A protein kinase inhibitor is an enzyme inhibitor that blocks the action of protein kinases. Protein kinases are important regulators of cell functions that utilize a process known as phosphorylation. In phosphorylation, phosphate groups are added to specific binding sites on other proteins resulting in a physical conformational change that can turn on or off the activity of the molecule.
This simple addition or subtraction of phosphate groups has an enormous impact on the activity in the cell. Protein kinases are responsible for regulating signal transduction, the cell cycle, proliferation, metabolism, and apoptosis. Because they are so integral to so many key cell functions, a disease like cancer (characterized by abnormal cell growth) relies heavily on protein kinases to survive and spread. Inhibition of this phosphate binding action has become a promising research area for cancer therapies.
LKT Laboratories carries hundreds of protein kinase inhibitors for use in the research of protein and cell functions, especially as they pertain to cancer, autoimmune disorders, cardiac disease, and other conditions.
Inhibitors By Binding Site
Protein kinase inhibitors are typically categorized by the amino acid they act on. Tyrosine, serine, and threonine are all possible binding locations for phosphate groups, and therefore possible targets for inhibition.
Inhibitors By Pathway
LKT’s broad selection of inhibitors target many different signaling pathways. These pathways are frequently involved with cellular proliferation and growth, so it’s not surprising that they are being studied in cancer research. Some of the most popular signaling pathway targets include: