galectin-3   Click here for help

GtoPdb Ligand ID: 6619

Synonyms: galectin 3 | GALIG | LGALS2 | MAC-2
Immunopharmacology Ligand
Compound class: Endogenous peptide in human, mouse or rat
Comment: Galectin 3 (Gal-3) is one of a group of 14 lectins that bind β-galactoside-containing carbohydrates, via a carbohydrate recognition domain (CRD), and it binds to galectin-3 binding protein. It plays regulatory functions in multiple biological processes, including cell-cell adhesion, cell-matrix interactions, macrophage activation, leukocyte migration, inflammation, angiogenesis, metastasis, apoptosis [6] and fibrosis. Galectin 3 is being investigated as a molecular target for the development of novel therapeutics for cancer [9,11], cardiovascular disease [3,5] and fibrosis (e.g. liver fibrosis in nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) [12]) [4]. GM-MD-02 (Galectin Therapeutics) is a galactoarabino-rhamnogalacturonan polysaccharide polymer (pectin) that binds to Gal-3 (Kd 8 μM: Gal-1 Kd 10 μM)) and reduces inflammation and fibrosis-associated effects in experimental models [2], but no clinical efficacy was observed in Phase 2 evaluation in patients with NASH cirrhosis (NCT02462967), although in the subset of patients with cirrhosis who had no esophageal varices some clinical benefit has been indicated, and Phase 3 testing in this subset of cirrhosis patients is planned.
In relation to cardiovascular disease, galectin 3/galectin 3 binding protein complexes co-localize to the leukocyte/endothelial cell interface of vein walls in mice and galectin 3 increases vein wall IL-6 levels and promotes venous thrombosis [5]. In human patients, elevated circulating galectin-3 binding protein correlates with acute venous thrombosis.
Species: Human
Additional information and targets (data relate to human unless otherwise stated)
Description Data Reference
Putative endogenous ligands at RTP Type K galectin-3 (LGALS3, P17931), galectin-3 binding protein (LGALS3BP, Q08380) 8
Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
olitigaltin Small molecule or natural product Hs Inhibitor Binding 7.8 pKd - 10
⤷ pKd 7.8 (Kd 1.4x10-8 M) [10]
Description: Binding affinity for galectin-3 determined using a competitive fluorescence anisotropy assay
GB1211 Small molecule or natural product Hs Inhibitor Binding 7.6 pKd - 1
⤷ pKd 7.6 (Kd 2.3x10-8 M) [1]