Protein kinase inhibitor
A protein kinase inhibitor is a type of enzyme inhibitor that specifically blocks the action of one or more protein kinases. Hence, they 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.
They can interfere with the repair of DNA double-strand breaks.[1]
Clinical use
Kinase inhibitors such as dasatinib are often used in the treatment of cancer and inflammation. The novel kinase inhibitor PLX5568 is currently in clinical trials for treatment of polycystic kidney disease as well as pain.[2]
Some of the kinase inhibitors used in treating cancer are inhibitors of tyrosine kinases.[3] The effectiveness of kinase inhibitors on various cancers can vary from patient to patient[4].
Examples
Currently there are several drugs launched or in development that target protein kinases and the receptors that activate them:
See also
References
External links
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| CI monoclonal antibodies ("-mab") |
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| Tyrosine-kinase inhibitors ("-nib") |
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ErbB: HER1/EGFR (Erlotinib, Gefitinib, Vandetanib) • HER1/EGFR and HER2/neu (Afatinib, Lapatinib, Neratinib)
RTK class III: C-kit and PDGFR (Axitinib, Pazopanib, Sunitinib, Sorafenib, Toceranib) • FLT3 (Lestaurtinib)
VEGFR ( Axitinib, Cediranib, Pazopanib, Regorafenib, Semaxanib, Sorafenib, Sunitinib, Toceranib, Vandetanib)
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| Other |
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