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Glabrescione B 是第一个结合 Hedgehog (Hh) 调节剂 Gli1 并通过干扰 Gli1-DNA 相互作用而削弱其活性的化合物。Glabrescione B 抑制 Hedgehog 依赖性肿瘤细胞的生长,抑制肿瘤源性干细胞的自我更新能力和克隆能力。
Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells[1][2].
Glabrescione B (5 μM; 24-72 hours) inhibits the growth of Gli-dependent basal cell carcinoma[2].Glabrescione B (1-10 μM; 24-48 hours) decreases Gli1 mRNA expression levels[2].
[1]. Ingallina C, et al. Polymeric glabrescione B nanocapsules for passive targeting of Hedgehog-dependent tumor therapy in vitro. Nanomedicine (Lond). 2017;12(7):711-728.
[2]. Infante P, et al. Gli1/DNA interaction is a druggable target for Hedgehog-dependent tumors. EMBO J. 2015;34(2):200-217.
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