which specific genes are mutated
within each patient's tumor. For example, agents inhibiting the epidermal growth factor …

[HTML][HTML] Targeting FGFR in non-small cell lung cancer: implications from the landscape of clinically actionable aberrations of FGFR kinases

Z Zhou, Z Liu, Q Ou, X Wu, X Wang, Y Shao… - Cancer Biology & …, 2021 - ncbi.nlm.nih.gov
Objective: Dysfunction in fibroblast growth factor receptor (FGFR) signaling has been
reported in diverse cancer types, including non-small cell lung cancer (NSCLC). The …

Kinase domain activation of FGFR2 yields high-grade lung adenocarcinoma sensitive to a Pan-FGFR inhibitor in a mouse model of NSCLC

JH Tchaicha, EA Akbay, A Altabef, OR Mikse, E Kikuchi… - Cancer research, 2014 - AACR
Somatic mutations in FGFR2 are present in 4% to 5% of patients diagnosed with non–small
cell lung cancer (NSCLC). Amplification and mutations in FGFR genes have been identified …

Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth

F Harbinski, VJ Craig, S Sanghavi, D Jeffery, L Liu… - Cancer discovery, 2012 - AACR
The overall power of kinase inhibitors is substantially overshadowed by the acquisition of
drug resistance. To address this issue, we systematically assessed the potential of secreted …

[HTML][HTML] KRAS and HRAS mutations confer resistance to MET targeting in preclinical models of MET-expressing tumor cells

D Leiser, M Medová, K Mikami, L Nisa, D Stroka… - Molecular …, 2015 - Elsevier
The MET receptor tyrosine kinase is often deregulated in human cancers and several MET
inhibitors are evaluated in clinical trials. Similarly to EGFR, MET signals through the RAS …

Combination of EGFR and MEK1/2 inhibitor shows synergistic effects by suppressing EGFR/HER3-dependent AKT activation in human gastric cancer cells

YK Yoon, HP Kim, SW Han, HS Hur, DY Oh… - Molecular cancer …, 2009 - AACR
EGFR tyrosine kinase inhibitors have shown promising efficacy in the treatment of tumors
with EGFR mutations and amplifications. However, tyrosine kinase inhibitors have also …

[HTML][HTML] Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use

H Patani, TD Bunney, N Thiyagarajan, RA Norman… - Oncotarget, 2016 - ncbi.nlm.nih.gov
Frequent genetic alterations discovered in FGFRs and evidence implicating some as drivers
in diverse tumors has been accompanied by rapid progress in targeting FGFRs for …