Assessing different E3 ligases for small molecule induced protein ubiquitination and degradation
P Ottis, M Toure, PM Cromm, E Ko… - ACS chemical …, 2017 - ACS Publications
Proteolysis targeting chimera (PROTAC) technology, the recruitment of E3 ubiquitin ligases
to induce the degradation of a protein target, is rapidly impacting chemical biology, as well …
to induce the degradation of a protein target, is rapidly impacting chemical biology, as well …
Stimuli‐Responsive PROTACs for Controlled Protein Degradation
K An, X Deng, H Chi, Y Zhang, Y Li… - Angewandte Chemie …, 2023 - Wiley Online Library
Abstract Proteolysis Targeting Chimeras (PROTACs) represent a promising therapeutic
modality to address undruggable and resistant issues in drug discovery. However, potential …
modality to address undruggable and resistant issues in drug discovery. However, potential …
[HTML][HTML] Clinical considerations for the design of PROTACs in cancer
C Nieto-Jiménez, EC Morafraile, C Alonso-Moreno… - Molecular Cancer, 2022 - Springer
Degradation of targeted proteins using proteolysis targeting chimeras (PROTACs) has
gained momentum. A PROTAC is a bifunctional molecule that consists of three parts: a …
gained momentum. A PROTAC is a bifunctional molecule that consists of three parts: a …
Blocking non-enzymatic functions by PROTAC-mediated targeted protein degradation
D Sun, J Zhang, G Dong, S He… - Journal of Medicinal …, 2022 - ACS Publications
The non-enzymatic functions of target proteins play key roles in the regulation of various cell
signaling pathways and are closely related to numerous human diseases. However …
signaling pathways and are closely related to numerous human diseases. However …
[HTML][HTML] The peptide PROTAC modality: a novel strategy for targeted protein ubiquitination
J Jin, Y Wu, J Chen, Y Shen, L Zhang, H Zhang… - Theranostics, 2020 - ncbi.nlm.nih.gov
Despite dramatic advances in drug discovery over the decades, effective therapeutic
strategies for cancers treatment are still in urgent demands. PROteolysis TArgeting Chimera …
strategies for cancers treatment are still in urgent demands. PROteolysis TArgeting Chimera …
Antibody–PROTAC conjugates enable HER2-dependent targeted protein degradation of BRD4
M Maneiro, N Forte, MM Shchepinova… - ACS chemical …, 2020 - ACS Publications
Targeting protein degradation with Proteolysis-Targeting Chimeras (PROTACs) is an area of
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
bioPROTACs as versatile modulators of intracellular therapeutic targets including proliferating cell nuclear antigen (PCNA)
S Lim, R Khoo, KM Peh, J Teo… - Proceedings of the …, 2020 - National Acad Sciences
Targeted degradation approaches such as proteolysis targeting chimeras (PROTACs) offer
new ways to address disease through tackling challenging targets and with greater potency …
new ways to address disease through tackling challenging targets and with greater potency …
PROTAC: A promising technology for cancer treatment
X Zhou, R Dong, JY Zhang, X Zheng, LP Sun - European journal of …, 2020 - Elsevier
Proteolysis-targeting chimeric molecules (PROTACs), which attract much more attention
today, may be a potential way to treat cancer. PROTACs are made up of ligands of target …
today, may be a potential way to treat cancer. PROTACs are made up of ligands of target …
PROTACs to address the challenges facing small molecule inhibitors
P Martín-Acosta, X Xiao - European journal of medicinal chemistry, 2021 - Elsevier
Small molecule inhibitors of proteins represent important medicines and critical chemical
tools to investigate the biology of the target proteins. Advances in various-omics …
tools to investigate the biology of the target proteins. Advances in various-omics …
[HTML][HTML] Lipid-mediated intracellular delivery of recombinant bioPROTACs for the rapid degradation of undruggable proteins
Recently, targeted degradation has emerged as a powerful therapeutic modality. Relying on
“event-driven” pharmacology, proteolysis targeting chimeras (PROTACs) can degrade …
“event-driven” pharmacology, proteolysis targeting chimeras (PROTACs) can degrade …