Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents

Zhang Shao-Lin; Hu Xiaohui; Zhang Wen; Yao Huankai; Tam Kin Yip

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Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents

机译：用特别强调抗癌剂的药物化学丙酮酸脱氢酶激酶抑制剂的研制

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Many cancer cells demonstrate a high rate of glucose consumption via glycolysis to provide intermediates for macromolecule biosynthesis. To accomplish this metabolic change, the expression of pyruvate dehydrogenase kinases (PDKs) is rapidly increased in cancer cells. Inhibition of PDKs could promote the function of mitochondria by increasing the oxidative metabolism of pyruvate, resulting in the death of cancer cells. In this review, we provide an overview of the structural information available for PDKs and their connections to known therapeutic effects. We then describe the development of small molecule PDK inhibitors in medicinal chemistry with particular emphasis as anticancer agents. Finally, directions for further development of PDK inhibitors as potential anticancer agents are discussed.

机译：许多癌细胞通过糖酵解证明了高葡萄糖消耗，以提供用于大分子生物合成的中间体。为了实现这种代谢变化，丙酮酸脱氢酶激酶（PDK）的表达在癌细胞中迅速增加。通过增加丙酮酸的氧化代谢来促进PDK的抑制可以促进线粒体的功能，导致癌细胞死亡。在本次审查中，我们概述了可用于PDK的结构信息及其与已知治疗效果的关系。然后，我们描述了药物化学中小分子PDK抑制剂的发展，特别强调抗癌剂。最后，讨论了PDK抑制剂进一步发展的方向作为潜在的抗癌剂。

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《Drug discovery today》 |2015年第9期|共8页
作者
Zhang Shao-Lin; Hu Xiaohui; Zhang Wen; Yao Huankai; Tam Kin Yip;
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作者单位

Univ Macau Fac Hlth Sci Drug Dev Core Macau Peoples R China;

Univ Macau Fac Hlth Sci Drug Dev Core Macau Peoples R China;

Univ Macau Fac Hlth Sci Drug Dev Core Macau Peoples R China;

Univ Macau Fac Hlth Sci Drug Dev Core Macau Peoples R China;

Univ Macau Fac Hlth Sci Drug Dev Core Macau Peoples R China;

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正文语种 eng
中图分类药学;
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1. Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents [J] . Zhang Shao-Lin, Hu Xiaohui, Zhang Wen, Drug discovery today . 2015,第9期

机译：丙酮酸脱氢酶激酶抑制剂在药物化学中的发展，特别是作为抗癌药
2. Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents [J] . Shao-Lin Zhang, Xiaohui Hu, Wen Zhang, Drug discovery today . 2015,第5a12期

机译：用特别强调抗癌剂的药物化学丙酮酸脱氢酶激酶抑制剂的研制
3. Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents [J] . Shao-Lin Zhang, Xiaohui Hu, Wen Zhang, Drug discovery today . 2015,第2期

机译：用特别强调抗癌剂的药物化学丙酮酸脱氢酶激酶抑制剂的研制
4. DEVELOPMENT OF SIMULTANEOUS BIOLUMINESCENT ASSAY OF ACETATE KINASE AND PYRUVATE PHOSPHATE DIKINASE USING FIREFLY LUCIFERASE-LUCIFERIN REACTION [C] . KATSUTOSHI ITO, KAZUTO NAKAGAWA, SEIJI MURAKAMI, 12th Symposium on Bioluminescence and Chemiluminescence, Apr 5-9, 2002, Robinson College, University of Cambridge, UK . 2002

机译：全萤光酶-萤光素反应同时开发乙酸激酶和丙酮酸磷酸二激酶的生物发光分析
5. The role of NQO1 in the metabolism of benzoquinone ansamycin Hsp90 inhibitors and development of novel Hsp90 inhibitors as anticancer agents. [D] . Guo, Wenchang. 2007

机译：NQO1在苯醌安沙霉素Hsp90抑制剂的代谢中的作用以及新型Hsp90抑制剂作为抗癌剂的开发。
6. Diisopropylamine Dichloroacetate a Novel Pyruvate Dehydrogenase Kinase 4 Inhibitor as a Potential Therapeutic Agent for Metabolic Disorders and Multiorgan Failure in Severe Influenza [O] . Kazuhiko Yamane, Irene L. Indalao, Junji Chida, -1

机译：二异丙基胺二氯乙酸盐一种新的丙酮酸脱氢酶激酶4抑制剂作为严重流感中代谢紊乱和多器官衰竭的潜在治疗剂
7. Inhibition of pyruvate dehydrogenase kinase redirects NSCLC cell metabolism and counteracts development of resistance to epidermal growth factor receptor tyrosine kinase inhibitors [O] . Sissel Elisabeth Dyrstad, Maria Lie Lotsberg, Tuan Zea Tan, 2020

机译：丙酮酸脱氢酶激酶的抑制重定向NSCLC细胞代谢并抵消表皮生长因子受体酪氨酸激酶抑制剂的抗性

Development of pyruvate dehydrogenase kinase inhibitors in medicinal chemistry with particular emphasis as anticancer agents

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