Novel quinazoline-based EGFR kinase inhibitors: A review focussing on SAR and molecular docking studies (2015-2019)
The over expression of EGFR has been recognized as the driver mechanism in the
occurrence and progression of carcinomas such as lung cancer, breast cancer, pancreatic …
occurrence and progression of carcinomas such as lung cancer, breast cancer, pancreatic …
Protein kinase inhibitors: contributions from structure to clinical compounds
LN Johnson - Quarterly reviews of biophysics, 2009 - cambridge.org
Protein kinases catalyse key phosphorylation reactions in signalling cascades that affect
every aspect of cell growth, differentiation and metabolism. The kinases have become prime …
every aspect of cell growth, differentiation and metabolism. The kinases have become prime …
Flavonoids as protein kinase inhibitors for cancer chemoprevention: direct binding and molecular modeling
DX Hou, T Kumamoto - Antioxidants & redox signaling, 2010 - liebertpub.com
Protein kinases play crucial roles in the regulation of multiple cell signaling pathways and
cellular functions. Deregulation of protein kinase function has been implicated in …
cellular functions. Deregulation of protein kinase function has been implicated in …
A conserved protonation-dependent switch controls drug binding in the Abl kinase
Y Shan, MA Seeliger, MP Eastwood… - Proceedings of the …, 2009 - National Acad Sciences
In many protein kinases, a characteristic conformational change (the “DFG flip”) connects
catalytically active and inactive conformations. Many kinase inhibitors—including the cancer …
catalytically active and inactive conformations. Many kinase inhibitors—including the cancer …
Mechanisms of drug resistance in kinases
R Barouch-Bentov, K Sauer - Expert opinion on investigational …, 2011 - Taylor & Francis
Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …
have become the second largest drug target family. The great success of the BCR-ABL …
Discovery of new quinoxaline-based derivatives as anticancer agents and potent VEGFR-2 inhibitors: Design, synthesis, and in silico study
VEGFR-2 is one of the most vital targets for the treatment of solid tumors. This work
represents synthetic approaches of new set of quinoxaline-based derivatives having …
represents synthetic approaches of new set of quinoxaline-based derivatives having …
Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase
ED Garcin, AS Arvai, RJ Rosenfeld, MD Kroeger… - Nature chemical …, 2008 - nature.com
Nitric oxide synthase (NOS) enzymes synthesize nitric oxide, a signal for vasodilatation and
neurotransmission at low concentrations and a defensive cytotoxin at higher concentrations …
neurotransmission at low concentrations and a defensive cytotoxin at higher concentrations …
Flying under the radar: the new wave of BCR–ABL inhibitors
A Quintás-Cardama, H Kantarjian… - Nature Reviews Drug …, 2007 - nature.com
The introduction of the BCR–ABL kinase inhibitor imatinib mesylate (Gleevec; Novartis)
revolutionized the treatment of chronic myeloid leukaemia (CML). However, most patients …
revolutionized the treatment of chronic myeloid leukaemia (CML). However, most patients …
Impact of Type II LRRK2 inhibitors on signaling and mitophagy
Much effort has been devoted to the development of selective inhibitors of the LRRK2 as a
potential treatment for LRRK2 driven Parkinson's disease. In this study, we first compare the …
potential treatment for LRRK2 driven Parkinson's disease. In this study, we first compare the …
Approaches to discover non-ATP site kinase inhibitors
LK Gavrin, E Saiah - MedChemComm, 2013 - pubs.rsc.org
The catalytic domain of kinases shows a high degree of sequence homology, especially for
kinases that belong to the same family. They share a common ATP binding site with a …
kinases that belong to the same family. They share a common ATP binding site with a …