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Research progress on pyruvate dehydrogenase kinase inhibitors
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Zuo-peng ZHANG, Ye ZHONG, Mao-sheng CHENG, Yang LIU*
Acta Pharmaceutica Sinica | 2020, 55(11) : 2549 - 2557
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Acta Pharmaceutica Sinica | 2020, 55(11): 2549-2557
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Research progress on pyruvate dehydrogenase kinase inhibitors
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Zuo-peng ZHANG, Ye ZHONG, Mao-sheng CHENG, Yang LIU*
Affiliations
  • Key Laboratory of Structure-Based Drug Design and Discovery(Ministry of Education), Shenyang Pharmaceutical University, Shenyang 110016, China
Published: 2020-11-12 doi: 10.16438/j.0513-4870.2020-0667
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Tumor cells can metabolize glucose through glycolysis to intermediates for biomacromolecule synthesis by inhibiting the activity of the pyruvate dehydrogenase complex (PDC) in mitochondria. In this process, pyruvate dehydrogenase kinases (PDKs) play a key role. The inhibition of the activity of PDKs can effectively block this metabolic pathway, activate mitochondrial oxidative metabolism, and induce tumor cell apoptosis. PDK inhibitors have become a research hotspot in medicinal chemistry, and novel structures targeting classical binding sites have been synthesized. In this paper, recent research progress on PDK inhibitors is reviewed to provide information on these latest entities and to explore their clinical applicability.

pyruvate dehydrogenase complex  /  pyruvate dehydrogenase kinase  /  binding site  /  glycolysis  /  oxidative metabolism
Zuo-peng ZHANG, Ye ZHONG, Mao-sheng CHENG, Yang LIU. Research progress on pyruvate dehydrogenase kinase inhibitors[J]. Acta Pharmaceutica Sinica, 2020 , 55 (11) : 2549 -2557 . DOI: 10.16438/j.0513-4870.2020-0667
Year 2020 volume 55 Issue 11
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doi: 10.16438/j.0513-4870.2020-0667
  • Receive Date:2020-04-30
  • Online Date:2026-01-23
  • Published:2020-11-12
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  • Received:2020-04-30
  • Revised:2020-06-10
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    Key Laboratory of Structure-Based Drug Design and Discovery(Ministry of Education), Shenyang Pharmaceutical University, Shenyang 110016, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

Genus
种数
Number of
species
占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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