Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy [PDF]
Journal of Hematology & Oncology, 2020 Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently ...
Xin Li, Yongcheng Song
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Proteolysis-Targeting Chimera (PROTAC): Is the Technology Looking at the Treatment of Brain Tumors? [PDF]
Frontiers in Cell and Developmental Biology, 2022 Post-translational modifications, such as ubiquitylation, need to be tightly controlled to guarantee the accurate localization and activity of proteins.
Ludovica Lospinoso Severini +4 more
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Proteolysis‐Targeting Chimera (PROTAC): Current Applications and Future Directions [PDF]
MedCommTargeted protein degradation (TPD) represents a paradigm shift in drug discovery, moving beyond traditional binding‐based inhibition toward active removal of disease‐driving proteins.
Gang Fan +9 more
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Proteolysis Targeting Chimera (PROTAC) for Macrophage Migration Inhibitory Factor (MIF) Has Anti-Proliferative Activity in Lung Cancer Cells [PDF]
Angewandte Chemie - International Edition, 2021 Macrophage migration inhibitory factor (MIF) is involved in protein-protein interactions that play key roles in inflammation and cancer. Current strategies to develop small molecule modulators of MIF functions are mainly restricted to the MIF tautomerase
Barbro N Melgert +2 more
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Targeted degradation of Influenza a virus nucleoprotein via aptamer-based PROTACs for antiviral therapy [PDF]
VirulenceInfluenza A virus (IAV) poses a serious threat to public health due to its high mutability and rapid transmissibility. The viral nucleoprotein (NP), a highly conserved and essential component, has emerged as an ideal target for antiviral therapies ...
Weiqiang Li +4 more
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Design, Synthesis and Biological Evaluation of α-Synuclein Proteolysis-Targeting Chimeras
Molecules, 2023 α-Synuclein aggregation under pathological conditions is one of the causes of related neurodegenerative diseases. PROTACs (proteolysis targeting chimeras) are bifunctional small molecules that induce a post-translational erasure of proteins via the ...
Tianzhi Wen +3 more
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Proteolysis targeting chimera (PROTAC)-driven antibody internalization of oncogenic cell surface receptors [PDF]
Communications BiologyAntibody-drug conjugates (ADCs) are increasingly used in clinic for multiple indications and may improve upon the activity of parental antibodies by delivering cytotoxic payloads into target cells.
Ezequiel J. Tolosa +9 more
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Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation [PDF]
Chemical Society Reviews, 2022 Yixin Wang, Weiping Tang, Quanyin Hu
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A lipid nanoparticle-based peptide-proteolysis-targeting chimera degrades BCL6 for diffuse large B-cell lymphoma treatment [PDF]
Discover OncologyB-cell lymphoma 6 (BCL6) is an attractive drug target for diffuse large B-cell lymphoma (DLBCL). This study aimed to create a lipid nanoparticle (LNP)-based peptide-proteolysis-targeting chimera (PROTAC), specifically BCL6-PROTAC, to develop effective ...
Shiwei Liu +11 more
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Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1 [PDF]
Acta Pharmaceutica Sinica B, 2020 Tinghong Ye, Yongmei Xie
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