PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1

Y Tao, D Remillard, EV Vinogradova… - Journal of the …, 2022 - ACS Publications
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

Clinical considerations for the design of PROTACs in cancer

C Nieto-Jiménez, EC Morafraile, C Alonso-Moreno… - Molecular Cancer, 2022 - Springer
Degradation of targeted proteins using proteolysis targeting chimeras (PROTACs) has
gained momentum. A PROTAC is a bifunctional molecule that consists of three parts: a …

Novel CRBN-recruiting proteolysis-targeting chimeras as degraders of stimulator of interferon genes with in vivo anti-inflammatory efficacy

J Liu, L Yuan, Y Ruan, B Deng, Z Yang… - Journal of medicinal …, 2022 - ACS Publications
The activation of the cyclic GMP-AMP synthase-stimulator of interferon gene (STING)
pathway has been associated with the pathogenesis of many autoimmune and inflammatory …

Applications of covalent chemistry in targeted protein degradation

D Lu, X Yu, H Lin, R Cheng, EY Monroy, X Qi… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …

Site-specific labeling of endogenous proteins using CoLDR chemistry

RN Reddi, A Rogel, E Resnick, R Gabizon… - Journal of the …, 2021 - ACS Publications
Chemical modifications of native proteins can affect their stability, activity, interactions,
localization, and more. However, there are few nongenetic methods for the installation of …

Unlocking the potential of PROTACs: A comprehensive review of protein degradation strategies in disease therapy

RP Bhole, PR Kute, RV Chikhale, CG Bonde, A Pant… - Bioorganic …, 2023 - Elsevier
The technology known asPROTACs (PROteolysisTArgeting Chimeras) is a method of
protein degradation. Utilising bifunctional small molecules, the ubiquitin-proteosome system …