What is a Kinase Inhibitor?

A protein kinase inhibitor is a type of enzyme inhibitor that can block the action of protein kinases. Protein kinases add a phosphate group to a protein in a process called phosphorylation, which can turn a protein on or off and therefore affect its level of activity and function.

Protein kinase inhibitors can be subdivided according to the amino acid on a protein that they add the phosphate to (e.g serine, threonine or tyrosine) in order to inhibit phosphorylation of that amino acid. Kinases mostly act on both serine and threonine, but tyrosine kinase acts on tyrosine only and some dual-specificity kinases act on all three of these amino acid residues. Some protein kinases also phosphorylate other amino acids, such as histidine kinases that act on histidine residues.

Phosphorylation is often a required step in the growth of some cancers and inflammatory disorders, meaning inhibition of the enzymes that trigger phosphorylation provides an approach to treating such diseases.

One example of a drug being used in this way is the tyrosine kinase inhibitor dasatinib, which is used as an anticancer therapy in several forms of leukemia. Another agent currently being tested in clinical trials for polycystic kidney disease is PLX5568.

Tyrosine kinase inhibitors are particularly important agents because these high-affinity cell surface receptors play a critical role in the progression of many cancers.

Tyrosine kinases are involved in various cell functions including cell signalling, cell growth and cell division. In some forms of cancer, these enzymes are present in high levels or overactive and inhibiting them can prevent the proliferation of cancer cells. Tyrosine kinase inhibitors therefore provide an important form of targeted therapy in the fight against cancer.

Further Reading

Last Updated: Jul 20, 2023

Dr. Ananya Mandal

Written by

Dr. Ananya Mandal

Dr. Ananya Mandal is a doctor by profession, lecturer by vocation and a medical writer by passion. She specialized in Clinical Pharmacology after her bachelor's (MBBS). For her, health communication is not just writing complicated reviews for professionals but making medical knowledge understandable and available to the general public as well.

Citations

Please use one of the following formats to cite this article in your essay, paper or report:

  • APA

    Mandal, Ananya. (2023, July 20). What is a Kinase Inhibitor?. News-Medical. Retrieved on November 06, 2024 from https://www.news-medical.net/life-sciences/What-is-a-Kinase-Inhibitor.aspx.

  • MLA

    Mandal, Ananya. "What is a Kinase Inhibitor?". News-Medical. 06 November 2024. <https://www.news-medical.net/life-sciences/What-is-a-Kinase-Inhibitor.aspx>.

  • Chicago

    Mandal, Ananya. "What is a Kinase Inhibitor?". News-Medical. https://www.news-medical.net/life-sciences/What-is-a-Kinase-Inhibitor.aspx. (accessed November 06, 2024).

  • Harvard

    Mandal, Ananya. 2023. What is a Kinase Inhibitor?. News-Medical, viewed 06 November 2024, https://www.news-medical.net/life-sciences/What-is-a-Kinase-Inhibitor.aspx.

Comments

The opinions expressed here are the views of the writer and do not necessarily reflect the views and opinions of News Medical.
Post a new comment
Post

While we only use edited and approved content for Azthena answers, it may on occasions provide incorrect responses. Please confirm any data provided with the related suppliers or authors. We do not provide medical advice, if you search for medical information you must always consult a medical professional before acting on any information provided.

Your questions, but not your email details will be shared with OpenAI and retained for 30 days in accordance with their privacy principles.

Please do not ask questions that use sensitive or confidential information.

Read the full Terms & Conditions.