Results 11 to 20 of about 7,362 (230)
mRNA PROTACs: engineering PROTACs for high‐efficiency targeted protein degradation
MedCommProteolysis‐targeting chimeras (PROTACs) are essential bifunctional molecules that target proteins of interest (POIs) for degradation by cellular ubiquitination machinery.
Xiaoqi Xue +10 more
doaj +3 more sources
Drug Discovery Today, 2021 Targeting protein-protein interactions (PPI) is a key focus in the development of new and emerging small-molecule therapeutics. Shallow interacting surfaces can render PPI targeting notoriously difficult. This leaves many therapeutically captivating targets 'undruggable'.
Gregory R. Hughes +3 more
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PROTAC-DB: an online database of PROTACs [PDF]
Nucleic Acids Research, 2020 Abstract Proteolysis-targeting chimeras (PROTACs), which selectively degrade targeted proteins by the ubiquitin-proteasome system, have emerged as a novel therapeutic technology with potential advantages over traditional inhibition strategies.
Gaoqi Weng +9 more
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Pharmaceutics, 2022 Targeting selective estrogen subtype receptors through typical medicinal chemistry approaches is based on occupancy-driven pharmacology. In occupancy-driven pharmacology, molecules are developed in order to inhibit the protein of interest (POI), and their popularity is based on their virtue of faster kinetics.
Arvind Negi +2 more
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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
openaire +2 more sources
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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An overview of PROTACs: a promising drug discovery paradigm
Molecular Biomedicine, 2022 Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target proteins by hijacking the ubiquitin–proteasome system.
Zi Liu +10 more
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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
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Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
Journal of Hematology & Oncology, 2020 Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI).
Yonghan He +10 more
doaj +1 more source
Pharmaceutics, 2023 Proteolysis-targeting chimeras (PROTACs) are rapidly emerging as a potential therapeutic strategy for cancer therapy by inducing the degradation of tumor-overexpressing oncogenic proteins.
Yujeong Moon +3 more
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