Protein degradation: a validated therapeutic strategy with exciting prospects

H Lebraud, TD Heightman - Essays in biochemistry, 2017 - portlandpress.com
In a time of unprecedented challenges in developing potent, selective and well-tolerated
protein inhibitors as therapeutics, drug hunters are increasingly seeking alternative …

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 …

A beginner's guide to PROTACs and targeted protein degradation

A Ciulli, N Trainor - The Biochemist, 2021 - portlandpress.com
Those with a keen interest in targeting proteins, from chemical biologists to drug hunters
alike, cannot help but take notice that a new type of molecule is making waves across this …

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 …

Targeted protein degradation by PROTACs

TK Neklesa, JD Winkler, CM Crews - Pharmacology & therapeutics, 2017 - Elsevier
Targeted protein degradation using the PROTAC technology is emerging as a novel
therapeutic method to address diseases driven by the aberrant expression of a disease …

Protac-induced protein degradation in drug discovery: breaking the rules or just making new ones?

I Churcher - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted protein degradation, using bifunctional small molecules (Protacs) to remove
specific proteins from within cells, has emerged as a novel drug discovery strategy with the …

Targeted protein degradation: current and future challenges

A Hanzl, GE Winter - Current opinion in chemical biology, 2020 - Elsevier
Traditional approaches in the development of small-molecule drugs typically aim to inhibit
the biochemical activity of functional protein domains. In contrast, targeted protein …

[HTML][HTML] The rise and rise of protein degradation: opportunities and challenges ahead

SJ Hughes, A Testa, N Thompson, I Churcher - Drug Discovery Today, 2021 - Elsevier
The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …

[HTML][HTML] 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 …

Clinical translation of targeted protein degraders

NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …