Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2).

Autor: Kennett, Alice, Epple, Sven, van der Valk, Gabriella, Georgiou, Irene, Gout, Evelyne, Vivεave;s, Romain R., Russell, Angela J.
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Zdroj: Chemical Communications; 1/14/2024, Vol. 60 Issue 4, p436-439, 4p
Abstrakt: 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. [ABSTRACT FROM AUTHOR]
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