Kinase or Protease

Kinase or Protease refers to two distinct and expansive superfamilies of enzymes that play fundamental roles in cellular physiology and are major focuses of modern pharmacology. Kinases are enzymes that catalyze the transfer of a phosphate group from ATP to specific substrates, a process known as phosphorylation that acts as a primary switch for signal transduction, cell growth, and metabolism (Manning et al., 2002). Proteases, or peptidases, are enzymes that catalyze the hydrolysis of peptide bonds, facilitating protein degradation, processing of signaling molecules, and blood coagulation (Puente et al., 2003). While both classes are critical therapeutic targets, the term Kinase or Protease is a broad categorical grouping rather than a specific molecular target. Dysregulation of kinases is frequently linked to oncogenesis and inflammatory disorders, whereas protease dysfunction is associated with viral infections, cardiovascular diseases, and neurodegeneration (Rawlings et al., 2018). Consequently, drugs targeting these enzymes, such as small-molecule kinase inhibitors or protease inhibitors, must be highly selective to avoid significant off-target toxicity arising from the high degree of structural conservation within these enzyme families (Roskoski, 2021).

Other names

PhosphotransferasesPeptidasesProteolytic enzymesProtein kinasesProteinases

Kinase inhibitors typically act via ATP-competitive or allosteric inhibition to block phosphorylation, while protease inhibitors bind to the active site to prevent proteolytic cleavage of substrate proteins.