Modified minimal-size fragments of heparan sulfate as inhibitors of endosulfatase-2 (Sulf-2).
Chem Commun (Camb)
; 60(4): 436-439, 2024 Jan 04.
Article
em En
| MEDLINE
| ID: mdl-38086706
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Oligossacarídeos
/
Heparitina Sulfato
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article