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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 PO 4, 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 ...
Human Chk1 is located on chromosome 11 on the cytogenic band 11q22-23. Chk1 has a N-terminal kinase domain, a linker region, a regulatory SQ/TQ domain and a C-terminal domain. [9] Chk1 contains four Ser/Gln residues. [8] Chk 1 activation occurs primarily through the phosphorylation of the conserved sites, Ser-317, Ser-345 and less often at Ser-366.
Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.
A Janus kinase inhibitor, also known as JAK inhibitor or jakinib, [1] is a type of immune modulating medication, which inhibits the activity of one or more of the Janus kinase family of enzymes (JAK1, JAK2, JAK3, TYK2), thereby interfering with the JAK-STAT signaling pathway in lymphocytes.
PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth. [2] [3] They are examples of a targeted therapy. [4] While PI3K inhibitors are an effective treatment, they can have very severe side effects and are therefore only used if other treatments have failed or are not suitable. [5] [6]
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Adavosertib is a Wee1 kinase inhibitor that is undergoing numerous clinical trials in the treatment of refractory solid tumors. [9] However, toxicities such as myelosuppression , diarrhea , and supraventricular tachyarrhythmia have arisen while attempting to determine the toxicity and effectiveness of the drug.