[HTML][HTML] Targeted protein degrader development for cancer: advances, challenges, and opportunities

Y Fang, S Wang, S Han, Y Zhao, C Yu, H Liu… - Trends in pharmacological …, 2023 - cell.com
Anticancer-targeted therapies inhibit various kinases implicated in cancer and have been
used in clinical settings for decades. However, many cancer-related targets are proteins …

[HTML][HTML] Targeted protein degradation in cancers: Orthodox PROTACs and beyond

J Li, X Chen, A Lu, C Liang - The Innovation, 2023 - cell.com
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …

[HTML][HTML] Targeted protein degradation: clinical advances in the field of oncology

AKAA Salama, MV Trkulja, E Casanova… - International Journal of …, 2022 - mdpi.com
The field of targeted protein degradation (TPD) is a rapidly developing therapeutic modality
with the promise to tame disease-relevant proteins in ways that are difficult or impossible to …

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 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 …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

[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 …

Targeted protein degradation technology and nanomedicine: powerful allies against cancer

JY Lin, HJ Liu, Y Wu, JM Jin, YD Zhou, H Zhang… - Small, 2023 - Wiley Online Library
Targeted protein degradation (TPD) is an emerging therapeutic strategy with the potential of
targeting undruggable pathogenic proteins. After the first proof‐of‐concept proteolysis …

[HTML][HTML] PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

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 …