[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 …
used in clinical settings for decades. However, many cancer-related targets are proteins …
[HTML][HTML] Targeted protein degradation in cancers: Orthodox PROTACs and beyond
Targeted protein degradation (TPD) is emerging as a strategy to overcome the limitations of
traditional small-molecule inhibitors. Proteolysis-targeting chimera (PROTAC) technology …
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 …
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 …
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 …
potential advantages over traditional occupancy-based inhibitors in terms of dosing, side …
Advancing targeted protein degradation for cancer therapy
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 …
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
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 (TPD) has changed the landscape of drug development …
Targeted protein degradation technology and nanomedicine: powerful allies against cancer
Targeted protein degradation (TPD) is an emerging therapeutic strategy with the potential of
targeting undruggable pathogenic proteins. After the first proof‐of‐concept proteolysis …
targeting undruggable pathogenic proteins. After the first proof‐of‐concept proteolysis …
[HTML][HTML] PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
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 …
protein inhibitors as therapeutics, drug hunters are increasingly seeking alternative …