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Harnessing the FBXW7 Somatic Mutant R465C for Targeted Protein Degradation. [PDF]
Basu AA +5 more
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Toward Anti-Herpesviral PROTACs: Assessing the Challenges for Targeted Protein Degradation on the Example of Kaposi's Sarcoma-Associated Herpesvirus Latency-Associated Nuclear Antigen. [PDF]
Berwanger A +10 more
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Exploration of degrons and their ability to mediate targeted protein degradation. [PDF]
Harris TJ, Trader DJ.
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Aptamer-Based Targeted Protein Degradation
ACS Nano, 2023The selective removal of misfolded, aggregated, or aberrantly overexpressed protein plays an essential role in maintaining protein-dominated biological processes. In parallel, the precise knockout of abnormal proteins is inseparable from the accurate identification of proteins within complex environments.
Yuan Liu +7 more
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Targeted Protein Degradation via Lysosomes
Biochemistry, 2022In the scope of targeted protein degradation (TPD), proteolysis-targeting chimeras (PROTACs), leveraging the ubiquitin-proteasome system, have been extensively studied. However, they are limited to the degradation of soluble and membrane proteins, excluding the aggregated and extracellular proteins and dysfunctional organelles.
Rishi R. Paudel +4 more
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Monomeric Targeted Protein Degraders
Journal of Medicinal Chemistry, 2020The discovery and development of targeted protein degraders have become important areas of research in the field of medicinal chemistry. Inducing degradation of a target protein presents several advantages relative to simple inhibition including a potential for extended duration of action and more profound pharmacology.
Emily J. Hanan +5 more
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Targeted protein degradation mechanisms
Drug Discovery Today: Technologies, 2019Targeted protein degradation mediated by small molecule degraders represents an exciting new therapeutic opportunity to eliminate disease-causing proteins. These molecules recruit E3 ubiquitin ligases to the protein of interest and mediate its ubiquitination and subsequent proteolysis by the proteasome.
Yi, Zhang +3 more
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Clinical Translation of Targeted Protein Degraders
Clinical Pharmacology & Therapeutics, 2023Targeted protein degradation (TPD) has emerged as a potentially transformational therapeutic modality with considerable promise. Molecular glue degraders remodel the surface of E3 ligases inducing interactions with neosubstrates resulting in their polyubiquitination and proteasomal degradation.
Nikki R. Kong, Lyn H. Jones
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