Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8

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Title Protein subtype-targeting through ligand epimerization: Talose-selectivity of galectin-4 and galectin-8
Author Oberg, Christopher T.; Blanchard, Helen; Leffler, Hakon; Nilsson, Ulf J.
Journal Name Bioorganic and Medicinal Chemistry Letters
Year Published 2008
Place of publication United Kingdom
Publisher Elsevier
Abstract A series of O2 and O3-derivatized methyl β-d-talopyranosides were synthesized and evaluated in vitro as inhibitors of the galactose-binding galectin-1, -2, -3, -4 (N- and C-terminal domains), 8 (N-terminal domain), and 9 (N-terminal domain). Galectin-4C and 8N were found to prefer the d-talopyranose configuration to the natural ligand d-galactopyranose configuration. Derivatization at talose O2 and/or O3 provided selective submillimolar inhibitors for these two galectins.
Peer Reviewed Yes
Published Yes
Alternative URI http://dx.doi.org/10.1016/j.bmcl.2008.05.066
Volume 18
Issue Number 13
Page from 3691
Page to 3694
ISSN 0960-894X
Date Accessioned 2008-10-07
Date Available 2011-06-09T22:41:13Z
Language en_AU
Research Centre Institute for Glycomics
Faculty Faculty of Science, Environment, Engineering and Technology
Subject PRE2009-Biological and Medical Chemistry
URI http://hdl.handle.net/10072/21598
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1

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