Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery | Zendy

George M. Burslem | Zendy; Craig M. Crews | Zendy

AI Assistant Blog Pricing

Home ZAIA Blog

Open Access

Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery

Author(s) -

George M. Burslem,

Craig M. Crews

Publication year - 2020

Publication title -

cell

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 26.304

H-Index - 776

eISSN - 1097-4172

pISSN - 0092-8674

DOI - 10.1016/j.cell.2019.11.031

Subject(s) - biology , drug discovery , computational biology , proteolysis , protein degradation , proteasome , ubiquitin , workflow , bioinformatics , microbiology and biotechnology , genetics , biochemistry , computer science , gene , enzyme , database

New biological tools provide new techniques to probe fundamental biological processes. Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which are capable of modulating protein concentrations at a post-translational level by co-opting the ubiquitin-proteasome system. We describe the PROTAC technology and its application to drug discovery and provide examples where PROTACs have enabled novel biological insights. Furthermore, we provide a workflow for PROTAC development and use and discuss the benefits and issues associated with PROTACs. Finally, we compare PROTAC-mediated protein-level modulation with other technologies, such as RNAi and genome editing.

The content you want is available to Zendy users.

Already have an account? Click here to sign in.

Having issues? You can contact us here

Accelerating Research