Protein kinases (PKs) are kinases that phosphorylate the amino acid residues of a protein. There are four major families of protein kinases in humans (listed here in descending order of number of known members present in humans):
- Serine/threonine PKs (1)
- Tyrosine PKs (or just tyrosine kinases) (2)
- Tyrosine kinase-like PKs (3)
- Mixed PKs (4)
(1) can be further subdivided into several different specific PKs, including:
- Glycogen synthase kinase-3 beta (GSK-3β) which is involved in glucose homeostasis, cell survival (especially neuronal cell survival where it is implicated in the pathogenesis of Alzheimer disease, Huntington disease and bipolar disorder), gene expression and microtubule formation.
- Protein kinase A
- Protein kinase C which is involved in the signalling cascades of cancers, diabetic complications, autoimmune diseases and lung diseases.
- Raf kinases like B-Raf (or BRAF) which involved in several malignancies. BRAF inhibitors like dabrafenib and vemurafenib have received regulatory approval for the treatment of malignant melanoma.
- Serine/threonine-protein kinase mTOR (usually just abbreviated mTOR) which is a kinase involved in cell signalling, cellular proliferation, differentiation, survival and ageing and is conserved in all eukaryotes.
- Bcr-Abl tyrosine kinase (also known as the Philadelphia chromosome), which is a constitutively active TK that is formed by the fusion of the Bcr and Abl genes on chromosome 9 and 22, respectively. It is present in almost all cases of chronic myeloid leukaemia and some cases of adult acute lymphoblastic leukaemia and acute myeloid leukaemia. Several inhibitors of the TK are available for the treatment of these leukaemias including: dasatinib, imatinib and nilotinib.
- VEGF-A receptors such as VEGFR1, VEGFR2, VEGFR3, etc. Plays a crucial role in angiogenesis; hence inhibitors often have therapeutic effects in cancers. Inhibited by various tyrosine kinase inhibitors (TKIs) including sorafenib and sunitinib.
- NCBI Bookshelf provides free book resources on this topic.
- PubMed provides review articles from the past five years (limit to free review articles or to systematic reviews)
- The TRIP database provides clinical publications about evidence-based medicine.
- ↑ Roskoski, R, Jr (27 August 2010). "RAF protein-serine/threonine kinases: structure and regulation." (PDF). Biochemical and Biophysical Research Communications 399 (3): 313–7. PMID 20674547. doi:10.1016/j.bbrc.2010.07.092.
- ↑ "GSK3B - Glycogen synthase kinase-3 beta - Homo Sapiens". UniProt. Switzerland, UK, USA: UniProt Consortium. 26 November 2014. Retrieved 5 January 2015.
- ↑ Sobhia, ME; Grewal, BK; Ml, SP; Patel, J; Kaur, A; Haokip, T; Kokkula, A (October 2013). "Protein kinase C inhibitors: a patent review (2008 - 2009).". Expert Opinion on Therapeutic Patents 23 (10): 1297–315. PMID 23795914. doi:10.1517/13543776.2013.805205.
- ↑ Iqbal, N; Iqbal, N (2014). "Imatinib: a breakthrough of targeted therapy in cancer.". Chemotherapy Research and Practice 2014: 357027. PMC 4055302. PMID 24963404. doi:10.1155/2014/357027.