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.[citation needed]
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.[citation needed] 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 kinase.[3] The effectiveness of kinase inhibitors on various cancers can vary from patient to patient[4].
Examples
Currently there are several drugs launched that target protein kinases and the receptors that activate them:
References
External links
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Targeted therapy / extracellular chemotherapeutic agents/antineoplastic agents (L01) |
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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, Lapatinib, Vandetanib, Neratinib) · HER2/neu (Lapatinib, Neratinib)
RTK class III: C-kit (Axitinib, Sunitinib, Sorafenib, Toceranib) · FLT3 (Lestaurtinib) · PDGFR (Axitinib, Sunitinib, Sorafenib, Toceranib)
VEGFR ( Vandetanib, Semaxanib, Cediranib, Axitinib, Sunitinib, Sorafenib, Toceranib, Regorafenib)
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