The PROTAC technology in drug development

• Published in: Cell biochemistry and function Vol. 37; no. 1; pp. 21 - 30
• Main Authors: Zou, Yutian, Ma, Danhui, Wang, Yinyin
• Format: Journal Article
• Language: English
• Published: England Wiley Subscription Services, Inc 01.01.2019; John Wiley and Sons Inc
• Subjects: Biodegradation; cancer; Drug development; Drug Development - methods; Humans; New technology; PROTAC; Proteasome Endopeptidase Complex - metabolism; protein degradation; Proteins; Proteolysis; Recombinant Fusion Proteins - metabolism; Review; small molecule; Ubiquitin; Ubiquitin-protein ligase; Ubiquitin-Protein Ligases - metabolism; Ubiquitination; drug development; small molecule; cancer; PROTAC; protein degradation
• ISSN: 0263-6484; 1099-0844; 1099-0844
• DOI: 10.1002/cbf.3369

Currently, a new technology termed PROTAC, proteolysis targeting chimera, has been developed for inducing the protein degradation by a targeting molecule. This technology takes advantage of a moiety of targeted protein and a moiety of recognizing E3 ubiquitin ligase and produces a hybrid molecule to specifically knock down a targeted protein. During the first decade, three pedigreed groups worked on the development of this technology. To date, this technology has been extended by different groups, aiming to develop new drugs against different diseases including cancers. This review summarizes the contributions of the groups for the development of PROTAC. Significance of the study This review summarized the development of the PROTAC technology for readers and also presented the author's opinions on the application of the technology in tumor therapy.