Water-soluble chitosan derivatives as a BACE1 inhibitor.
BACE1 (the beta-site APP-cleaving enzyme) inhibitory activities of water-soluble chitosan derivatives substituted with aminoethyl, dimethylaminoethyl and diethylaminoethyl groups were investigated. AE-chitosan (90%) prepared from 90% deacetylated chitosan showed the strongest BACE1 inhibitory activity than those of other derivatives. The inhibitory pattern was found to be non-competitive by Dixon plot, and the value of the inhibition constant (K(i)) was 85 microg/mL.
Je
Jae-Young
JY
Department of Chemistry, Pukyong National University, Busan, Republic of Korea.
Kim
Se-Kwon
SK
D053829:Amyloid Precursor Protein Secretases; D048271:Chitosan / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D010450:Endopeptidases / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water / Q000737:chemistry*
D004791:Enzyme Inhibitors; D014867:Water; D048271:Chitosan; D053829:Amyloid Precursor Protein Secretases; D010450:Endopeptidases