Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery.

Abstract:

: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.

journal_name

Cell

journal_title

Cell

authors

Burslem GM,Crews CM

doi

10.1016/j.cell.2019.11.031

subject

Has Abstract

pub_date

2020-04-02 00:00:00

pages

102-114

issue

1

eissn

0092-8674

issn

1097-4172

pii

S0092-8674(19)31316-9

journal_volume

181

pub_type

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