The DOI matches its Crossref record; 70 of the 70 references it cites were found in a registry or an index.
Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)
Open accessAbstract
Here we report the development of a proteolysis targeting chimera (PROTAC) based on the combination of the unique features of the sirtuin rearranging ligands (SirReals) as highly potent and isotype-selective Sirt2 inhibitors with thalidomide, a bona fide cereblon ligand. For the first time, we report the formation of a PROTAC by Cu(I)-catalyzed cycloaddition of a thalidomide-derived azide to an alkynylated inhibitor. This thalidomide-derived azide as well as the highly versatile linking strategy can be readily adapted to alkynylated ligands of other targets. In HeLa cells, our SirReal-based PROTAC induced isotype-selective Sirt2 degradation that results in the hyperacetylation of the microtubule network coupled with enhanced process elongation. Thus, our SirReal-based PROTAC is the first example of a probe that is able to chemically induce the degradation of an epigenetic eraser protein.
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Cited by
PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future
Pettersson, M., & Crews, C. M. (2019) · Drug Discovery Today: Technologies · doi:10.1016/j.ddtec.2019.01.002 · Cited by 800
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
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A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo
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PROTACs: great opportunities for academia and industry
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PROTACs: An Emerging Therapeutic Modality in Precision Medicine
Nalawansha, D. A., & Crews, C. M. (2020) · Cell Chemical Biology · doi:10.1016/j.chembiol.2020.07.020 · Cited by 490
Metadata
- Authors
- Schiedel, M., Herp, D., Hammelmann, S., Swyter, S., Lehotzky, A., Robaa, D., Oláh, J., Ovádi, J., Sippl, W., & Jung, M.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2017-04-17
- Volume
- 61
- Issue
- 2
- Pages
- 482-491
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2604930678
- Cited by
- 263
- References
- 70
- FWCI
- 10.97
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). https://app.cochat.ai/papers/10.1021/acs.jmedchem.6b01872
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- Schiedel, M., Herp, D., Hammelmann, S., Swyter, S., Lehotzky, A., Robaa, D., Oláh, J., Ovádi, J., Sippl, W., & Jung, M. (2018). Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.6b01872
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