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Overview

Kinases are a class of enzymes that catalyze the transfer of phosphate groups from high-energy donor molecules (such as ATP) to specific substrate molecules. Protein kinases constitute the largest subfamily, regulating target protein activity, localization, and interactions through phosphorylation, and play central roles in signal transduction, cell cycle control, metabolic regulation, and gene expression. The human genome encodes more than 500 protein kinases, accounting for approximately 2% of all protein-coding genes.

Dysregulation or mutation of protein kinases is closely associated with various human diseases, including cancer, inflammatory disorders, neurodegenerative diseases, and metabolic syndromes. It is estimated that approximately 30% of all human cancers harbor kinase mutations or overexpression. Consequently, kinases have become the second largest drug target family after GPCRs. To date, more than 80 small-molecule kinase inhibitors have been approved by the FDA for the treatment of various cancers, autoimmune diseases, and inflammatory disorders. Recombinant kinase proteins serve as indispensable tools in drug screening, target validation, and structure-function studies.

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