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Synfacts 2020; 16(05): 0591
DOI: 10.1055/s-0040-1707493
DOI: 10.1055/s-0040-1707493
Chemistry in Medicine and Biology
PHOTACs Enable Optical Control of Protein Degradation
Reynders M,
Matsuura BS,
Bérouti M,
Simoneschi D,
Marzio A,
Pagano M.
*
Trauner D.
* New York University, USA
PHOTACs Enable Optical Control of Protein Degradation.
Sci. Adv. 2020;
6
DOI: 10.1126/sciadv.aay5064.
PHOTACs Enable Optical Control of Protein Degradation.
Sci. Adv. 2020;
6
DOI: 10.1126/sciadv.aay5064.
Further Information
Publication History
Publication Date:
20 April 2020 (online)
Significance
PROTACs (PROteolysis TArgeting Chimeras) have emerged as a new modality in pharmacology (Sakamoto et al. PNAS 2001, 98, 8554), but their catalytic mechanism of action poses risks. PHOTACs (PHOtochemically TArgeting Chimeras) can be spatiotemporally controlled for precise and reversible switching between active and inactive states using light.
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Comment
Based on a photoswitchable analog of the cereblon ligand thalidomide, this approach provides a general method to turn PROTACs into PHOTACs, which are active only upon irradiation. The authors use this strategy for the targeted degradation of BRD2/3/4 and FKBP12.
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