An acceptor analogue of β-1,4-galactosyltransferase: Substrate, inhibitor, or both?
نویسندگان
چکیده
منابع مشابه
The first C-glycosidic analogue of a novel galactosyltransferase inhibitor.
Structural analogues and mimics of the natural sugar-nucleotide UDP-galactose (UDP-Gal) are sought after as chemical tools for glycobiology and drug discovery. We have recently developed a novel class of galactosyltransferase (GalT) inhibitors derived from UDP-Gal, bearing an additional substituent at the 5-position of the uracil base. Herein we report the first C-glycosidic derivative of this ...
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The hydrolysis of the donor substrate uridine diphosphate galactose (UDP-Gal) by human blood group B galactosyltransferase (GTB) has been followed by nuclear magnetic resonance in the presence and in the absence of an acceptor substrate analog. It is observed that the presence of the acceptor substrate analog promotes hydrolysis of UDP-Gal. Subsequent analysis of the kinetics of the enzymatic h...
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The β-1,4-galactosyltransferase 7 (β4GalT7) enzyme is involved in proteoglycan synthesis. In the presence of a manganese ion, it transfers galactose from UDP-galactose to xylose on a proteoglycan acceptor substrate. We present here the crystal structures of human β4GalT7 in open and closed conformations. A comparison of these crystal structures shows that, upon manganese and UDP or UDP-Gal bind...
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The fluorescent nucleobase analogues of the tricyclic cytosine (tC) family, tC and tC(O), possess high fluorescence quantum yields and single fluorescence lifetimes, even after incorporation into double-stranded DNA, which make these base analogues particularly useful as fluorescence resonance energy transfer (FRET) probes. Recently, we reported the first all-nucleobase FRET pair consisting of ...
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ژورنال
عنوان ژورنال: Carbohydrate Research
سال: 2017
ISSN: 0008-6215
DOI: 10.1016/j.carres.2017.08.012