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 …

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 …

PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
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 …

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 …

[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 …

An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
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

W Xiang, L Zhao, X Han, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
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 …

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 …

[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 …