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Research progress in controllable proteolysis targeting chimeras
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Yi MOU1, Shuai WEN1, Yan WANG1, Zheng-yu JIANG2, *
Acta Pharmaceutica Sinica | 2023, 58(8) : 2193 - 2202
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Acta Pharmaceutica Sinica | 2023, 58(8): 2193-2202
Research progress in controllable proteolysis targeting chimeras
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Yi MOU1, Shuai WEN1, Yan WANG1, Zheng-yu JIANG2, *
Affiliations
  • 1. College of Pharmacy and Chemistry & Chemical Engineering, Taizhou University, Taizhou 225300, China
  • 2. Jiangsu Key Laboratory of Drug Design and Optimization, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
Published: 2023-08-12 doi: 10.16438/j.0513-4870.2023-0553
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Proteolysis targeting chimeras (PROTACs) is an innovative technique in targeted protein degradation. PROTACs is a heterobifunctional molecule which can bind to the E3 ligase and target protein to form a ubiquitination complex, resulting in the ubiquitin-proteasome system dependent degradation of target protein. PROTACs has been regarded as the promising method in drug discovery campaign, for its high commonality, potent degradation activity and unique selectivity profile. However, the catalytic mechanism also induces the uncontrollable protein degradation risk. Controllable PROTACs contain the responsive element in the molecular entity. In certain conditions, the element can be triggered to activate or terminate the degradation event. In this review, we will briefly summarize the strategies in controllable PROTACs and describe the representative examples according to the responsive mechanism. We hope this review could provide some insight into the further development of controllable PROTACs.

proteolysis targeting chimeras  /  targeted protein degradation  /  controllable proteolysis targeting chimeras
Yi MOU, Shuai WEN, Yan WANG, Zheng-yu JIANG. Research progress in controllable proteolysis targeting chimeras[J]. Acta Pharmaceutica Sinica, 2023 , 58 (8) : 2193 -2202 . DOI: 10.16438/j.0513-4870.2023-0553
Year 2023 volume 58 Issue 8
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doi: 10.16438/j.0513-4870.2023-0553
  • Receive Date:2023-05-01
  • Online Date:2025-11-21
  • Published:2023-08-12
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  • Received:2023-05-01
  • Revised:2023-07-13
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    1. College of Pharmacy and Chemistry & Chemical Engineering, Taizhou University, Taizhou 225300, China
    2. Jiangsu Key Laboratory of Drug Design and Optimization, 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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