Issue 4, 2024

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

Abstract

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.

Graphical abstract: Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2)

Associated articles

Supplementary files

Article information

Article type
Communication
Submitted
26 Jūn. 2023
Accepted
03 Nov. 2023
First published
07 Nov. 2023
This article is Open Access
Creative Commons BY license

Chem. Commun., 2024,60, 436-439

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

A. Kennett, S. Epple, G. van der Valk, I. Georgiou, E. Gout, R. R. Vivès and A. J. Russell, Chem. Commun., 2024, 60, 436 DOI: 10.1039/D3CC02565A

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