Advances in covalent drug discovery

L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

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 …

Liquid versus tissue biopsy for detecting acquired resistance and tumor heterogeneity in gastrointestinal cancers

AR Parikh, I Leshchiner, L Elagina, L Goyal… - Nature medicine, 2019 - nature.com
During cancer therapy, tumor heterogeneity can drive the evolution of multiple tumor
subclones harboring unique resistance mechanisms in an individual patient,–. Previous …

TAS-120 overcomes resistance to ATP-competitive FGFR inhibitors in patients with FGFR2 fusion–positive intrahepatic cholangiocarcinoma

L Goyal, L Shi, LY Liu, F Fece de la Cruz, JK Lennerz… - Cancer discovery, 2019 - AACR
ATP-competitive fibroblast growth factor receptor (FGFR) kinase inhibitors, including
BGJ398 and Debio 1347, show antitumor activity in patients with intrahepatic …

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 …

Polyclonal Secondary FGFR2 Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

L Goyal, SK Saha, LY Liu, G Siravegna, I Leshchiner… - Cancer discovery, 2017 - AACR
Genetic alterations in the fibroblast growth factor receptor (FGFR) pathway are promising
therapeutic targets in many cancers, including intrahepatic cholangiocarcinoma (ICC). The …

Futibatinib is a novel irreversible FGFR 1–4 inhibitor that shows selective antitumor activity against FGFR-deregulated tumors

H Sootome, H Fujita, K Ito, H Ochiiwa, Y Fujioka, K Ito… - Cancer Research, 2020 - AACR
FGFR signaling is deregulated in many human cancers, and FGFR is considered a valid
target in FGFR-deregulated tumors. Here, we examine the preclinical profile of futibatinib …

Fibroblast growth factor receptors as treatment targets in clinical oncology

M Katoh - Nature reviews Clinical oncology, 2019 - nature.com
FGFRs are receptor tyrosine kinases with a role in several biological processes, such as the
regulation of development and tissue repair. However, alterations in FGFRs 1–4, such as …

Receptor tyrosine kinase-targeted cancer therapy

T Yamaoka, S Kusumoto, K Ando, M Ohba… - International journal of …, 2018 - mdpi.com
In the past two decades, several molecular targeted inhibitors have been developed and
evaluated clinically to improve the survival of patients with cancer. Molecular targeted …

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 …