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

Öberg, Christopher LU ; Blanchard, Helen; Leffler, Hakon LU and Nilsson, Ulf LU (2008) In Bioorganic & Medicinal Chemistry Letters 18(13). p.3691-3694
Abstract
A series of O2 and O3-derivatized methyl beta-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.
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Bioorganic & Medicinal Chemistry Letters
volume
18
issue
13
pages
3691 - 3694
publisher
Elsevier
external identifiers
  • WOS:000256708000003
  • PMID:18539029
  • Scopus:44749093873
ISSN
1090-2120
DOI
10.1016/j.bmcl.2008.05.066
language
English
LU publication?
yes
id
03fbe0d6-ecf0-4fd1-8da0-3c2fc4aef9c5 (old id 1169011)
alternative location
http://www.ncbi.nlm.nih.gov/pubmed/18539029?dopt=Abstract
date added to LUP
2008-07-03 11:30:21
date last changed
2016-11-27 04:28:38
@misc{03fbe0d6-ecf0-4fd1-8da0-3c2fc4aef9c5,
  abstract     = {A series of O2 and O3-derivatized methyl beta-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.},
  author       = {Öberg, Christopher and Blanchard, Helen and Leffler, Hakon and Nilsson, Ulf},
  issn         = {1090-2120},
  language     = {eng},
  number       = {13},
  pages        = {3691--3694},
  publisher    = {ARRAY(0xb6a9b38)},
  series       = {Bioorganic & Medicinal Chemistry Letters},
  title        = {Protein subtype-targeting through ligand epimerization: talose-selectivity of galectin-4 and galectin-8.},
  url          = {http://dx.doi.org/10.1016/j.bmcl.2008.05.066},
  volume       = {18},
  year         = {2008},
}