GB1107 是一种有效的、选择性的、口服活性的 Galectin-3 (Gal-3) 抑制剂，对人 Galectin-3 的 Kd 为 37 nM。 GB1107 在同基因模型中减少人和小鼠肺腺癌的生长并阻止转移。
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model[1].
Treatment with GB1107 (0-1 μM) increases tumor M1 macrophage polarization and CD8+ T cell infiltration in LLC cells by flow cytometric analysis. GB1107 potentiates 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[1].
GB1107 (10 mg/kg, p.o., once daily from day 18-30 post implantation) treatment results in significantly reduced tumor growth and final tumor weights[1].
Reference:
[1]. Vuong L, et al. An orally active galectin-3 antagonist inhibits lung adenocarcinoma growth and augments response to PD-L1 blockade. Cancer Res. 2019 Jan 23. pii: canres.2244.2018.
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