Ligand compatibility of salacinol-type α-glucosidase inhibitors toward the GH31 family

We show that salacinol-type α-glucosidase inhibitors are ligand-compatible with the GH 31 family. Salacinol and its 3′-O-benzylated analogs inhibit human lysosomal α-glucosidase at submicromolar levels. Simple structure-activity relationship studies reveal that the salacinol side-chain stereochemist...

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Detalles Bibliográficos
Autores principales: Ishikawa, Fumihiro, Hirano, Aiko, Yoshimori, Yuuto, Nishida, Kana, Nakamura, Shinya, Takashima, Katsuki, Marumoto, Shinsuke, Ninomiya, Kiyofumi, Nakanishi, Isao, Xie, Weijia, Morikawa, Toshio, Muraoka, Osamu, Tanabe, Genzoh
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8694024/
https://www.ncbi.nlm.nih.gov/pubmed/35424309
http://dx.doi.org/10.1039/d0ra10038b
Descripción
Sumario:We show that salacinol-type α-glucosidase inhibitors are ligand-compatible with the GH 31 family. Salacinol and its 3′-O-benzylated analogs inhibit human lysosomal α-glucosidase at submicromolar levels. Simple structure-activity relationship studies reveal that the salacinol side-chain stereochemistry significantly influences binding to GH31 α-glucosidases.

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