Proteolysis Targeting Chimera Degraders of the METTL3–14 m6A‑RNA Methyltransferase [PDF]
JACS AuFrancesco Errani +9 more
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Molecules, 2022 Viral infections pose a persistent threat to human health. The relentless epidemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has become a global health problem, with millions of infections and fatalities so far.
Shujing Xu +7 more
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Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
Nature Communications, 2022 SMARCA2 has been identified as a synthetic lethal target in SMARCA4 mutated tumors, however, homology between the two has hindered the development of selective SMARCA2 inhibitors.
Jennifer Cantley +28 more
doaj +1 more source
Proteolysis Targeting Chimeras (PROTACs)
ACS Pharmacology and Translational Science, 2022 Targeted protein degradation (TPD) is a promising therapeutic modality to modulate protein levels and its application promises to reduce the "undruggable"proteome. Among TPD strategies, Proteolysis TArgeting Chimera (PROTAC) technology has shown a tremendous potential with attractive advantages when compared to the inhibition of the same target.
Ruffilli, Camilla +5 more
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Proteolysis targeting chimeras (PROTACs) in cancer therapy [PDF]
Journal of Experimental & Clinical Cancer Research, 2020 AbstractExploitation of the protein degradation machinery as a therapeutic strategy to degrade oncogenic proteins is experiencing revolutionary advances with the development of proteolysis targeting chimeras (PROTACs). PROTACs are heterobifunctional structures consisting of a ligand that binds a protein to be degraded and a ligand for an E3 ubiquitin ...
Alberto Ocaña, Atanasio Pandiella
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Photopharmacology of Proteolysis-Targeting Chimeras: A New Frontier for Drug Discovery
Frontiers in Chemistry, 2021 Photopharmacology is an emerging field that uses light to precisely control drug activity. This strategy promises to improve drug specificity for reducing off-target effects.
Shenxin Zeng +7 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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Frontiers in Oncology, 2023 Enhancer of zeste homolog 2 (EZH2) and Bruton’s tyrosine kinase (BTK) are both key factors involved in the development and progression of hematological malignancies.
Yurim Jeong +7 more
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Assays and Technologies for Developing Proteolysis Targeting Chimera Degraders [PDF]
Future Medicinal Chemistry, 2020 Targeted protein degradation by small-molecule degraders represents an emerging mode of action in drug discovery. Proteolysis targeting chimeras (PROTACs) are small molecules that can recruit an E3 ligase and a protein of interest (POI) into proximity, leading to induced ubiquitination and degradation of the POI by the proteasome system.
Xingui Liu +5 more
openaire +2 more sources
Inhibition of bromodomain and extra-terminal (BET) proteins increases NKG2D ligand MICA expression and sensitivity to NK cell-mediated cytotoxicity in multiple myeloma cells. role of cMYC-IRF4-miR-125b interplay [PDF]
, 2016 Background: Anticancer immune responses may contribute to the control of tumors after conventional chemotherapy and different observations have indicated that chemotherapeutic agents can induce immune responses resulting in cancer cell death and immune ...
Abruzzese, MARIA PIA +13 more
core +15 more sources