Results 11 to 20 of about 464,369 (258)
Gluing Proteins for Targeted Degradation [PDF]
Cancer Cell, 2021 Targeted protein degradation is an emerging technology for drug development. An article published in Nature reported a novel mechanism of targeted protein degradation triggered by small-molecule-induced polymerization of the oncogenic transcription factor BCL6.
Mikihiko, Naito, Shigeo, Murata
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Targeting proteins for degradation [PDF]
Nature Chemical Biology, 2009 Protein degradation plays a central role in many cellular functions. Misfolded and damaged proteins are removed from the cell to avoid toxicity. The concentrations of regulatory proteins are adjusted by degradation at the appropriate time. Both foreign and native proteins are digested into small peptides as part of the adaptive immune response.
Erin K, Schrader +2 more
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Targeting Protein Kinases Degradation by PROTACs [PDF]
Frontiers in Chemistry, 2021 Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development. However, traditional kinase inhibitors binding to catalytic or allosteric sites are associated with significant challenges.
Fei Yu +3 more
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mBio, 2022 The human pathogen Pseudomonas aeruginosa (Pa) is one of the most frequent and severe causes of nosocomial infection. This organism is also a major cause of airway infections in people with cystic fibrosis (CF). Pa is known to have a remarkable metabolic
Stephen K. Dolan +7 more
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Proteolysis-Targeting Chimeras (PROTACs) in Cancer Therapy: Present and Future
Molecules, 2022 The PROteolysis TArgeting Chimeras (PROTACs) is an innovative technique for the selective degradation of target proteins via the ubiquitin–proteasome system.
Rui Li +5 more
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Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases
Life, 2021 Neurodegenerative diseases, including Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease, are a class of diseases that lead to dysfunction of cognition and mobility.
Soonsil Hyun, Dongyun Shin
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Targeted protein degradation as an antiviral approach
Antiviral Research, 2023 Targeted protein degradation (TPD) has emerged as a new modality in drug discovery. In this approach, small molecules are used to drive degradation of the target protein of interest. Whereas most direct-acting antivirals (DAAs) inhibit or derange the activity of their viral protein targets and have occupancy-driven pharmacology, small molecules with a ...
Antara, Chakravarty, Priscilla L, Yang
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Targeted protein degradation: mechanisms, strategies and application
Signal Transduction and Targeted Therapy, 2022 Traditional drug discovery mainly focuses on direct regulation of protein activity. The development and application of protein activity modulators, particularly inhibitors, has been the mainstream in drug development.
Lin Zhao +4 more
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Targeted protein degradation as a tumor suppressor [PDF]
Cell Cycle, 2014 Targeted protein degradation by the ubiquitin-proteasome system (UPS) has an essential role in carcinogenesis and cancer cell survival. Thus, the search for proteasome inhibitors is of great interest as a potential anticancer therapy.1 Recent studies by the Ferbeyre group suggest that certain UPS-targeted proteins play a role not just in carcinogenesis,
Arat, Nezahat Ozlem, Harrington, Lea
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Advances in targeted degradation of endogenous proteins [PDF]
Cellular and Molecular Life Sciences, 2019 Protein silencing is often employed as a means to aid investigations in protein function and is increasingly desired as a therapeutic approach. Several types of protein silencing methodologies have been developed, including targeting the encoding genes, transcripts, the process of translation or the protein directly.
Sascha Röth +2 more
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