Protein kinase inhibitor

A protein kinase inhibitor is a type of enzyme inhibitor that specifically blocks the action of one or more protein kinases. Protein kinases are enzymes that add a phosphate (PO₄) group to a proteins or other organic molecule, usually on the serine, threonine, or tyrosine amino acid. Hence, protein kinase inhibitors can be subdivided or characterised by the amino acids whose phosphorylation is inhibited: 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.^{[citation needed]}

Phosphorylation is a necessary step in some cancers and inflammatory diseases. Inhibiting the protein kinases, and therefore the phosphorylation, can treat these diseases. Therefore, protein kinase inhibitors are used as drugs.

Clinical use

Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation.^{[citation needed]} The novel kinase inhibitor PLX5568 is currently in clinical trials for treatment of polycystic kidney disease as well as pain.^[1]

Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinases.^[2] The effectiveness of kinase inhibitors on various cancers can vary from patient to patient^[3].

Examples

Currently there are several drugs launched or in development that target protein kinases and the receptors that activate them:

See also

• Tyrosine kinase inhibitor
• amino acid

References

External links

• MeSH Protein+kinase+inhibitors
• IC50 values for common inhibitors
• "Chemical structures and known kinase targets for clinically approved kinase inhibitors" Nature.com

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