Design, Synthesis and Biological Activity Evaluation of Kinase Inhibitors

Dear Colleagues,

The enzymes commonly referred to as kinases are responsible for catalyzing the transfer of a phosphate group from ATP to proteins or small biomolecules, such as lipids and carbohydrates. Phosphorylation introduces structural changes in substrates, affecting their important functions in different crucial cellular processes, including proliferation, differentiation, and apoptosis. Hence, dysregulation of kinase activity prevents the substrates from playing their critical role in the regulation of intracellular homeostasis or extracellular signal transduction, leading to progressive disorders such as cancer.  Advancements of disease biology over the last decade have allowed the scientific community to validate several protein and lipid kinases as therapeutic targets for cancer. However, the emergence of drug resistance has restricted the efficacy of kinase inhibitors, resulting in recurrence and poor prognosis. Growing evidence suggests many factors, including tumor microenvironment and epigenetics, as plausible underlying causes for kinase resistance. Over the past few years, there have been steadily increasing efforts in the development of multitargeted kinase inhibitors, as well as adjuvant therapies to overcome drug resistance and improve clinical benefits.

This Special Issue offers a platform for high-quality articles on design, development, and biological evaluation of kinase inhibitors, with the hope being that a better understanding of their structure, function, regulation, and biological roles can be achieved. Both review articles and research articles addressing current advances in the field are welcome.

Dr. Souvik Banerjee
Guest Editor

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• kinase inhibitors
• dual inhibitors
• adjuvant therapy
• metabolic stability
• drug resistance