Articles on kinase
Comprehensive analysis of kinase inhibitor selectivity
10/30/2011 - Nature Biotechnology
The interaction of 72 kinase inhibitors with 442 kinases of the human protein kinome was tested. The data set suggests compounds to use as tools to study kinases for which no dedicated inhibitors exist. It also provides a foundation for further exploring kinase inhibitor biology and toxicity, as well as for studying the structural basis of the observed interaction patterns.
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity
10/30/2011 - Nature Biotechnology
The activity profile of 178 commercially available kinase inhibitors against a panel of 300 recombinant protein kinases was established. The results have implications for drug development and provide a resource for selecting compounds to elucidate kinase function and for interpreting the results of experiments involving kinase inhibitors.
05/22/2011 - Nature Medicine
An siRNA screen identified kinases whose silencing alters the estrogen response: among the most potent regulators was lemur tyrosine kinase-3 (LMTK3), for which a role has not previously been assigned. This finding reveals LMTK3 as a new therapeutic target.
04/28/2011 - PLoS Computational Biology
We propose inhibition by Nelfinavir of multiple protein kinase targets. We suggest that broad-spectrum low affinity binding by a drug or drugs to multiple targets may lead to a collective effect important in treating complex diseases such as cancer.
Development of a Cell-Selective and Intrinsically Active Multikinase Inhibitor Bioconjugate
03/28/2011 - Bioconjugate Chem.
Here, we describe a new approach in which platinum coordination chemistry is applied for the development of a cell-selective multikinase inhibitor bioconjugate.
A small molecule AMPK activator protects the heart against ischemia–reperfusion injury
03/11/2011 - Journal of Molecular and Cellular Cardiology
AMPK is a therapeutic target that can be stimulated by a direct-acting small molecule in order to prevent injury during ischemia–reperfusion. The use of AMPK activators may represent a novel strategy to protect the heart and other solid organs against ischemia.