Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease
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DOI: 10.1021/acs.jmedchem.2c00660
Abstract: Galectin-3 is a carbohydrate-binding protein central to regulating mechanisms of diseases such as fibrosis, cancer, metabolic, inflammatory, and heart disease. We recently found a high affinity (nM) thiodigalactoside GB0139 which currently is in clinical development… read more here.
Keywords: disease; optimization first; discovery optimization; first highly ... See more keywords
Design and synthesis of novel 3-triazolyl-1-thiogalactosides as galectin-1, -3 and -8 inhibitors
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DOI: 10.1039/d2ra03163a
Abstract: Galectins are galactoside-binding proteins that play a role in various pathophysiological conditions, making them attractive targets in drug discovery. We have designed and synthesised a focused library of aromatic 3-triazolyl-1-thiogalactosides targeting their core site for… read more here.
Keywords: design synthesis; synthesis novel; galectin inhibitors; triazolyl thiogalactosides ... See more keywords
Galectin-3 Inhibitors Suppress Anoikis Resistance and Invasive Capacity in Thyroid Cancer Cells
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DOI: 10.1155/2021/5583491
Abstract: Accumulating evidence suggests that galectin-3 is a histologic marker of thyroid cancer. However, the pharmacological lectin-based approach has not been well studied. In the present study, we aimed to investigate the therapeutic potential of novel… read more here.
Keywords: thyroid cancer; anoikis resistance; galectin inhibitors; cancer cells ... See more keywords