Results 1 to 10 of about 280 (69)
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 ...
Jiyan Pang, Tianzhi Wen
exaly +3 more sources
Molecular Strategies to Target Protein Aggregation in Huntington’s Disease
Frontiers in Molecular Biosciences, 2021 Huntington’s disease (HD) is a neurodegenerative disorder caused by the aggregation of the mutant huntingtin (mHTT) protein in nerve cells. mHTT self-aggregates to form soluble oligomers and insoluble fibrils, which interfere in a number of key cellular ...
Olga D. Jarosińska +3 more
doaj +1 more source
The clinical advances of proteolysis targeting chimeras in oncology
Exploration of Targeted Anti-tumor Therapy, 2021 Proteolysis targeting chimeras (PROTACs) are a class of small molecules designed to target proteins for degradation. Their novel and unique modes of action provide PROTACs with the potential for their application in the management of both solid and ...
Hao Xie +3 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
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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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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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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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Proceedings, 2019 Proteolysis targeting chimera molecules (PROTACS) are heterobifunctional small moleculesdesigned to induce intracellular protein degradation [...]
Carles Galdeano
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Current Status of Oligonucleotide-Based Protein Degraders
Pharmaceutics, 2023 Transcription factors (TFs) and RNA-binding proteins (RBPs) have long been considered undruggable, mainly because they lack ligand-binding sites and are equipped with flat and narrow protein surfaces. Protein-specific oligonucleotides have been harnessed
Po-Chang Shih +3 more
doaj +1 more source
PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
Exploration of Targeted Anti-tumor Therapy, 2020 BCL-XL is an anti-apoptotic protein that plays an important role in tumorigenesis, metastasis, and intrinsic or therapy-induced cancer drug resistance.
Peiyi Zhang +5 more
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