Title |
‘Click’ assembly of glycoclusters and discovery of a trehalose analogue that retards Aβ40 aggregation and inhibits Aβ40-induced neurotoxicity
|
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Published in |
Bioorganic & Medicinal Chemistry Letters, August 2014
|
DOI | 10.1016/j.bmcl.2014.07.077 |
Pubmed ID | |
Authors |
Hemalatha Rajaram, Manoj Kumar Palanivelu, Thiruma V. Arumugam, Venkatesan M. Rao, P. Nicholas Shaw, Ross P. McGeary, Benjamin P. Ross |
Abstract |
Osmolytes have been proposed as treatments for neurodegenerative proteinopathies including Alzheimer's disease. However, for osmolytes to reach the clinic their efficacy must be improved. In this work, copper(I)-catalyzed azide-alkyne cycloaddition chemistry was used to synthesize glycoclusters bearing six copies of trehalose, lactose, galactose or glucose, with the aim of improving the potency of these osmolytes via multivalency. A trehalose glycocluster was found to be superior to monomeric trehalose in its ability to retard the formation of amyloid-beta peptide 40 (Aβ40) fibrils and protect neurons from Aβ40-induced cell death. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 27 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Researcher | 9 | 33% |
Student > Ph. D. Student | 4 | 15% |
Student > Doctoral Student | 3 | 11% |
Other | 2 | 7% |
Student > Master | 1 | 4% |
Other | 2 | 7% |
Unknown | 6 | 22% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 5 | 19% |
Biochemistry, Genetics and Molecular Biology | 3 | 11% |
Pharmacology, Toxicology and Pharmaceutical Science | 2 | 7% |
Medicine and Dentistry | 2 | 7% |
Agricultural and Biological Sciences | 1 | 4% |
Other | 4 | 15% |
Unknown | 10 | 37% |