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Research progress and medicinal chemistry strategies of URAT1 inhibitors
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Xiao-yu SHI, Tong ZHAO, Jian ZHANG, Rui-peng LIANG, Zhi-jiao ZHANG, Xin-yong LIU*, Peng ZHAN*
Acta Pharmaceutica Sinica | 2022, 57(10) : 2960 - 2971
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Acta Pharmaceutica Sinica | 2022, 57(10): 2960-2971
Special Reports Ⅰ: New Targets, New Strategies for Drug Discovery and Advances in Antiviral Drug Research
Research progress and medicinal chemistry strategies of URAT1 inhibitors
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Xiao-yu SHI, Tong ZHAO, Jian ZHANG, Rui-peng LIANG, Zhi-jiao ZHANG, Xin-yong LIU*, Peng ZHAN*
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  • Key laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China
Published: 2022-10-12 doi: 10.16438/j.0513-4870.2022-0573
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The urate transporter 1 (URAT1) which controls urate reabsorption is a membrane transporter in the apical membrane of human renal proximal tubule epithelial cells. It was found that about 90% of patients suffer from hyperuricemia due to insufficient uric acid excretion. Therefore, the development of URAT1 inhibitors that can reduce the level of serum uric acid in vivo by enhancing renal urate excretion has been a hot spot in seeking anti-gout drugs in recent years. In this article, the representative URAT1 inhibitors with uric acid-lowering or anti-gout effects are reviewed, and related medicinal chemical strategies are analyzed, hoping to provide valuable insights into the discovery of new URAT1 inhibitors.

uric acid  /  hyperuricemia  /  gout  /  lesinurad  /  URAT1 inhibitor
Xiao-yu SHI, Tong ZHAO, Jian ZHANG, Rui-peng LIANG, Zhi-jiao ZHANG, Xin-yong LIU, Peng ZHAN. Research progress and medicinal chemistry strategies of URAT1 inhibitors[J]. Acta Pharmaceutica Sinica, 2022 , 57 (10) : 2960 -2971 . DOI: 10.16438/j.0513-4870.2022-0573
Year 2022 volume 57 Issue 10
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doi: 10.16438/j.0513-4870.2022-0573
  • Receive Date:2022-05-11
  • Online Date:2025-12-24
  • Published:2022-10-12
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  • Received:2022-05-11
  • Revised:2022-06-01
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    Key laboratory of Chemical Biology (Ministry of Education), Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, 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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