Results 21 to 30 of about 14,786 (290)
Advanced ScienceProteolysis targeting chimeras (PROTACs) have emerged as a promising strategy for drug discovery and exploring protein functions, offering a revolutionary therapeutic modality.
Ke‐Nian Yan +7 more
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PROTAC-Splitter: a machine learning framework for automated identification of PROTAC substructures. [PDF]
J CheminformAbstract Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules composed of an E3 ligase ligand, a linker, and a warhead targeting a protein of interest. Despite their modular structure, accurately identifying and annotating these components in PROTACs is challenging and typically relies on ...
Ribes S +6 more
europepmc +4 more sources
PROTAC-DB 2.0: an updated database of PROTACs
Nucleic Acids Research, 2022 AbstractProteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system to selectively induce targeted protein degradation, represent an emerging therapeutic technology with the potential to modulate traditional undruggable targets.
Gaoqi Weng +9 more
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PROTACs in gastrointestinal cancers
Molecular Therapy - Oncolytics, 2022 Proteolysis targeting chimera (PROTAC) presents a powerful strategy for targeted protein degradation (TPD). The heterobifunctional PROTAC molecule consists of an E3 ligase ligand covalently linked to a protein of interest (POI) via a linker. PROTAC can induce ubiquitinated proteasomal degradation of proteins by hijacking the ubiquitin-proteasome ...
Yu Chen +19 more
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PROTACs: Walking through hematological malignancies
Frontiers in Pharmacology, 2023 Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that uses the proteasome ubiquitin system to target proteins of interest and promote their degradation with remarkable selectivity.
Lara J. Bou Malhab +5 more
doaj +1 more source
Advanced Science, 2023 PROteolysis TArgeting Chimeras (PROTACs) are an emerging class of promising therapeutic modalities that selectively degrade intracellular proteins of interest by hijacking the ubiquitin‐proteasome system.
Hai‐Jun Liu +13 more
doaj +1 more source
Light-Controllable PROTACs for Temporospatial Control of Protein Degradation
Frontiers in Cell and Developmental Biology, 2021 PROteolysis-TArgeting Chimeras (PROTACs) is an emerging and promising approach to target intracellular proteins for ubiquitination-mediated degradation, including those so-called undruggable protein targets, such as transcriptional factors and scaffold ...
Jing Liu, Yunhua Peng, Wenyi Wei
doaj +1 more source
Nano-Proteolysis Targeting Chimeras (Nano-PROTACs) in Cancer Therapy
International Journal of NanomedicineYue Song,1,* Qing-Qing Dong,2,* Yi-Ke Ni,3 Xiao-Ling Xu,3 Chao-Xiang Chen,3 Wei Chen2 1Stomatology Hospital, School of Stomatology, Zhejiang University School of Medicine, Hangzhou, Zhejiang Province, 310003, People’s Republic of China; 2ICU ...
Song Y +5 more
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PROTAC-Design-Evaluator (PRODE): An Advanced Method for In-Silico PROTAC Design
ACS Omega, 2023 Abstract PROTAC (proteolysis-targeting chimeras) is a rapidly evolving technology to target undruggable targets. The mechanism by which this happens is when a bifunctional molecule binds to a target protein and also brings in proximity an E3 ubiquitin ligase to trigger ubiquitination and degradation of the target protein.
Ben Geoffrey A S +4 more
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Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation [PDF]
, 2003 The proteome contains hundreds of proteins that in theory could be excellent therapeutic targets for the treatment of human diseases. However, many of these proteins are from functional classes that have never been validated as viable candidates for the ...
Crews, Craig M. +6 more
core +1 more source