Chapter 2
Anticancer Drugs - E. Kinase Modulators
A protein
kinase modifies a specific protein (substrate) by chemically adding a phosphate
group (from ATP) to change the function/activity of the substrate that
regulates the cellular pathways, especially signal transduction pathways. This
process of adding a phosphate group to a substrate is referred to as
phosphorylation. During the phosphorylation process, ATP loses a phosphate
group and becomes ADP.
Phosphorylation is a very important
reaction, which regulates a lot of biological processes. The phosphate groups
are often added to tyrosine, threonine, or serine. As a result of the
phosphorylation, many biological processes are regulated. Many diseases are due
to the hyperactivity of protein kinases. Therefore, it makes sense to tackle
these diseases by modulating the protein kinases.
More than 500 protein kinases have
been identified in humans. For example, tyrosine kinase is an enzyme that helps
attach a phosphate group onto a tyrosine residue in a protein; it is important
in signal transduction and is implicated in the treatment of cancer.
Kinase modulators target a molecular
abnormality by modulating the activity of certain kinase. Kinase modulators
have been used in certain types of cancer. Examples of kinase modulators are
shown below.
© Jiajiu Shaw, 2019
Disclaimer: This blog is written solely for informational purposes. It does not constitute the practice of any medical, nursing or other medical professional health care advice, diagnosis, or treatment. All contents posted are extracted from the book, "SIDE EFFECTS OF CHEMOTHERAPY AND RADIOTHERAPY", prepared by Dr. Jiajiu Shaw, Dr. Frederick Valeriote, and Dr. Ben Chen.
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