Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021 - nature.com
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

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 …

Kinase-targeted cancer therapies: progress, challenges and future directions

KS Bhullar, NO Lagarón, EM McGowan, I Parmar… - Molecular cancer, 2018 - Springer
The human genome encodes 538 protein kinases that transfer a γ-phosphate group from
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …

Small molecule inhibitors targeting the cancers

GH Liu, T Chen, X Zhang, XL Ma, HS Shi - MedComm, 2022 - Wiley Online Library
Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and
tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer …

Ten things you should know about protein kinases: IUPHAR R eview 14

D Fabbro, SW Cowan‐Jacob… - British journal of …, 2015 - Wiley Online Library
Many human malignancies are associated with aberrant regulation of protein or lipid
kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein …

Structural insight and development of EGFR tyrosine kinase inhibitors

T Amelia, RE Kartasasmita, T Ohwada, DH Tjahjono - Molecules, 2022 - mdpi.com
Lung cancer has a high prevalence, with a growing number of new cases and mortality
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …

Targeting cancer with small molecule kinase inhibitors

J Zhang, PL Yang, NS Gray - Nature reviews cancer, 2009 - nature.com
Deregulation of kinase activity has emerged as a major mechanism by which cancer cells
evade normal physiological constraints on growth and survival. To date, 11 kinase inhibitors …

Epidermal growth factor receptor mutations in lung cancer

SV Sharma, DW Bell, J Settleman, DA Haber - Nature Reviews Cancer, 2007 - nature.com
The development and clinical application of inhibitors that target the epidermal growth factor
receptor (EGFR) provide important insights for new lung cancer therapies, as well as for the …

Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain

W Pao, VA Miller, KA Politi, GJ Riely, R Somwar… - PLoS …, 2005 - journals.plos.org
Background Lung adenocarcinomas from patients who respond to the tyrosine kinase
inhibitors gefitinib (Iressa) or erlotinib (Tarceva) usually harbor somatic gain-of-function …

Frequent and Focal FGFR1 Amplification Associates with Therapeutically Tractable FGFR1 Dependency in Squamous Cell Lung Cancer

J Weiss, ML Sos, D Seidel, M Peifer, T Zander… - Science translational …, 2010 - science.org
Lung cancer remains one of the leading causes of cancer-related death in developed
countries. Although lung adenocarcinomas with EGFR mutations or EML4-ALK fusions …