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Advanced Search. Register Login. International Journal of Molecular Medicine. This article is mentioned in:. Introduction Protein phosphorylation is one of the most common and important post-translational modifications PTMs 1 , 2.
Protein kinases contain hydrophobic catalytic and regulatory spines and collateral shell residues that are required to assemble the active enzyme.
There are two general kinds of conformational changes associated with most protein kinases. The first conformational change involves the formation of an intact regulatory spine to form an active enzyme. The second conformational change occurs in active kinases as they toggle between open and closed conformations during their catalytic cycles. Because mutations and dysregulation of protein kinases play causal roles in human disease, this family of enzymes has become one of the most important drug targets over the past two decades.
Imatinib was approved by the United States FDA for the treatment of chronic myelogenous leukemia in ; this small molecule inhibits the BCR-Abl protein kinase oncoprotein that results from the formation of the Philadelphia chromosome. More than two dozen other orally effective mechanism-based small molecule protein kinase inhibitors have been subsequently approved by the FDA. These drugs bind to the ATP-binding site of their target enzymes and extend into nearby hydrophobic pockets.
Most of these protein kinase inhibitors prolong survival in cancer patients only weeks or months longer than standard cytotoxic therapies. The article by R. Lee et al. The review article by A. Slupe et al. It is well documented that aberrant regulation of protein kinases and phosphatases contributes to the development of diseases.
Protein kinases and phosphatases are regulated by protein-protein interactions, binding of ligands, and reversible or irreversible covalent modifications such as phosphorylation and limited proteolysis.
In this special issue, the article by I. Nakashima et al. Dick et al. Among the cellular processes in which protein kinases and phosphatases are involved, this issue contains review articles detailing how protein kinases and phosphatases regulate cell cycle, mediate toll-like receptor signaling, and control of cell fate and potassium channel and intracellular calcium concentration in renal tubule epithelial cells. This issue contains three review articles on the function, catalytic mechanism, and regulation of this important group of phosphatases.
Heung-Chin Cheng Robert Z. This is an open access article distributed under the Creative Commons Attribution License , which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Article of the Year Award: Outstanding research contributions of , as selected by our Chief Editors. Read the winning articles. Special Issues. Article Sections On this page References Copyright. Heung-Chin Cheng , 1 Robert Z. Received 03 Nov Accepted 03 Nov Published 13 Dec References J. Ubersax and J.
Holt, B. Tuch, J. Villen, A. Johnson, S. Gygi, and D. Serber and J. Johnson and D. View at: Google Scholar J. Hurley, A. Dean, P. Thorsness, D. Koshland Jr. Hurley, P. Thorsness, V. Ramalingam, N. Helmers, D.
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