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Trends in kinase drug discovery: targets, indications and inhibitor design
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 …
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 …
processes. Deregulation of FGFR signalling is observed in a subset of many cancers …
Kinase-targeted cancer therapies: progress, challenges and future directions
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 …
ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with …
Small molecule inhibitors targeting the cancers
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 …
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 …
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 …
every year. Furthermore, the survival rate of patients with non-small-cell lung carcinoma …
Targeting cancer with small molecule kinase inhibitors
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 …
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 …
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
Background Lung adenocarcinomas from patients who respond to the tyrosine kinase
inhibitors gefitinib (Iressa) or erlotinib (Tarceva) usually harbor somatic gain-of-function …
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
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 …
countries. Although lung adenocarcinomas with EGFR mutations or EML4-ALK fusions …