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Development of targeted protein degradation therapeutics
Nature Chemical Biology, 2019Targeted protein degradation as a therapeutic modality has seen dramatic progress and massive investment in recent years because of the convergence of two key scientific breakthroughs: optimization of first-generation peptidic proteolysis-targeted chimeras (PROTACs) into more drug-like molecules able to support in vivo proof of concept and the ...
Philip P, Chamberlain +1 more
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Targeted Degradation of Proteins by PROTACs
Current Protocols in Chemical Biology, 2010AbstractIn recent years, small interference RNAs (siRNAs) have greatly enhanced our understanding of protein functions by allowing knockdown of targeted proteins at the mRNA level. Similarly, in an effort to achieve degradation of targeted proteins at the post‐translational level, chimeric small molecules called “PROTACs” (PROteolysis TArgeting ...
Eun Ryoung, Jang +2 more
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Degrading the signal amplifier: ITK as a target for targeted protein degradation
Cell Chemical Biology, 2023In this issue of Cell Chemical Biology, Jiang and colleagues show for the first time that the Tec kinase ITK can be targeted using PROTAC approaches. This new modality has implications for the treatment of T cell lymphomas, but also potentially for the treatment of T cell-mediated inflammatory diseases, that depend on ITK signaling.
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Next steps for targeted protein degradation
Cell Chemical BiologyTargeted protein degradation (TPD) has greatly advanced as a therapeutic strategy in the past two decades, and we are on the cusp of rationally designed protein degraders reaching clinical approval. Offering pharmacological advantages relative to occupancy-driven protein inhibition, chemical methods for regulating biomolecular proximity have provided ...
Mackenzie W. Krone, Craig M. Crews
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Targeted Protein Degraders- The Druggability Perspective
Journal of Pharmaceutical SciencesTargeted Protein degraders (TPDs) show promise in harnessing cellular machinery to eliminate disease-causing proteins, even those previously considered undruggable. Especially if protein turnover is low, targeted protein removal bestows lasting therapeutic effect over typical inhibition.
Satinder, Singh, Pratima, Srivastava
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Targeted protein degradation for cancer therapy
Nature Reviews CancerTargeted protein degradation (TPD) aims at reprogramming the target specificity of the ubiquitin-proteasome system, the major cellular protein disposal machinery, to induce selective ubiquitination and degradation of therapeutically relevant proteins. Since its conception over 20 years ago, TPD has gained a lot of attention mainly due to improvements ...
Matthias Hinterndorfer +3 more
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Advancing targeted protein degradation modalities
Trends in Pharmacological Sciences, 2023openaire +2 more sources
Lysosome Targeting Chimaeras for Glut1-Facilitated Targeted Protein Degradation
Journal of the American Chemical SocietyTargeted protein degradation technology holds great potential in biomedicine, particularly in treating tumors and other protein-related diseases. Research on intracellular protein degradation using molecular glues and PROTAC technology is leading, while research on the degradation of membrane proteins and extracellular proteins through the lysosomal ...
Jinyan Luo +12 more
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The contemporary management of cancers of the sinonasal tract in adults
Ca-A Cancer Journal for Clinicians, 2023Rajat Thawani
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