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Selective Galectin-8N Ligands : The Design and Synthesis of Phthalazinone-d-Galactals

van Klaveren, Sjors LU ; Sundin, Anders P. LU ; Jakopin, Žiga ; Anderluh, Marko LU ; Leffler, Hakon LU ; Nilsson, Ulf J. LU and Tomašič, Tihomir (2021) In ChemMedChem 17(6).
Abstract

Ligand selectivity among the highly conserved galectins has been an ever-challenging objective. For galectin-8, a protein prevalent in both pathology and tissue distribution, we report phthalazinone-galactals that show excellent selectivity for the galectin-8N-terminal domain. A dissection of structure–activity relationships of the phthalazinone and an extensive molecular dynamics meta-analysis accompany the discovery of the selective galectin-8N ligands presented here. These selective compounds will facilitate the study of galectin-8 biology and may have pharmaceutical relevance in the wide range of galectin-8 associated pathologies.

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author
; ; ; ; ; and
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
ChemMedChem
volume
17
issue
6
article number
e202100575
publisher
Wiley-Blackwell
external identifiers
  • scopus:85122034809
  • pmid:34913595
ISSN
1860-7179
DOI
10.1002/cmdc.202100575
language
English
LU publication?
yes
id
557a9c1f-2c8b-48e9-9e56-4863a7d1bbe4
date added to LUP
2022-03-23 11:49:19
date last changed
2025-03-16 23:35:36
@article{557a9c1f-2c8b-48e9-9e56-4863a7d1bbe4,
  abstract     = {{<p>Ligand selectivity among the highly conserved galectins has been an ever-challenging objective. For galectin-8, a protein prevalent in both pathology and tissue distribution, we report phthalazinone-galactals that show excellent selectivity for the galectin-8N-terminal domain. A dissection of structure–activity relationships of the phthalazinone and an extensive molecular dynamics meta-analysis accompany the discovery of the selective galectin-8N ligands presented here. These selective compounds will facilitate the study of galectin-8 biology and may have pharmaceutical relevance in the wide range of galectin-8 associated pathologies.</p>}},
  author       = {{van Klaveren, Sjors and Sundin, Anders P. and Jakopin, Žiga and Anderluh, Marko and Leffler, Hakon and Nilsson, Ulf J. and Tomašič, Tihomir}},
  issn         = {{1860-7179}},
  language     = {{eng}},
  number       = {{6}},
  publisher    = {{Wiley-Blackwell}},
  series       = {{ChemMedChem}},
  title        = {{Selective Galectin-8N Ligands : The Design and Synthesis of Phthalazinone-d-Galactals}},
  url          = {{http://dx.doi.org/10.1002/cmdc.202100575}},
  doi          = {{10.1002/cmdc.202100575}},
  volume       = {{17}},
  year         = {{2021}},
}