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The application of small molecule PROTAC in researches of different targets
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Yuan WANG1, 2, Jing LONG3, Qi CHANG1, Wei-wen HU4, Gao-yun HU1, Qian-bin LI1, *
Acta Pharmaceutica Sinica | 2020, 55(3) : 446 - 452
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Acta Pharmaceutica Sinica | 2020, 55(3): 446-452
• Reviews •
The application of small molecule PROTAC in researches of different targets
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Yuan WANG1, 2, Jing LONG3, Qi CHANG1, Wei-wen HU4, Gao-yun HU1, Qian-bin LI1, *
Affiliations
  • 1. Department of Medicinal Chemistry, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410012, China
  • 2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
  • 3. The Department of Dermatology, Xiangya Hospital, Central South University, Changsha 410012, China
  • 4. Pharmaceutical Department, Yunnan Provincial Hospital of Traditional Chinese Medicine, Kunming 650021, China
Published: 2020-03-12 doi: 10.16438/j.0513-4870.2019-0924
Outline
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The protein proteolysis-targeting chimeras (PROTAC) are a kind of bifunctional compound that can recruit target proteins and degrade the enzyme of target proteins. The mechanism of PROTAC is using the ubiquitin-proteasome pathway to degrade target protein specifically. Because of its potential to target non-proprietary proteins and to play roles in drug resistance, PROTAC has attracted wide attention. This review summarizes the application of small molecule PROTAC in previous studies of different targets, such as nuclear proteins, membrane proteins and cytoplasmic proteins.

PROTAC  /  drug resistance  /  nuclear protein  /  membrane protein  /  cytoplasmic protein
Yuan WANG, Jing LONG, Qi CHANG, Wei-wen HU, Gao-yun HU, Qian-bin LI. The application of small molecule PROTAC in researches of different targets[J]. Acta Pharmaceutica Sinica, 2020 , 55 (3) : 446 -452 . DOI: 10.16438/j.0513-4870.2019-0924
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Article Info
doi: 10.16438/j.0513-4870.2019-0924
  • Receive Date：2019-11-20
  • Online Date：2026-01-20
  • Published：2020-03-12
Article Data
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History
  • Received：2019-11-20
  • Revised：2019-12-17
Funding
Affiliations
    1. Department of Medicinal Chemistry, Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410012, China
    2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
    3. The Department of Dermatology, Xiangya Hospital, Central South University, Changsha 410012, China
    4. Pharmaceutical Department, Yunnan Provincial Hospital of Traditional Chinese Medicine, Kunming 650021, China
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