通过糖苷酶抑制剂的非糖部分相互作用进行调节：法布雷病和神经节苷脂贮积症的药理学伴侣分子。
Tuning glycosidase inhibition through aglycone interactions: pharmacological chaperones for Fabry disease and GM1 gangliosidosis.
机构信息
Dpto. Química Orgánica, Fac. de Química, Universidad de Sevilla, c/ Professor García González 1, E-41012 Sevilla, Spain.
出版信息
Chem Commun (Camb). 2012 Jul 4;48(52):6514-6. doi: 10.1039/c2cc32065g. Epub 2012 May 23.
PMID:22618082
Abstract
Competitive inhibitors of either α-galactosidase (α-Gal) or β-galactosidase (β-Gal) with high affinity and selectivity have been accessed by exploiting aglycone interactions with conformationally locked sp(2)-iminosugars. Selected compounds were profiled as potent pharmacological chaperones for mutant lysosomal α- and β-Gal associated with Fabry disease and GM(1) gangliosidosis.
摘要
通过利用糖苷配基与构象固定的 sp(2)-亚氨基糖之间的相互作用，获得了对α-半乳糖苷酶（α-Gal）或β-半乳糖苷酶（β-Gal）具有高亲和力和选择性的竞争性抑制剂。选择的化合物被用作法布里病和 GM(1)神经节苷脂贮积症相关突变溶酶体α-和β-半乳糖苷酶的有效药理学伴侣。
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