Azo-PROTAC: Novel Light-Controlled Small-Molecule Tool for Protein Knockdown

• Published in: Journal of medicinal chemistry Vol. 63; no. 9; pp. 4644 - 4654
• Main Authors: Jin, Yu-Hui, Lu, Meng-Chen, Wang, Yan, Shan, Wen-Xin, Wang, Xuan-Yu, You, Qi-Dong, Jiang, Zheng-Yu
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 14.05.2020; Amer Chemical Soc
• Subjects: Chemistry, Medicinal; Life Sciences & Biomedicine; Pharmacology & Pharmacy; Science & Technology; OPTICAL CONTROL; SPATIOTEMPORAL CONTROL; DESIGN; GLUTAMATE; PHOTOCHROMIC AGONIST; IN-VIVO; DEGRADATION; RECEPTOR; PROTEOLYSIS; PROTEASOME INHIBITORS

Reversibly altering endogenous protein levels are persistent issues. Herein, we designed photoswitchable azobenzene-proteolysis targeting chimeras (Azo-PROTACs) by including azobenzene moieties between ligands for the E3 ligase and the protein of interest. Azo-PROTACs are light-controlled small-mole...