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Synthesis of bisubstrate analogues targeting α-1,3-fucosyltransferase and their activities
| Content Provider | Semantic Scholar |
|---|---|
| Author | Izumi, Masayuki Kaneko, Syunsuke Yuasa, Hideya Hashimoto, Hironobu |
| Copyright Year | 2006 |
| Abstract | We designed two bisubstrate analogues targeting α-1,3-fucosyltransferases, based on the three dimensional structure of Lewis X, which is the product of a α-1,3-fucosyltransferase reaction. We selected guanosine-5′-diphospho-L-galactose as a donor mimic and 2-hydroxyethyl β-D-galactoside as an acceptor mimic, and tethered these two mimics with a methylene or ethylene linker. For the synthesis, the 6-position of L-galactose and the 6-position of D-galactose were first tethered via a methylene or ethylene linker. The L-galactose moiety was then converted to a GDP derivative. Both bisubstrate analogues were moderate inhibitors against α-1,3-fucosyltransferase V and VI. The fact that they were substrates of α-1,3-fucosyltransferase VI suggested that these compounds bound to the donor binding site, but not to the acceptor binding site. |
| File Format | PDF HTM / HTML |
| DOI | 10.1039/B513897C |
| Alternate Webpage(s) | http://www.rsc.org/suppdata/ob/b5/b513897c/b513897c.pdf |
| Alternate Webpage(s) | https://doi.org/10.1039/B513897C |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
