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Controlling PROTACs with Light.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-06-17 , DOI: 10.1002/cmdc.202000249 Shreya Verma 1 , Debasish Manna 1
ChemMedChem ( IF 3.6 ) Pub Date : 2020-06-17 , DOI: 10.1002/cmdc.202000249 Shreya Verma 1 , Debasish Manna 1
Affiliation
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Proteolysis targeting chimeras, PROTACs, are emerging as a powerful strategy for exerting exogenous control over protein levels, allowing small molecules to exploit the ubiquitin–proteasome pathway for targeted protein degradation. This highlight focuses on the fusion of photochemistry with these bifunctional compounds, which has provided a novel pathway for spatiotemporally tuning the activation of PROTACs in the form of their photocaged and photoswitchable versions. Photocaged PROTACs consist of a hindered optolabile group that detaches only upon irradiation at a specific wavelength, releasing the active PROTAC. These modified PROTACs are inactive in the dark. Photoswitchable PROTACs are photoisomerizable molecules with azobenzene linkages that are active in either the cis or trans form and inactive in the other. The isomers interconvert upon irradiation with an appropriate wavelength of light and relax to the thermodynamically stable isomer in the dark or with another wavelength of light. Although photocaged PROTACs only permit activation control for protein degradation, photoswitching PROTACs offer reversible activation and deactivation by using suitable wavelengths of light.
中文翻译：
用光控制PROTAC。
靶向嵌合体（PROTAC）的蛋白水解正在成为一种强大的策略，可以对蛋白质水平进行外源控制，允许小分子利用泛素-蛋白酶体途径进行靶向蛋白质降解。该亮点集中在光化学与这些双功能化合物的融合上，这为时空调节PROTAC的光笼化和光开关形式提供了一条新途径。光笼PROTAC由受阻的光不稳定基团组成，该基团仅在以特定波长照射后才会脱离，释放出活性的PROTAC。这些修饰的PROTAC在黑暗中不起作用。可光转换的PROTAC是具有偶氮苯键的可光异构的分子，在顺式或反式中均具有活性形式和对方不活跃。异构体在适当波长的光照射下相互转化，并在黑暗或另一波长的光下松弛成热力学稳定的异构体。尽管光笼PROTAC仅允许激活控制以降解蛋白质，但光开关PROTAC通过使用合适的光波长提供可逆的激活和去激活。
更新日期：2020-07-20
中文翻译：
用光控制PROTAC。
靶向嵌合体（PROTAC）的蛋白水解正在成为一种强大的策略，可以对蛋白质水平进行外源控制，允许小分子利用泛素-蛋白酶体途径进行靶向蛋白质降解。该亮点集中在光化学与这些双功能化合物的融合上，这为时空调节PROTAC的光笼化和光开关形式提供了一条新途径。光笼PROTAC由受阻的光不稳定基团组成，该基团仅在以特定波长照射后才会脱离，释放出活性的PROTAC。这些修饰的PROTAC在黑暗中不起作用。可光转换的PROTAC是具有偶氮苯键的可光异构的分子，在顺式或反式中均具有活性形式和对方不活跃。异构体在适当波长的光照射下相互转化，并在黑暗或另一波长的光下松弛成热力学稳定的异构体。尽管光笼PROTAC仅允许激活控制以降解蛋白质，但光开关PROTAC通过使用合适的光波长提供可逆的激活和去激活。
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