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Fragment-based development of triazole-substituted O-galactosyl aldoximes with fragment-induced affinity and selectivity for galectin-3.

Tejler, Johan LU ; Salameh, Bader; Leffler, Hakon LU and Nilsson, Ulf LU (2009) In Organic and Biomolecular Chemistry 7(19). p.3982-3990
Abstract
A fragment-based development of 3C-triazol-1-yl-O-galactopyranosyl aldoximes led to the discovery of highly selective and high affinity (K(d) down to 11 microm) small monosaccharide based inhibitors of galectin-3. Galectin-7, 8 N-terminal CRD, and 9 N-terminal CRD bound the inhibitors only weakly. The galectin-3 selectivity was hypothesized to stem from interaction of the aldoxime moiety with a site not present in the other galectins.
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Organic and Biomolecular Chemistry
volume
7
issue
19
pages
3982 - 3990
publisher
Royal Society of Chemistry
external identifiers
  • wos:000269892900015
  • pmid:19763301
  • scopus:70349281538
ISSN
1477-0539
DOI
10.1039/b909091f
language
English
LU publication?
yes
id
2a635acc-a8de-47e0-86cc-690e0cfb0a19 (old id 1483366)
date added to LUP
2009-10-09 07:30:05
date last changed
2017-01-01 04:23:53
@article{2a635acc-a8de-47e0-86cc-690e0cfb0a19,
  abstract     = {A fragment-based development of 3C-triazol-1-yl-O-galactopyranosyl aldoximes led to the discovery of highly selective and high affinity (K(d) down to 11 microm) small monosaccharide based inhibitors of galectin-3. Galectin-7, 8 N-terminal CRD, and 9 N-terminal CRD bound the inhibitors only weakly. The galectin-3 selectivity was hypothesized to stem from interaction of the aldoxime moiety with a site not present in the other galectins.},
  author       = {Tejler, Johan and Salameh, Bader and Leffler, Hakon and Nilsson, Ulf},
  issn         = {1477-0539},
  language     = {eng},
  number       = {19},
  pages        = {3982--3990},
  publisher    = {Royal Society of Chemistry},
  series       = {Organic and Biomolecular Chemistry},
  title        = {Fragment-based development of triazole-substituted O-galactosyl aldoximes with fragment-induced affinity and selectivity for galectin-3.},
  url          = {http://dx.doi.org/10.1039/b909091f},
  volume       = {7},
  year         = {2009},
}