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Clicked tacrine conjugates as acetylcholinesterase and β-amyloid directed compounds
Umeå University, Faculty of Medicine, Department of Medical Biochemistry and Biophysics.
Umeå University, Faculty of Medicine, Department of Medical Biochemistry and Biophysics.
Umeå University, Faculty of Medicine, Department of Medical Biochemistry and Biophysics. (Anders Olofsson)
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2011 (English)In: Organic and biomolecular chemistry, ISSN 1477-0520, E-ISSN 1477-0539, Vol. 9, no 4, 1140-1147 p.Article in journal (Refereed) Published
Abstract [en]

The multifaceted nature of Alzheimer's disease (AD) has led to the development of multi-targeted compounds based on the classical AD drug, tacrine, first known to inhibit the acetylcholine-degrading enzyme acetylcholinesterase (AChE). In the present work, we explore the potentiality of multimers of tacrine in this field. The synthesis using the so-called "click chemistry" and the in vitro study of the conjugates are described. Two or four copies of the tacrine molecule are "clicked" on a constrained cyclopeptide template proven to be a convenient tool for multimeric presentation. The multimers significantly inhibit self-induced amyloid fibril formation from Aβ(40) at low inhibitor to Aβ molar ratios at which the tacrine monomer is fully inactive (Thioflavin T assays and AFM observation). Moreover, they have the capacity to bind to Aβ(40) fibrils (SPR assays) while retaining the AChE inhibitory activity of the parent tacrine.

Place, publisher, year, edition, pages
The Royal Society of Chemistry , 2011. Vol. 9, no 4, 1140-1147 p.
National Category
Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)
Research subject
Biochemistry
Identifiers
URN: urn:nbn:se:umu:diva-40239DOI: 10.1039/c0ob00393jOAI: oai:DiVA.org:umu-40239DiVA: diva2:398639
Funder
Swedish Research Council
Available from: 2011-02-21 Created: 2011-02-18 Last updated: 2017-12-11Bibliographically approved

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Brännström, KristofferVestling, MonikaOlofsson, Anders
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