[HTML][HTML] Proteolysis-targeting chimeras (PROTACs) in cancer therapy
X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
[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 …
[HTML][HTML] Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation
RP Wurz, H Rui, K Dellamaggiore… - Nature …, 2023 - nature.com
Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
Accelerated rational PROTAC design via deep learning and molecular simulations
Proteolysis-targeting chimeras (PROTACs) have emerged as effective tools to selectively
degrade disease-related proteins by using the ubiquitin-proteasome system. Developing …
degrade disease-related proteins by using the ubiquitin-proteasome system. Developing …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
emerged as new promising pharmacological modalities and the first PROTAC drug …
Current advances and development strategies of orally bioavailable PROTACs
S Zeng, Y Ye, H Xia, J Min, J Xu, Z Wang, Y Pan… - European Journal of …, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …
potential to extend drug space not target to traditional molecules. In the last half decade, we …
Microneedle patch delivery of PROTACs for anti-cancer therapy
Proteolysis-targeting chimera (PROTAC) is an emerging technique for degrading disease-
related proteins. However, the current PROTACs suffer from inadequate solubility and lack …
related proteins. However, the current PROTACs suffer from inadequate solubility and lack …
Targeted protein degradation: advances, challenges, and prospects for computational methods
The therapeutic approach of targeted protein degradation (TPD) is gaining momentum due
to its potentially superior effects compared with protein inhibition. Recent advancements in …
to its potentially superior effects compared with protein inhibition. Recent advancements in …
A versatile and sustainable multicomponent platform for the synthesis of protein degraders: proof-of-concept application to BRD4-degrading PROTACs
IP Bhela, A Ranza, FC Balestrero… - Journal of Medicinal …, 2022 - ACS Publications
The use of small molecules to induce targeted protein degradation is increasingly growing in
the drug discovery landscape, and protein degraders have progressed rapidly through the …
the drug discovery landscape, and protein degraders have progressed rapidly through the …
[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 …