[HTML][HTML] Proteomic approaches advancing targeted protein degradation

G Sathe, GP Sapkota - Trends in pharmacological sciences, 2023 - cell.com
Targeted protein degradation (TPD) is an emerging modality for research and therapeutics.
Most TPD approaches harness cellular ubiquitin-dependent proteolytic pathways …

[HTML][HTML] The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation

KM Riching, EA Caine, M Urh, DL Daniels - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …

[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 …

Targeted protein degradation: from mechanisms to clinic

JM Tsai, RP Nowak, BL Ebert, ES Fischer - Nature Reviews Molecular …, 2024 - nature.com
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

[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 …

Targeted protein degradation in drug development: Recent advances and future challenges

J Song, M Hu, J Zhou, S Xie, T Li, Y Li - European Journal of Medicinal …, 2023 - Elsevier
Targeted protein degradation (TPD) has emerged as a promising therapeutic approach with
potential advantages over traditional occupancy-based inhibitors in terms of dosing, side …

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 …

Critical assessment of targeted protein degradation as a research tool and pharmacological modality

M Kostic, LH Jones - Trends in pharmacological sciences, 2020 - cell.com
Small molecules continue to dominate drug discovery because of their ease of use, lower
cost of manufacturing, and access to intracellular targets. However, despite these …

[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 …