Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2),Chemical Communications

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Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2)
Chemical Communications ( IF 4.3 ) Pub Date : 2023-11-07 , DOI: 10.1039/d3cc02565a
Alice Kennett ₁ , Sven Epple ₁ , Gabriella van der Valk ₁ , Irene Georgiou ₁ , Evelyne Gout ₂ , Romain R Vivès ₂ , Angela J Russell _{1,

3}

Affiliation

Sulf-2 has been identified as a putative target for anticancer therapies. Here we report the design and synthesis of sulfated disaccharide inhibitors based on IdoA(2S)-GlcNS(6S). Trisulfated disaccharide inhibitor IdoA(2S)-GlcNS(6Sulfamate) demonstrated potent Sulf-2 inhibition. The IC₅₀ value was determined to be 39.8 μM ± 18.3, which is comparable to a tetrasaccharide inhibitor of HSulf-1 reported in the literature. We propose that the disaccharide IdoA(2S)-GlcNS(6S) is the shortest fragment size required for effective inhibition of the Sulfs.

中文翻译：

修饰的硫酸乙酰肝素最小尺寸片段作为内切硫酸酯酶 2 (Sulf-2) 的抑制剂

Sulf-2 已被确定为抗癌治疗的推定靶点。在此，我们报道了基于IdoA(2S)-GlcNS(6S)的硫酸化二糖抑制剂的设计和合成。三硫酸化二糖抑制剂 IdoA(2S)-GlcNS(6Sulfamate) 表现出有效的 Sulf-2 抑制作用。测定IC ₅₀值为39.8 μM ± 18.3，与文献报道的HSulf-1四糖抑制剂相当。我们认为二糖 IdoA(2S)-GlcNS(6S) 是有效抑制 Sulf 所需的最短片段大小。

更新日期：2023-11-07

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