Current Enzyme Inhibition - Volume 13, Issue 2, 2017

After G protein-coupled (GPC) receptors, protein kinases are considered as most important drug targets. Kinase family consists of multigene, which is particularly relevant to various diseases. Protein phosphorylation by kinases plays a crucial activity in many cellular processes like apoptosis, cell division, survival, metabolism, etc. The emergence of various protein kinases crystal structures from many research groups gives a dee Read More

Objective: To delineate specificity of binding in protein kinases with its substrate or inhibitors so that the design of its inhibitors can be facilitated. Background: For the treatment of a variety of disorders in humans such as cancer, inflammation, diabetes, infections, cardiovascular diseases, etc., protein kinases have been found as a very prominent target and thus attempts have been made to find the potent inhibitors of these kin Read More

Almost thirty percent of the protein targets currently under exploration and study constitute the protein kinases which have always attracted the pharmaceutical companies as they are easy targets for drug development. Although the kinases will remain major focus of oncology for many years to come in the development of anticancer drugs, the number of kinase inhibitors as therapeutic targets for the treatment of sever Read More

The current review deals with the involvement of glycogen synthase kinase-3 (GSK-3) in major neurodegenerative disorders like Alzheimer’s Disease (AD), Cerebral ischemia, Parkinson’s Disease (PD) and Amyotrophic Lateral Sclerosis (ALS). GSK-3 is a proline-directed serine/threonine kinase, considered as a key influencer in these pathologies. From gene to protein, every process has crucial involvement in the genesis Read More

The Abl family of non-receptor tyrosine kinases encoded by the genes ABL1 and ABL2 are part of the signaling pathways that control cell proliferation, migration and apoptosis. The activity of Abl family kinases is tightly controlled through an autoinhibitory mechanism based on intramolecular interactions controlling the activity of the kinase domain. Activation of Abl kinases is promoted by phosphorylation by ups Read More

Objective: To investigate the various physicochemical descriptors employed towards biological activity of tyrosine kinase inhibitors. Background: In oncology, kinase domain has emerged as an important pharmacological target. The receptor tyrosine kinases on deregulation (i.e. over expression, chromosomal translocation, gene amplication, mutation) contribute towards development of cancer and thus it has been emerged as p Read More