Inhibition of Galectins with Small Molecules
(2011) In Chimia 65(1-2). p.18-23- Abstract
- Evidence that the galectin family of proteins plays crucial roles in cancer, inflammation, and immunity has accumulated over the last decade. The galectins have consequently emerged as interesting drug targets. A majority of galectin functions occurs by means of cross-linking glycoproteins and by doing so controlling gly-coproteirl cellular localization and residence times. The glycoprotein cross-linking occurs when galectin dimers or multimers, or galectins with two binding sites, bind galactose-containing glycans of the glycoproteins. Such galectin-glycan interactions have been successfully blocked with compounds having multivalent presentation of galactose, lactose, or N-acetyllactosamine, with peptides, and with small carbohydrate... (More)
- Evidence that the galectin family of proteins plays crucial roles in cancer, inflammation, and immunity has accumulated over the last decade. The galectins have consequently emerged as interesting drug targets. A majority of galectin functions occurs by means of cross-linking glycoproteins and by doing so controlling gly-coproteirl cellular localization and residence times. The glycoprotein cross-linking occurs when galectin dimers or multimers, or galectins with two binding sites, bind galactose-containing glycans of the glycoproteins. Such galectin-glycan interactions have been successfully blocked with compounds having multivalent presentation of galactose, lactose, or N-acetyllactosamine, with peptides, and with small carbohydrate (galactose) derivatives. This review summarizes and analyzes attempts to develop efficient and selective small-molecule galectin inhibitors through derivatization of monosaccharides, mainly galactosides, with non-carbohydrate structures that protrude into subsites adjacent to the core-conserved galactose-recognizing site of the galectins. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/1868550
- author
- Öberg, Christopher LU ; Leffler, Hakon LU and Nilsson, Ulf LU
- organization
- publishing date
- 2011
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Cancer, Galectin, Immunity, Inflammation, Inhibitor
- in
- Chimia
- volume
- 65
- issue
- 1-2
- pages
- 18 - 23
- publisher
- Swiss Chemical Society
- external identifiers
-
- wos:000287981400004
- pmid:21469439
- scopus:79952576615
- ISSN
- 0009-4293
- DOI
- 10.2533/chimia.2011.18
- language
- English
- LU publication?
- yes
- additional info
- The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240), Division of Microbiology, Immunology and Glycobiology - MIG (013025200)
- id
- bcc019e3-c3e2-43a3-96c3-796a55b73c8f (old id 1868550)
- date added to LUP
- 2016-04-01 14:18:13
- date last changed
- 2022-03-29 20:13:11
@article{bcc019e3-c3e2-43a3-96c3-796a55b73c8f,
abstract = {{Evidence that the galectin family of proteins plays crucial roles in cancer, inflammation, and immunity has accumulated over the last decade. The galectins have consequently emerged as interesting drug targets. A majority of galectin functions occurs by means of cross-linking glycoproteins and by doing so controlling gly-coproteirl cellular localization and residence times. The glycoprotein cross-linking occurs when galectin dimers or multimers, or galectins with two binding sites, bind galactose-containing glycans of the glycoproteins. Such galectin-glycan interactions have been successfully blocked with compounds having multivalent presentation of galactose, lactose, or N-acetyllactosamine, with peptides, and with small carbohydrate (galactose) derivatives. This review summarizes and analyzes attempts to develop efficient and selective small-molecule galectin inhibitors through derivatization of monosaccharides, mainly galactosides, with non-carbohydrate structures that protrude into subsites adjacent to the core-conserved galactose-recognizing site of the galectins.}},
author = {{Öberg, Christopher and Leffler, Hakon and Nilsson, Ulf}},
issn = {{0009-4293}},
keywords = {{Cancer; Galectin; Immunity; Inflammation; Inhibitor}},
language = {{eng}},
number = {{1-2}},
pages = {{18--23}},
publisher = {{Swiss Chemical Society}},
series = {{Chimia}},
title = {{Inhibition of Galectins with Small Molecules}},
url = {{http://dx.doi.org/10.2533/chimia.2011.18}},
doi = {{10.2533/chimia.2011.18}},
volume = {{65}},
year = {{2011}},
}