Back Inhibidor de la proteïna quinasa Catalan Proteinkinaseinhibitor German مهارکننده پروتئین کیناز Persian Inhibiteur de kinase French מעכבי פרוטאין קינאז HE Zaviralec proteinskih kinaz Slovenian
A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases.[1] Protein kinases are enzymes that phosphorylate (add a phosphate, or PO4, group) to a protein and can modulate its function.[2]
The phosphate groups are usually added to serine, threonine, or tyrosine amino acids on the protein. Most kinases act on both serine and threonine, the tyrosine kinases act on tyrosine, and a number (dual-specificity kinases) act on all three. There are also protein kinases that phosphorylate other amino acids, including histidine kinases that phosphorylate histidine residues.[3]
Phosphorylation regulates many biological processes, and protein kinase inhibitors can be used to treat diseases due to hyperactive protein kinases (including mutant or overexpressed kinases in cancer) or to modulate cell functions to overcome other disease drivers.
- ^ "Protein Kinase Inhibitors", LiverTox: Clinical and Research Information on Drug-Induced Liver Injury, Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases, 2012, PMID 31643906, retrieved 2025-01-07
- ^ Cheng, Heung-Chin; Qi, Robert Z.; Paudel, Hemant; Zhu, Hong-Jian (2011-12-13). "Regulation and Function of Protein Kinases and Phosphatases". Enzyme Research. 2011: 1–3. doi:10.4061/2011/794089. ISSN 2090-0414. PMC 3238372. PMID 22195276.
- ^ Wolanin, Peter M.; Thomason, Peter A.; Stock, Jeffry B. (2002-09-25). "Histidine protein kinases: key signal transducers outside the animal kingdom". Genome Biology. 3 (10): reviews3013.1. doi:10.1186/gb-2002-3-10-reviews3013. ISSN 1474-760X. PMC 244915. PMID 12372152.