Advances and challenges in targeting FGFR signalling in cancer

IS Babina, NC Turner - Nature Reviews Cancer, 2017 - nature.com
Fibroblast growth factors (FGFs) and their receptors (FGFRs) regulate numerous cellular
processes. Deregulation of FGFR signalling is observed in a subset of many cancers …

Advances in covalent kinase inhibitors

A Abdeldayem, YS Raouf, SN Constantinescu… - Chemical Society …, 2020 - pubs.rsc.org
Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

[HTML][HTML] Androgen receptor pathway-independent prostate cancer is sustained through FGF signaling

EG Bluemn, IM Coleman, JM Lucas, RT Coleman… - Cancer cell, 2017 - cell.com
Androgen receptor (AR) signaling is a distinctive feature of prostate carcinoma (PC) and
represents the major therapeutic target for treating metastatic prostate cancer (mPC) …

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 …

A comprehensive transcriptional portrait of human cancer cell lines

C Klijn, S Durinck, EW Stawiski, PM Haverty… - Nature …, 2015 - nature.com
Tumor-derived cell lines have served as vital models to advance our understanding of
oncogene function and therapeutic responses. Although substantial effort has been made to …

Activation of cardiac fibroblast growth factor receptor 4 causes left ventricular hypertrophy

A Grabner, AP Amaral, K Schramm, S Singh, A Sloan… - Cell metabolism, 2015 - cell.com
Chronic kidney disease (CKD) is a worldwide public health threat that increases risk of
death due to cardiovascular complications, including left ventricular hypertrophy (LVH) …

FGF23 induces left ventricular hypertrophy

C Faul, AP Amaral, B Oskouei, MC Hu… - The Journal of …, 2011 - Am Soc Clin Investig
Chronic kidney disease (CKD) is a public health epidemic that increases risk of death due to
cardiovascular disease. Left ventricular hypertrophy (LVH) is an important mechanism of …

Ex vivo culture of circulating breast tumor cells for individualized testing of drug susceptibility

M Yu, A Bardia, N Aceto, F Bersani, MW Madden… - science, 2014 - science.org
Circulating tumor cells (CTCs) are present at low concentrations in the peripheral blood of
patients with solid tumors. It has been proposed that the isolation, ex vivo culture, and …

FGF21 acts centrally to induce sympathetic nerve activity, energy expenditure, and weight loss

BM Owen, X Ding, DA Morgan, KC Coate, AL Bookout… - Cell metabolism, 2014 - cell.com
The mechanism by which pharmacologic administration of the hormone FGF21 increases
energy expenditure to cause weight loss in obese animals is unknown. Here we report that …

Antitumor activity of lenvatinib (e7080): an angiogenesis inhibitor that targets multiple receptor tyrosine kinases in preclinical human thyroid cancer models

O Tohyama, J Matsui, K Kodama… - Journal of thyroid …, 2014 - Wiley Online Library
Inhibition of tumor angiogenesis by blockading the vascular endothelial growth factor
(VEGF) signaling pathway is a promising therapeutic strategy for thyroid cancer. Lenvatinib …