[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 …

[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 …

[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 …

Accelerated rational PROTAC design via deep learning and molecular simulations

S Zheng, Y Tan, Z Wang, C Li, Z Zhang… - Nature Machine …, 2022 - nature.com
Proteolysis-targeting chimeras (PROTACs) have emerged as effective tools to selectively
degrade disease-related proteins by using the ubiquitin-proteasome system. Developing …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
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 …

Microneedle patch delivery of PROTACs for anti-cancer therapy

X Cheng, S Hu, K Cheng - ACS nano, 2023 - ACS Publications
Proteolysis-targeting chimera (PROTAC) is an emerging technique for degrading disease-
related proteins. However, the current PROTACs suffer from inadequate solubility and lack …

Targeted protein degradation: advances, challenges, and prospects for computational methods

B Mostofian, HJ Martin, A Razavi, S Patel… - Journal of Chemical …, 2023 - ACS Publications
The therapeutic approach of targeted protein degradation (TPD) is gaining momentum due
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 …

[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 …