The DOI matches its Crossref record; 41 of the 41 references it cites were found in a registry or an index.
Targeted protein degradation: elements of PROTAC design
Open accessAbstract
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the degradation of select proteins of interest (POIs) by hijacking the activity of E3 ubiquitin ligases for POI ubiquitination and subsequent degradation by the 26S proteasome. This hijacking mechanism has been used to degrade various types of disease-relevant POIs. In this review, we aim to highlight the recent advances in targeted protein degradation and describe the challenges that need to be addressed in order to efficiently develop potent PROTACs.
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Cites
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Self-citationHistone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders
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“Similarly, degradation of HDAC6, a class IIB Zn2+-dependent HDAC, was achieved using a PROTAC incorporating a hydroxamic-acid-based HDAC6 inhibitor and pomalidomide as its E3RE [81].”
BackgroundUbiquitin ligases: structure, function, and regulation
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Catalytic in vivo protein knockdown by small-molecule PROTACs
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Cited by
A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo
Bai, L., Zhou, H., Xu, R., Zhao, Y., Chinnaswamy, K., McEachern, D., Chen, J., Yang, C.-Y., Liu, Z., Wang, M., et al. (2019) · Cancer Cell · doi:10.1016/j.ccell.2019.10.002 · Cited by 652
Zhong, Q., Xiao, X., Qiu, Y., Xu, Z., Chen, C., Chong, B., Zhao, X., Hai, S., Li, S., An, Z., et al. (2023) · MedComm · doi:10.1002/mco2.261 · Cited by 442
Targeted Degradation of Oncogenic KRAS G12C by VHL-Recruiting PROTACs
Bond, M. J., Chu, L., Nalawansha, D. A., Li, K., & Crews, C. M. (2020) · ACS Central Science · doi:10.1021/acscentsci.0c00411 · Cited by 450
Self-citationAdvances in Targeting ‘Undruggable’ transcription Factors With Small Molecules
Henley, M. J., & Koehler, A. N. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00199-0 · Cited by 409
Current strategies for the design of PROTAC linkers: a critical review
Troup, R. I., Fallan, C., & Baud, M. G. J. (2020) · Exploration of Targeted Anti-tumor Therapy · doi:10.37349/etat.2020.00018 · Cited by 424
“Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules consisting of two ligands connected by a linker [1-5].”
Background
Metadata
- Authors
- Paiva, S.-L., & Crews, C. M.
- Venue
- Current Opinion in Chemical Biology
- Publisher
- Elsevier BV
- Published
- 2019-06
- Volume
- 50
- Pages
- 111-119
- ISSN
- 1367-5931 (ISSN-L)
- OpenAlex
- W2936661052
- Cited by
- 576
- References
- 41
- FWCI
- 4.76
- Type
- journal article
- Language
- en
- Open access
- green
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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