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 …
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 …
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
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
E3 ligase ligand chemistries: from building blocks to protein degraders
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …
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 …
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 …
pathway has been associated with the pathogenesis of many autoimmune and inflammatory …
Applications of covalent chemistry in targeted protein degradation
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …
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 …
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
The technology known asPROTACs (PROteolysisTArgeting Chimeras) is a method of
protein degradation. Utilising bifunctional small molecules, the ubiquitin-proteosome system …
protein degradation. Utilising bifunctional small molecules, the ubiquitin-proteosome system …