The role of protein phosphorylation in human health and disease - Delivered on June 30th 2001 at the FEBS Meeting in Lisbon

The role of protein phosphorylation in human health and disease - Delivered on June 30th 2001 at the FEBS Meeting in Lisbon
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DOI:
10.1046/j.0014-2956.2001.02473.x
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发表时间:
2001-10-01
期刊:
EUROPEAN JOURNAL OF BIOCHEMISTRY
影响因子:
--
通讯作者:
Cohen, P
Cohen, P
中科院分区:
其他
文献类型:
--
作者:
Cohen, P

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蛋白质的可逆磷酸化调节细胞生命的几乎所有方面,而异常磷酸化是许多疾病的原因或结果。特别是蛋白激酶和磷酸酶的突变引起许多疾病,许多天然存在的毒素和病原体通过改变细胞内蛋白质的磷酸化状态发挥其作用。在这次演讲中,我提出了一个正在开发的蛋白激酶的治疗癌症和慢性炎症性疾病的特异性抑制剂的进展的概述,并描述了如何在我们的理解的特异性和调节一个特定的蛋白激酶(GSK3)的最新进展可能会促进药物的发展,以治疗糖尿病,不会有潜在的致癌。我还讨论了利用特定的蛋白激酶抑制剂的细胞信号的研究,并提出建议,为他们的有效使用细胞为基础的测定。
The reversible phosphorylation of proteins regulates almost all aspects of cell life, while abnormal phosphorylation is a cause or consequence of many diseases. Mutations in particular protein kinases and phosphatases gives rise to a number of disorders and many naturally occurring toxins and pathogens exert their effects by altering the phosphorylation states of intracellular proteins. In this lecture, I present an overview of the progress that is being made in developing specific inhibitors of protein kinases for the treatment of cancer and chronic inflammatory diseases and describe how recent advances in our understanding of the specificity and regulation of one particular protein kinase (GSK3) may facilitate the development of drugs to treat diabetes that would not have the potential to be oncogenic. I also discuss the exploitation of specific protein kinase inhibitors for the study of cell signalling and make recommendations for their effective use in cell-based assays.