Opportunities and challenges of protein-based targeted protein degradation

L Dassama, F Shen - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …

[HTML][HTML] Targeted protein degradation directly engaging lysosomes or proteasomes

J Kim, I Byun, H Joh, HJ Kim, MJ Lee - Chemical Society Reviews, 2024 - pubs.rsc.org
Targeted protein degradation (TPD) has been established as a viable alternative to
attenuate the function of a specific protein of interest in both biological and clinical contexts …

Beyond canonical PROTAC: biological targeted protein degradation (bioTPD)

H Wang, R Zhou, F Xu, K Yang, L Zheng… - Biomaterials …, 2023 - spj.science.org
Targeted protein degradation (TPD) is an emerging therapeutic strategy with the potential to
modulate disease-associated proteins that have previously been considered undruggable …

Extracellular targeted protein degradation: an emerging modality for drug discovery

JA Wells, K Kumru - Nature Reviews Drug Discovery, 2024 - nature.com
Targeted protein degradation (TPD) has emerged in the past decade as a major new drug
modality to remove intracellular proteins with bispecific small molecules that recruit the …

Biologics-based degraders—an expanding toolkit for targeted-protein degradation

D VanDyke, JD Taylor, KJ Kaeo, J Hunt… - Current opinion in …, 2022 - Elsevier
Highlights•Targeted-protein degradation supports fundamental discovery and drug
development.•Biologics-based degraders target intracellular, extracellular, and membrane …

[HTML][HTML] Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

Advancement of targeted protein degradation strategies as therapeutics for undruggable disease targets

MP Kannan, S Sreeraman, CS Somala… - Future Medicinal …, 2023 - Taylor & Francis
Targeted protein degradation (TPD) aids in developing novel bifunctional small-molecule
degraders and eliminates proteins of interest. The TPD approach shows promising results in …

[HTML][HTML] Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …

PROTACs: an emerging targeting technique for protein degradation in drug discovery

S Gu, D Cui, X Chen, X Xiong, Y Zhao - BioEssays, 2018 - Wiley Online Library
Proteolysis‐targeting chimeric molecules (PROTACs) represent an emerging technique that
is receiving much attention for therapeutic intervention. The mechanism is based on the …

[HTML][HTML] Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …