[HTML][HTML] PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
[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 …
c-Myc-targeting PROTAC based on a TNA-DNA bivalent binder for combination therapy of triple-negative breast cancer
X Li, Z Zhang, F Gao, Y Ma, D Wei, Z Lu… - Journal of the …, 2023 - ACS Publications
Triple-negative breast cancer (TNBC) is highly aggressive with a poor clinical prognosis and
no targeted therapy. The c-Myc protein is a master transcription factor and a potential …
no targeted therapy. The c-Myc protein is a master transcription factor and a potential …
Enriching proteolysis targeting chimeras with a second modality: When two are better than one
A Salerno, F Seghetti, J Caciolla, E Uliassi… - Journal of Medicinal …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC)-mediated protein degradation has prompted a
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …
Novel approaches to targeted protein degradation technologies in drug discovery
Y Xue, AA Bolinger, J Zhou - Expert opinion on drug discovery, 2023 - Taylor & Francis
Introduction Target protein degradation (TPD) provides a novel therapeutic modality, other
than inhibition, through the direct depletion of target proteins. Two primary human protein …
than inhibition, through the direct depletion of target proteins. Two primary human protein …
Proteolysis-targeting chimeras in biotherapeutics: Current trends and future applications
The success of inhibitor-based therapeutics is largely constrained by the acquisition of
therapeutic resistance, which is partially driven by the undruggable proteome. The …
therapeutic resistance, which is partially driven by the undruggable proteome. The …
Exploitation of proximity-mediated effects in drug discovery: an update of recent research highlights in perturbing pathogenic proteins and correlated issues
C Zhao, H Wang, W Zhan, X Lv… - Journal of Medicinal …, 2023 - ACS Publications
The utilization of proximity-mediated effects to perturb pathogenic proteins of interest (POIs)
has emerged as a powerful strategic alternative to conventional drug design approaches …
has emerged as a powerful strategic alternative to conventional drug design approaches …
Discovery of the GSH responsive “Y-PROTACs” targeting ALK and CDK4/6 as a potential treatment for cancer
S Wang, D Luo, C Pu, X Ma, H Zhang, Z Feng… - European Journal of …, 2023 - Elsevier
Combination of different molecular target inhibitors is an available method to improve the
therapeutic effect on tumors. Herein, to achieve both tumor cell targeting and ALK …
therapeutic effect on tumors. Herein, to achieve both tumor cell targeting and ALK …
Repurposing AS1411 for constructing ANM-PROTACs
X Fu, J Li, X Chen, H Chen, Z Wang, F Qiu, D Xie… - Cell Chemical …, 2024 - cell.com
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
two ligands joined by a linker, enabling them to simultaneously bind with an E3 ligase and a …
two ligands joined by a linker, enabling them to simultaneously bind with an E3 ligase and a …
Development of decoy oligonucleotide-warheaded chimeric molecules targeting STAT3
Proteolysis-targeting chimera (PROTAC) technology is a disruptive innovation in the drug
development community, and over 20 PROTAC molecules are currently under clinical …
development community, and over 20 PROTAC molecules are currently under clinical …