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Protein degradation as an innovative strategy in drug discovery
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Qi-dong YOU1, 2, *, Meng-chen LU1, 2, Zheng-yu JIANG1, 2
Acta Pharmaceutica Sinica | 2017, 52(12) : 1777 - 1782
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Acta Pharmaceutica Sinica | 2017, 52(12): 1777-1782
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Protein degradation as an innovative strategy in drug discovery
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Qi-dong YOU1, 2, *, Meng-chen LU1, 2, Zheng-yu JIANG1, 2
Affiliations
  • 1. Jiang Su Key Laboratory of Drug Design and Optimization, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
  • 2. Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
Published: 2017-12-15 doi: 10.16438/j.0513-4870.2017-0659
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The success rate of mechanism-based drug discovery depends on the drug targets. With the rapid development of genomics and proteomics, a lot of nonenzymic proteins have been identified as potential drug targets. However, these nonenzymic proteins cannot be regulated by occupying the active site, which were recognized as undruggable targets. Direct regulation of the concentration of these proteins in cells by the innate ubiquitin-proteasome is a potential approach to target these proteins. The ubiquitination of target protein by E3 ligase is the key step for ubiquitin-proteasome mediated protein degradation. Proteolysis targeting chimeras (PROTACs) can facilitate the assembly of complex that consists of the target protein and E3 ligase. The target protein will be ubiquitinated, leading to the degradation by proteasome. This type of regulation mechanism can expand the scope of potential drug targets, and the development of PROTACs may be an innovative strategy in drug discovery.

ubiquitin E3 ligase  /  protein degradation  /  proteolysis targeting chimeras
Qi-dong YOU, Meng-chen LU, Zheng-yu JIANG. Protein degradation as an innovative strategy in drug discovery[J]. Acta Pharmaceutica Sinica, 2017 , 52 (12) : 1777 -1782 . DOI: 10.16438/j.0513-4870.2017-0659
Year 2017 volume 52 Issue 12
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Article Info
doi: 10.16438/j.0513-4870.2017-0659
  • Receive Date:2017-07-07
  • Online Date:2026-01-14
  • Published:2017-12-15
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  • Received:2017-07-07
  • Revised:2017-10-07
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    1. Jiang Su Key Laboratory of Drug Design and Optimization, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
    2. Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, 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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