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1
A MedChem toolbox for cereblon-directed PROTACs.
Medchemcomm. 2019 May 28;10(6):1037-1041. doi: 10.1039/c9md00185a. eCollection 2019 Jun 1.
2
Recent advancements in the discovery of cereblon-based protease-targeted chimeras with potential for therapeutic intervention.
Future Med Chem. 2022 Oct;14(19):1403-1416. doi: 10.4155/fmc-2022-0149. Epub 2022 Sep 1.
3
Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead.
RSC Chem Biol. 2023 Aug 31;4(11):906-912. doi: 10.1039/d3cb00103b. eCollection 2023 Nov 1.
4
Expansion of targeted degradation by Gilteritinib-Warheaded PROTACs to ALK fusion proteins.
Bioorg Chem. 2024 Apr;145:107204. doi: 10.1016/j.bioorg.2024.107204. Epub 2024 Feb 14.
5
Current strategies for the design of PROTAC linkers: a critical review.
Explor Target Antitumor Ther. 2020;1(5):273-312. doi: 10.37349/etat.2020.00018. Epub 2020 Oct 30.
6
CRBN ligand expansion for hematopoietic prostaglandin D synthase (H-PGDS) targeting PROTAC design and their in vitro ADME profiles.
Bioorg Med Chem. 2023 Apr 15;84:117259. doi: 10.1016/j.bmc.2023.117259. Epub 2023 Mar 30.
7
E3 ligase ligand optimization of Clinical PROTACs.
Front Chem. 2023 Jan 17;11:1098331. doi: 10.3389/fchem.2023.1098331. eCollection 2023.
8
Effective degradation of EGFR mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems.
Eur J Med Chem. 2021 Jun 5;218:113328. doi: 10.1016/j.ejmech.2021.113328. Epub 2021 Mar 7.
9
E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points.
Front Chem. 2021 Jul 5;9:707317. doi: 10.3389/fchem.2021.707317. eCollection 2021.

引用本文的文献

1
FDA-approved kinase inhibitors in PROTAC design, development and synthesis.
J Enzyme Inhib Med Chem. 2025 Dec;40(1):2542357. doi: 10.1080/14756366.2025.2542357. Epub 2025 Aug 12.
2
Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs.
Commun Chem. 2025 Jul 29;8(1):218. doi: 10.1038/s42004-025-01598-9.
3
Application of a bivalent "click" approach to target tyrosyl-DNA phosphodiesterase 1 (TDP1).
RSC Med Chem. 2025 Feb 21;16(5):1969-1985. doi: 10.1039/d4md00824c. eCollection 2025 May 22.
4
Use of Aldehyde-Alkyne-Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers.
ACS Med Chem Lett. 2025 Jan 25;16(2):278-284. doi: 10.1021/acsmedchemlett.4c00531. eCollection 2025 Feb 13.
5
Investigating protein degradability through site-specific ubiquitin ligase recruitment.
RSC Chem Biol. 2024 Dec 13;6(2):240-248. doi: 10.1039/d4cb00273c. eCollection 2025 Feb 5.
6
Investigating Protein Degradability through Site-Specific Ubiquitin Ligase Recruitment.
bioRxiv. 2024 Nov 12:2024.11.11.623099. doi: 10.1101/2024.11.11.623099.
7
Targeted degradation of zDHHC-PATs decreases substrate S-palmitoylation.
PLoS One. 2024 Mar 21;19(3):e0299665. doi: 10.1371/journal.pone.0299665. eCollection 2024.
8
Targeted Protein Degradation of Histone Deacetylases by Hydrophobically Tagged Inhibitors.
ACS Med Chem Lett. 2023 Nov 15;14(12):1863-1868. doi: 10.1021/acsmedchemlett.3c00468. eCollection 2023 Dec 14.
9
Identification of non-conventional small molecule degraders and stabilizers of squalene synthase.
Chem Sci. 2023 Oct 18;14(45):12973-12983. doi: 10.1039/d3sc04064j. eCollection 2023 Nov 22.
10
Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs.
J Med Chem. 2023 Nov 9;66(21):14513-14543. doi: 10.1021/acs.jmedchem.3c00851. Epub 2023 Oct 30.

本文引用的文献

1
Chemical Ligand Space of Cereblon.
ACS Omega. 2018 Sep 14;3(9):11163-11171. doi: 10.1021/acsomega.8b00959. eCollection 2018 Sep 30.
2
4
A chemical approach for global protein knockdown from mice to non-human primates.
Cell Discov. 2019 Feb 5;5:10. doi: 10.1038/s41421-018-0079-1. eCollection 2019.
5
PROTAC-mediated crosstalk between E3 ligases.
Chem Commun (Camb). 2019 Feb 5;55(12):1821-1824. doi: 10.1039/c8cc09541h.
6
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase.
Nat Commun. 2019 Jan 10;10(1):131. doi: 10.1038/s41467-018-08027-7.
7
Bruton tyrosine kinase degradation as a therapeutic strategy for cancer.
Blood. 2019 Feb 28;133(9):952-961. doi: 10.1182/blood-2018-07-862953. Epub 2018 Dec 13.
9
Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule.
Chem Commun (Camb). 2019 Jan 2;55(3):369-372. doi: 10.1039/c8cc07813k.
10
Selective Degradation of Polo-like Kinase 1 by a Hydrophobically Tagged Inhibitor of the Polo-Box Domain.
Angew Chem Int Ed Engl. 2018 Dec 21;57(52):17043-17047. doi: 10.1002/anie.201809640. Epub 2018 Nov 27.

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