1257633-67-2Relevant academic research and scientific papers
Highly-efficient and versatile fluorous-tagged Cu(i)-catalyzed azide-alkyne cycloaddition ligand for preparing bioconjugates
Sun, Lingyi,Gai, Yongkang,Anderson, Carolyn J.,Zeng, Dexing
, p. 17072 - 17075 (2015)
A novel ligand (FBTTBE) for Cu(i)-catalyzed azide-alkyne cycloaddition (CuAAC) has been developed, which demonstrates not only superior catalytic efficiency but also the ease of removing toxic copper species. FBTTBE has also been successfully applied in the synthesis of radiometal-labeled peptide and antibody without observable transchelation with the non-radioactive Cu(i) catalyst.
Biocompatible copper(I) catalysts for in vivo imaging of glycans
Soriano Del Amo, David,Wang, Wei,Jiang, Hao,Besanceney, Christen,Yan, Amy C.,Levy, Matthew,Liu, Yi,Marlow, Florence L.,Wu, Peng
, p. 16893 - 16899 (2010)
The Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) is the standard method for bioorthogonal conjugation. However, current Cu(I) catalyst formulations are toxic, hindering their use in living systems. Here we report that BTTES, a tris(triazolylmethyl)amine-based ligand for Cu(I), promotes the cycloaddition reaction rapidly in living systems without apparent toxicity. This catalyst allows, for the first time, noninvasive imaging of fucosylated glycans during zebrafish early embryogenesis. We microinjected embryos with alkyne-bearing GDP-fucose at the one-cell stage and detected the metabolically incorporated unnatural sugars using the biocompatible click chemistry. Labeled glycans could be imaged in the enveloping layer of zebrafish embryos between blastula and early larval stages. This new method paves the way for rapid, noninvasive imaging of biomolecules in living organisms.
CU(I)-CATALYZED AZIDE-ALKYNE CYCLOADDITIONS (CUAAC) LIGANDS AND METHODS FOR CARRYING OUT CU(I)-CATALYZED AZIDE-ALKYNE CYCLOADDITION REACTIONS
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Paragraph 0055, (2017/11/08)
A Cu(I)-Catalyzed Azide-Alkyne Cycloadditions (CuAAC) ligand comprising: a catalytic core; a fluorous tag; and a linker binding the fluorous tag to the catalytic core. A method for carrying out a Cu(I)-Catalyzed Azide-Alkyne Cycloaddition reaction, comprising: combining in a solution an alkyne-tagged component, an azide-tagged component and a Cu(I)-Catalyzed Azide-Alkyne Cycloadditions (CuAAC) ligand comprising: a catalytic core; a fluorous tag; and a linker binding the fluorous tag to the catalytic core; filtering the solution through a solid phase extraction filter to remove Cu(I)-ligand catalyst and/or excess ligand.
LIGANDS AND METHODS FOR LABELING BIOMOLECULES IN VIVO
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Paragraph 0062; 0063, (2013/11/19)
Disclosed are tris(triazolylmethyl)amine ligands, and kits and methods for labeling and/or imaging a biomolecule of interest in a subject or living system.
Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-α production in human whole blood
Wu, Junjun,Green, Neal,Hotchandani, Rajeev,Hu, Yonghan,Condon, Jeffrey,Huang, Adrian,Kaila, Neelu,Li, Huan-Qiu,Guler, Satenig,Li, Wei,Tam, Steve Y.,Wang, Qin,Pelker, Jeffrey,Marusic, Suzana,Hsu, Sang,Perry Hall,Telliez, Jean-Baptiste,Cui, Junqing,Lin, Lih-Ling
scheme or table, p. 3485 - 3488 (2010/03/03)
Tpl2 (cot/MAP3K8) is an upstream kinase of MEK in the ERK pathway. It plays an important role in Tumor Necrosis Factor-α (TNF-α) production and signaling. We have discovered that 8-halo-4-(3-chloro-4-fluoro-phenylamino)-6-[(1H-[1,2,3]triazol-4-ylmethyl)-a
