Syntheses of sulfated glycopolymers and analyses of their BACE-1 inhibitory activity.
Bioorg Med Chem Lett
; 23(23): 6390-5, 2013 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-24125881
ABSTRACT
The glycopolymers for glycosaminoglycan mimic were synthesized, and the inhibitory effects of Alzheimer's ß-secretase (BACE-1) were examined. The regio-selective sulfation was conducted on N-acetyl glucosamine (GlcNAc), and the acrylamide derivatives were synthesized with the consequent sulfated GlcNAc. The glycopolymers were synthesized with acrylamide using radical initiator. The glycopolymer with sulfated GlcNAc showed the strong inhibitory effect on BACE-1, and the inhibitory effects were dependent on the sulfation positions. Especially, glycopolymers carrying 3,4,6-O-sulfo-GlcNAc showed the strong inhibitory effect. The docking simulation suggested that glycopolymers bind to the active site of BACE-1.
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Base de dados:
MEDLINE
Assunto principal:
Acetilglucosamina
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Sulfatos
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Ácido Aspártico Endopeptidases
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Secretases da Proteína Precursora do Amiloide
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Glicosaminoglicanos
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article