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Clicked tacrine con...
Clicked tacrine conjugates as acetylcholinesterase and β-amyloid directed compounds
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Ouberai, Myriam (author)
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- Brännström, Kristoffer (author)
- Umeå universitet,Institutionen för medicinsk kemi och biofysik
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- Vestling, Monika (author)
- Umeå universitet,Institutionen för medicinsk kemi och biofysik
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- Olofsson, Anders, 1970- (author)
- Umeå universitet,Institutionen för medicinsk kemi och biofysik,Anders Olofsson
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Dumy, Pascal (author)
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Chierici, Sabine (author)
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Garcia, Julian (author)
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(creator_code:org_t)
- 2011
- 2011
- English.
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In: Organic and biomolecular chemistry. - : The Royal Society of Chemistry. - 1477-0520 .- 1477-0539. ; 9:4, s. 1140-1147
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
Keyword
- Biochemistry
- Biokemi
- Biochemistry
- biokemi
Publication and Content Type
- ref (subject category)
- art (subject category)
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