Galectins are a family of proteins that possess β-galactoside-binding properties through their carbohydrate recognition domains (CRDs). Galectins can be secreted from cells by nonclassic pathways to interact with external glycoconjugates and have a variety of activities both extra- and intracellularly, with important implicated roles in immunity, inflammation, and cancer.
Galectins can be classified according to the CRD features. Galectin-1, -2, -5, -7, -10, -11, -13, and -14 are composed of a CRD and a short N-terminal sequence (prototype). Galectin-4, -6, -8, -9, and -12 have two nonidentical CRDs in tandem with a short linker sequence (tandem-repeat type). Galectin-3 has an exceptional structure, with a CRD and an extended N-terminal domainconsisting of gycine/proline-rich repeats and a short N-terminal end (chimera type). Galectin-1 (Gal1), a carbohydrate-binding protein is implicated in cancer cell proliferation, invasion and tumour angiogenesis. Galectin-3 (Gal3) is a β-galactoside binding lectin that is highly expressed in fibrotic tissue of diverse etiologies.
Galectins have emerged as key players in the tumor microenvironment. Galectins are expressed and released by different celltypes, including tumor, stromal, endothelial and immune cells. Galectins critically influence tumor progression by modulating tumor cell migration, invasiveness, angiogenesis and antitumor immune responses. Intracellularly, galectins modulate survival and proliferation and they interact with a variety of signaling pathways. Given these extracellular and intracellular functions and their regulated expression at sites of tumor growth and metastasis, galectins have stimulated great interest as relevant biomarkers and novel targets in cancer therapy.
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GB1107 (GB-1107, GB 1107) is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with Kd of 37 nM (human Galectin-3); displays >100-fold lower affinity for most of the tested human galectins, and 20 and 4-fold lower affinity for galectin-2 and the C-terminal CRD of galectin-4, respectively; prevents human lung adenocarcinoma growth in vivo, increases tumor M1 macrophage polarization and CD8+ T cell infiltration; GB1107 also can potentiate the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules.
TD-139 (TD139) is a highly potent, selecitve inhibitor of Galectin-3 (Gal-3) carbohydrate binding domain with Ki of 14 nM; reduces TGF-β1-induced β-catenin translocation to the nucleus, blocks β-catenin phosphorylation in vitro and in vivo; attenuates the late-stage progression of lung fibrosis in murine models; attenuates liver injury and milder infiltration of IFNγ- and IL-17- and -4-producing CD4(+) T cells, increases IL-10-producing CD4(+) T cells and F4/80(+) CD206(+) alternatively activated macrophages and prevents the apoptosis of liver-infiltrating MNCs in WT C57BL/6 mice.
LLS2 is a novel potent Galectin-1 (Gal1) inhibitor that decreases membrane-associated H-Ras and K-Ras and contributed to the suppression of pErk pathway; kills SKOV3, HT29, PC3, XPA3, MCF7, and A549 with an IC50 of 11.7, 24.5, 28.2, 20.9, 23.2 and 34.3 uM respectively; exhibits synergistic activity against several human cancer cell lines, significantly inhibits the growth of ovarian cancer xenografts in athymic mice combined with paclitaxel.
LLS30 is a potent, allosteric Galectin-1 (Gal-1) inhibitor, inhibits AR negative cells PC3, DU145, and AR positive cells, 22RV1 and CWR-R1 cells with IC50 of 10.4 μM, 5.3 μM, 3.3 μM and 5.9 μM, respectively; decreases Gal-1 binding affinity to its binding partners; showes in vivo efficacy in both AR positive and AR negative xenograft models; not only can potentiate the anti-tumor effect of docetaxel to cause complete regression of tumors, but also effectively inhibit the invasion and metastasis of PCa cells in vivo.
OTX008 is a selective inhibitor of galectin-1.
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