Acid-Triggered Colorimetric Hydrophobic Benzyl Alcohols for Soluble Tag-Assisted Liquid-Phase Synthesis
Simple screening of acid-triggered reactions of methoxybenzyl alcohols led to the development of a novel colorimetric hydrophobic benzyl alcohol (HBA) tag. HBA tag-3 (14) retained high solubility in less polar solvents and excellent precipitation properti
Okada, Yohei,Wakamatsu, Hiroki,Sugai, Masae,Kauppinen, Esko I.,Chiba, Kazuhiro
supporting information
p. 4264 - 4267
(2015/09/15)
Development of retro-inverso peptides as anti-aggregation drugs for β-amyloid in Alzheimer's disease
Alzheimer's disease (AD) is a devastating degenerative disorder of the brain for which there is no cure or effective treatment. There is much evidence to suggest that β-amyloid protein (Aβ) aggregation in the brain leading to deposits is an important step in the development of AD. Recently, two peptides, RGKLVFFGR (OR1) and RGKLVFFGR-NH2 (OR2) containing the sequence KLVFF, which is the central region (residues 16-20) of Aβ, have been found to be potent inhibitors of Aβ aggregate formation. Here we report that retro-inversion of these sequences increases efficacy of the peptides in the inhibition of aggregation and toxicity of β-amyloid. We describe the synthesis and inhibitory properties of these retro-inverso peptides.
Matharu, Balpreet,El-Agnaf, Omar,Razvi, Amna,Austen, Brian M.
experimental part
p. 1866 - 1872
(2011/01/12)
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