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Controlling the Flow of Energy: Inhibition and Stimulation of the Creatine Transporter

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Creatine in its free and phosphorylated form plays an essential role for maintenance and distribution of ATP levels in tissues with high and fluctuating energy demands such as muscle, brain and heart. Alterations in the creatine concentration in these tissues produce marked functional changes. Creatine concentration is largely determined by a specific creatine transporter, a member of the Na+ dependent transporters family, that is localized on the cells' plasma membrane. This transporter is needed to carry creatine into the cells against a high concentration gradient. In recent years the mechanisms regulating the expression and the function of this transporter are being unraveled. Even if our knowledge of this matter is still limited, we have now tools for either stimulating or inhibiting this transporter, tools that may be relevant to several experimental and clinical conditions. This review will examine the data and the tools that are available in relation to the regulation and expression of the creatine transporter. Furthermore, we will briefly review the possible practical relevance of manipulating the creatine transporter activity.

Keywords: Creatine; SLC6A8; creatine transporter; inhibition; phosphocreatine; stimulation

Document Type: Research Article

Publication date: 2009-12-01

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  • Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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