In 2022,Henning, Nathaniel J.; Boike, Lydia; Spradlin, Jessica N.; Ward, Carl C.; Liu, Gang; Zhang, Erika; Belcher, Bridget P.; Brittain, Scott M.; Hesse, Matthew J.; Dovala, Dustin; McGregor, Lynn M.; Valdez Misiolek, Rachel; Plasschaert, Lindsey W.; Rowlands, David J.; Wang, Feng; Frank, Andreas O.; Fuller, Daniel; Estes, Abigail R.; Randal, Katelyn L.; Panidapu, Anoohya; McKenna, Jeffrey M.; Tallarico, John A.; Schirle, Markus; Nomura, Daniel K. published an article in Nature Chemical Biology. The title of the article was 《Deubiquitinase-targeting chimeras for targeted protein stabilization》.Related Products of 51644-96-3 The author mentioned the following in the article:
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we present deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small mols. consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner. Using chemoproteomic approaches, we discovered the covalent ligand EN523 that targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1. We showed that a DUBTAC consisting of our EN523 OTUB1 recruiter linked to lumacaftor, a drug used to treat cystic fibrosis that binds ΔF508-cystic fibrosis transmembrane conductance regulator (CFTR), robustly stabilized ΔF508-CFTR protein levels, leading to improved chloride channel conductance in human cystic fibrosis bronchial epithelial cells. We also demonstrated stabilization of the tumor suppressor kinase WEE1 in hepatoma cells. Our study showcases covalent chemoproteomic approaches to develop new induced proximity-based therapeutic modalities and introduces the DUBTAC platform for TPS. [graphic not available: see fulltext] After reading the article, we found that the author used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)
Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Related Products of 51644-96-3
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