Protein kinase inhibitor

A protein kinase inhibitor ( PKI) is a type of enzyme inhibitor that blocks the action of one or more . Protein kinases are enzymes that phosphorylate (add a phosphate, or PO₄, group) to a protein and can modulate its function.

The phosphate groups are usually added to serine, threonine, or tyrosine on the protein. Most kinases act on both serine and threonine, the act on tyrosine, and a number (dual-specificity kinases) act on all three. There are also protein kinases that phosphorylate other amino acids, including that phosphorylate histidine residues.

Phosphorylation regulates many biological processes, and protein kinase inhibitors can be used to treat diseases due to hyperactive protein kinases (including mutant or overexpressed kinases in cancer) or to modulate cell functions to overcome other disease drivers.

Some of the kinase inhibitors used in treating cancer are inhibitors of . The effectiveness of kinase inhibitors on various cancers can vary from patient to patient.

! Name !! Target !! Company !! Class !! FDA approval

Note:
AD = Approval date.
MS = Myelosuppression.
D = Diarrhoea.
FR = Fluid retention.
As far as myelosuppression, diarrhoea and fluid retention goes: +++ means >70% of patients exhibit clinically significant myelosuppression. ++ means 30-70% of patients exhibit significant myelosuppression. + means 10-30% of patients exhibit significant myelosuppression. - means 0-10% of patients exhibit this side effect.
General references templates are given, which refer the reader to the respective drug database.

• Tyrosine kinase inhibitor

• PKIDB: A searchable database of kinase inhibitors in clinical trials containing physicochemical properties and structures, protein kinase targets, therapeutic indications, year of first approval, and trade names
• A list of US FDA-approved small molecule protein kinase inhibitors, their protein kinase targets, therapeutic indications, and links to the FDA label are provided at the Blue Ridge Institute for Medical Research web site.