Targeting RSK: An Overview of Small Molecule Inhibitors
Targeting RSK: An Overview of Small Molecule Inhibitors
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DOI：
10.2174/187152008785914770
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发表时间：
2008-10-01
影响因子：
2.8
通讯作者：
Nguyen, Tam Luong
中科院分区：
文献类型：
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作者：
Nguyen, Tam Luong
核糖体S6激酶（RSK）是一个丝氨酸/苏氨酸激酶家族，已被确定为有前途的抗癌靶点。虽然许多对其他丝氨酸/苏氨酸激酶具有有效活性的蛋白激酶抑制剂也显示出抑制RSK，但人们对显示为RSK特异性的三种不同抑制剂化学型非常感兴趣，因为这些化合物作为化学探针在阐明RSK信号级联的生物化学和揭示癌症的分子基础方面具有巨大的实用性。由于每种化合物都可能具有治疗潜力，因此将讨论非特异性激酶抑制剂以及RSK特异性抑制剂。
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.