蛋白酶靶向嵌合体（PROTAC）：小分子药物发现中的一种范式转变方法。 - Suppr

Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery.

作者信息

Wang Pingyuan, Zhou Jia

机构信息

Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas 77555, United States.

出版信息

Curr Top Med Chem. 2018;18(16):1354-1356. doi: 10.2174/1568026618666181010101922.

DOI:10.2174/1568026618666181010101922

PMID:30306871

Abstract

摘要

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Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery.

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Future Med Chem. 2020 May;12(10):915-938. doi: 10.4155/fmc-2019-0340. Epub 2020 Apr 9.

Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.

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PROTAC-DB: an online database of PROTACs.

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Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery.

Curr Top Med Chem. 2018;18(16):1354-1356. doi: 10.2174/1568026618666181010101922.

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges.

Eur J Med Chem. 2021 Jan 15;210:112981. doi: 10.1016/j.ejmech.2020.112981. Epub 2020 Oct 31.

Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands.

J Med Chem. 2019 Dec 26;62(24):11218-11231. doi: 10.1021/acs.jmedchem.9b01393. Epub 2019 Dec 5.

New therapies on the horizon: Targeted protein degradation in neuroscience.

Cell Chem Biol. 2024 Sep 19;31(9):1688-1698. doi: 10.1016/j.chembiol.2024.08.010.

Protein degradation technology: a strategic paradigm shift in drug discovery.

J Hematol Oncol. 2021 Sep 6;14(1):138. doi: 10.1186/s13045-021-01146-7.

Targeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs.

Adv Exp Med Biol. 2020;1217:317-347. doi: 10.1007/978-981-15-1025-0_19.

Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC).

Bioorg Chem. 2022 Feb;119:105508. doi: 10.1016/j.bioorg.2021.105508. Epub 2021 Nov 29.

Small-molecule PROTACs: novel agents for cancer therapy.

Future Med Chem. 2020 May;12(10):915-938. doi: 10.4155/fmc-2019-0340. Epub 2020 Apr 9.

Discovery of thalidomide-based PROTAC small molecules as the highly efficient SHP2 degraders.

Eur J Med Chem. 2021 Jun 5;218:113341. doi: 10.1016/j.ejmech.2021.113341. Epub 2021 Mar 11.

PROTAC-DB: an online database of PROTACs.

Nucleic Acids Res. 2021 Jan 8;49(D1):D1381-D1387. doi: 10.1093/nar/gkaa807.

引用本文的文献

An updated patent review of BRD4 degraders.

Expert Opin Ther Pat. 2024 Oct;34(10):929-951. doi: 10.1080/13543776.2024.2400166. Epub 2024 Sep 4.

Lessons learnt from broad-spectrum coronavirus antiviral drug discovery.

Expert Opin Drug Discov. 2024 Sep;19(9):1023-1041. doi: 10.1080/17460441.2024.2385598. Epub 2024 Jul 30.

Potential therapeutic targets of the JAK2/STAT3 signaling pathway in triple-negative breast cancer.

Front Oncol. 2024 Apr 18;14:1381251. doi: 10.3389/fonc.2024.1381251. eCollection 2024.

Targeting EED as a key PRC2 complex mediator toward novel epigenetic therapeutics.

Drug Discov Today. 2024 Jun;29(6):103986. doi: 10.1016/j.drudis.2024.103986. Epub 2024 Apr 18.

Orphan GPR52 as an emerging neurotherapeutic target.

Drug Discov Today. 2024 Apr;29(4):103922. doi: 10.1016/j.drudis.2024.103922. Epub 2024 Feb 20.

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Signal Transduct Target Ther. 2023 Nov 6;8(1):420. doi: 10.1038/s41392-023-01647-6.

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Drug Discov Today. 2023 Nov;28(11):103774. doi: 10.1016/j.drudis.2023.103774. Epub 2023 Sep 19.

Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2).

J Med Chem. 2023 Aug 24;66(16):10991-11026. doi: 10.1021/acs.jmedchem.3c00948. Epub 2023 Aug 14.

Novel approaches to targeted protein degradation technologies in drug discovery.

Expert Opin Drug Discov. 2023 Apr;18(4):467-483. doi: 10.1080/17460441.2023.2187777. Epub 2023 Mar 9.

Bromodomain-containing protein 4 (BRD4): a key player in inflammatory bowel disease and potential to inspire epigenetic therapeutics.

Expert Opin Ther Targets. 2023 Jan;27(1):1-7. doi: 10.1080/14728222.2023.2175317. Epub 2023 Feb 7.

Proteolysis Targeting Chimera (PROTAC): A Paradigm-Shifting Approach in Small Molecule Drug Discovery.

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