Synonyms: compound 11d [Zetterberg et al., 2022] | Example 44 [WO2016120403A1] | GB-1211
Compound class:
Synthetic organic
Comment: GB1211 is an orally active small molecule galectin-3 inhibitor [1,5]. It was developed by Galecto Biotech for the treatment of fibrotic disease and cancer. In the fibrotic setting, blocking galectin-3's biological function is predicted to combat the enhanced TGF-β receptor-mediated macrophage differentiation and myofibroblast activation that drives pathological fibrotic changes [2-4].
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References |
1. Brimert T, Johnsson R, Leffler H, Nilsson U, Zetterberg F. (2017)
Alpha-d-galactoside inhibitors of galectins. Patent number: WO2016120403A1. Assignee: Galecto Biotech AB. Priority date: 30/01/2015. Publication date: 07/12/2017. |
2. MacKinnon AC, Farnworth SL, Hodkinson PS, Henderson NC, Atkinson KM, Leffler H, Nilsson UJ, Haslett C, Forbes SJ, Sethi T. (2008)
Regulation of alternative macrophage activation by galectin-3. J Immunol, 180 (4): 2650-8. [PMID:18250477] |
3. Mackinnon AC, Gibbons MA, Farnworth SL, Leffler H, Nilsson UJ, Delaine T, Simpson AJ, Forbes SJ, Hirani N, Gauldie J et al.. (2012)
Regulation of transforming growth factor-β1-driven lung fibrosis by galectin-3. Am J Respir Crit Care Med, 185 (5): 537-46. [PMID:22095546] |
4. Partridge EA, Le Roy C, Di Guglielmo GM, Pawling J, Cheung P, Granovsky M, Nabi IR, Wrana JL, Dennis JW. (2004)
Regulation of cytokine receptors by Golgi N-glycan processing and endocytosis. Science, 306 (5693): 120-4. [PMID:15459394] |
5. Zetterberg FR, MacKinnon A, Brimert T, Gravelle L, Johnsson RE, Khal-Knutson B, Leffler H, Nilsson UJ, Pedersen A, Peterson K et al.. (2022)
Discovery and Optimization of the First Highly Effective and Orally Available Galectin-3 Inhibitors for Treatment of Fibrotic Disease. Journal of Medicinal Chemistry,. DOI: 10.1021/acs.jmedchem.2c00660 |