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 …

Glioblastoma multiforme: Pathogenesis and treatment

C Alifieris, DT Trafalis - Pharmacology & therapeutics, 2015 - Elsevier
Abstract Each year, about 5–6 cases out of 100,000 people are diagnosed with primary
malignant brain tumors, of which about 80% are malignant gliomas (MGs). Glioblastoma …

Comprehensive analysis of kinase inhibitor selectivity

MI Davis, JP Hunt, S Herrgard, P Ciceri… - Nature …, 2011 - nature.com
We tested the interaction of 72 kinase inhibitors with 442 kinases covering> 80% of the
human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more …

Targeting RTK signaling pathways in cancer

T Regad - Cancers, 2015 - mdpi.com
The RAS/MAP kinase and the RAS/PI3K/AKT pathways play a key role in the regulation of
proliferation, differentiation and survival. The induction of these pathways depends on …

Targeting MET in cancer: rationale and progress

E Gherardi, W Birchmeier, C Birchmeier… - Nature reviews …, 2012 - nature.com
Uncontrolled cell survival, growth, angiogenesis and metastasis are essential hallmarks of
cancer. Genetic and biochemical data have demonstrated that the growth and motility factor …

MET: a promising anticancer therapeutic target

S Peters, AA Adjei - Nature reviews Clinical oncology, 2012 - nature.com
The MET pathway is dysregulated in many human cancers and promotes tumour growth,
invasion and dissemination. Abnormalities in MET signalling have been reported to …

Targeting receptor tyrosine kinase MET in cancer: small molecule inhibitors and clinical progress

JJ Cui - Journal of medicinal chemistry, 2014 - ACS Publications
The HGF/MET signaling pathway is critical in mediating a wide range of normal
physiological functions including embryological development, wound healing, and tissue …

Small molecule kinase inhibitors for the treatment of brain cancer

TP Heffron - Journal of medicinal chemistry, 2016 - ACS Publications
In addition to each of the factors that govern the identification of a successful oncology drug
candidate, drug discovery aimed at treating neurological cancer must also consider the …

EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors

F Bladt, B Faden, M Friese-Hamim, C Knuehl… - Clinical Cancer …, 2013 - AACR
Purpose: The mesenchymal–epithelial transition factor (c-Met) receptor, also known as
hepatocyte growth factor receptor (HGFR), controls morphogenesis, a process that is …

Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective …

H Jia, G Dai, J Weng, Z Zhang, Q Wang… - Journal of medicinal …, 2014 - ACS Publications
HGF/c-Met signaling has been implicated in human cancers. Herein we describe the
invention of a series of novel triazolopyrazine c-Met inhibitors. The structure–activity …