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 …
[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 …
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] 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 …
[PDF][PDF] 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 degrader development for cancer: advances, challenges, and opportunities
Y Fang, S Wang, S Han, Y Zhao, C Yu, H Liu… - Trends in …, 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] The rise and rise of protein degradation: opportunities and challenges ahead
The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …
Transforming targeted cancer therapy with PROTACs: A forward-looking perspective
Small-molecule targeted protein degraders have in recent years made a great impact on the
strategies of many industry and academic cancer research endeavours. We seek here to …
strategies of many industry and academic cancer research endeavours. We seek here to …
[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
Targeted protein degradation: expanding the toolbox
M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …