Abstract
Ribosomal S6 kinase (RSK) is a family of serine/threonine kinases that has been identified as a promising anti-cancer target. While a number of protein kinase inhibitors that have potent activity against other serine/threonine kinases were shown to also inactivate RSK, there is keen interest in the three different inhibitor chemotypes that were shown to be RSK specific, since these compounds have tremendous utility as chemical probes in elucidating the biochemistry of the RSK signaling cascade and unraveling the molecular basis of cancer. Because each compound may have therapeutic potential, the nonspecific kinase inhibitors as well as the RSK specific inhibitors will be discussed.
Keywords: Serine/threonine kinase, inhibitor, RSK specific
Anti-Cancer Agents in Medicinal Chemistry
Title: Targeting RSK: An Overview of Small Molecule Inhibitors
Volume: 8 Issue: 7
Author(s): Tam Luong Nguyen
Affiliation:
Keywords: Serine/threonine kinase, inhibitor, RSK specific
Abstract: Ribosomal S6 kinase (RSK) is a family of serine/threonine kinases that has been identified as a promising anti-cancer target. While a number of protein kinase inhibitors that have potent activity against other serine/threonine kinases were shown to also inactivate RSK, there is keen interest in the three different inhibitor chemotypes that were shown to be RSK specific, since these compounds have tremendous utility as chemical probes in elucidating the biochemistry of the RSK signaling cascade and unraveling the molecular basis of cancer. Because each compound may have therapeutic potential, the nonspecific kinase inhibitors as well as the RSK specific inhibitors will be discussed.
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Cite this article as:
Nguyen Luong Tam, Targeting RSK: An Overview of Small Molecule Inhibitors, Anti-Cancer Agents in Medicinal Chemistry 2008; 8 (7) . https://dx.doi.org/10.2174/187152008785914770
DOI https://dx.doi.org/10.2174/187152008785914770 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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