Protein degraders enter the clinic—a new approach to cancer therapy
D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
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 …
PROTAC: an effective targeted protein degradation strategy for cancer therapy
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …
degradation tool developed in recent years that can ubiquitinate the target proteins through …
Proteolysis-targeting chimeras as therapeutics and tools for biological discovery
GM Burslem, CM Crews - Cell, 2020 - cell.com
New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …
Revisiting the grammar of Tau aggregation and pathology formation: how new insights from brain pathology are shaping how we study and target Tauopathies
G Limorenko, HA Lashuel - Chemical Society Reviews, 2022 - pubs.rsc.org
Converging evidence continues to point towards Tau aggregation and pathology formation
as central events in the pathogenesis of Alzheimer's disease and other Tauopathies …
as central events in the pathogenesis of Alzheimer's disease and other Tauopathies …
[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review
RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
An overview of PROTACs: a promising drug discovery paradigm
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
Discovery of ARD-2585 as an exceptionally potent and orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
We report herein the discovery of exceptionally potent and orally bioavailable PROTAC AR
degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC50 …
degraders with ARD-2585 being the most promising compound. ARD-2585 achieves DC50 …
PROTAC technology: opportunities and challenges
H Gao, X Sun, Y Rao - ACS medicinal chemistry letters, 2020 - ACS Publications
PROTACs-induced targeted protein degradation has emerged as a novel therapeutic
strategy in drug development and attracted the favor of academic institutions, large …
strategy in drug development and attracted the favor of academic institutions, large …
[HTML][HTML] Degradation of proteins by PROTACs and other strategies
Y Wang, X Jiang, F Feng, W Liu, H Sun - Acta Pharmaceutica Sinica B, 2020 - Elsevier
Blocking the biological functions of scaffold proteins and aggregated proteins is a
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …