59
Views
6
CrossRef citations to date
0
Altmetric
Review

Selective tyrosine kinase inhibitors

&
Pages 287-297 | Published online: 24 Feb 2005
 

Abstract

The tyrosine specific protein kinases (TK) are a subgroup of the largest known gene family, the kinases. Latest estimates suggest that there are over 2000 kinases encoded in the human genome [1]. TKs catalyse the transfer of phosphate to the phenolic hydroxyl of tyrosine residues in substrate proteins, consequently modifying the target protein properties. By working in concert with tyrosine phosphatases, which drive the reverse process, the TKs provide a switching system resulting in the transduction of signals from cell surface receptor to the nucleus. Inappropriate activation of TKs can lead to abnormal, dysregulated cellular proliferation and many of the known oncogenes are kinases. Naturally, there has been great interest in TKs as potential molecular targets for developing drugs for the treatment of cancer and results from the first clinical trials are now being published. Preclinical research is also focused on other therapeutic applications of TK inhibitors. This review concentrates on TK inhibitors which are either already in the clinic or likely to enter Phase I studies in the near future.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.