- Fast and Tight Boronate Formation for Click Bioorthogonal Conjugation
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A new click bioorthogonal reaction system was devised to enable the fast ligation (kON≈340 m-1 s-1) of conjugatable derivatives of a rigid cyclic diol (nopoldiol) and a carefully optimized boronic acid partner, 2-methyl-5-carboxymethylphenylboronic acid. Using NMR and fluorescence spectroscopy studies, the corresponding boronates were found to form reversibly within minutes at low micromolar concentration in water, providing submicromolar equilibrium constant (Keq≈105-106 m-1). Efficient protein conjugation under physiological conditions was demonstrated with model proteins thioredoxin and albumin, and characterized by mass spectrometry and gel electrophoresis.
- Akgun, Burcin,Hall, Dennis G.
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supporting information
p. 3909 - 3913
(2016/03/19)
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- 2-AMINOQUINAZOLINE DERIVATIVE
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The present invention provides a compound represented by Formula (I) (wherein R 1 and R 2 are the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl and the like, R 3 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group and the like, R 4 and R 5 are the same or different, and each represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl and the like, proviso that they are not simultaneously hydrogen atoms, and R 6 represents hydroxy or substituted or unsubstituted lower alkoxy), or a pharmaceutically acceptable salt thereof and the like.
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Page/Page column 46
(2010/11/24)
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- Modular Solid-Phase Synthetic Approach to Optimize Structural and Electronic Properties of Oligoboronic Acid Receptors and Sensors for the Aqueous Recognition of Oligosaccharides
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This article describes the design and optimization of the first entirely modular, parallel solid-phase synthetic approach for the generation of well-defined polyamine oligoboronic acid receptors and fluorescence sensors for complex oligosaccharides. The s
- Stones, Duane,Manku, Sukhdev,Lu, Xiaosong,Hall, Dennis G.
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