Development of retro-inverso peptides as anti-aggregation drugs for β-amyloid in Alzheimer's disease

Peptides
Balpreet MatharuBrian M Austen

Abstract

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-NH(2) (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.

References

Aug 6, 2005·Clinical Chemistry·Benjamin GodberMatthew A Cooper

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Citations

Feb 3, 2016·ACS Chemical Neuroscience·Sunil BansalRahul Jain
Dec 25, 2015·Molecular Therapy : the Journal of the American Society of Gene Therapy·Hayate JavedOmar M A El-Agnaf
Mar 15, 2015·Bioorganic & Medicinal Chemistry·Antonio FranciosoLuciana Mosca
Apr 22, 2015·Biomolecules·Afsaneh PorzoorIan Macreadie
Feb 2, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Samo Ribarič
Dec 13, 2017·Journal of Translational Medicine·Emily B MartinJonathan S Wall
May 4, 2017·Scientific Reports·Maria Vincenza CarrieroAntonello Pessi
Dec 6, 2020·International Journal of Biological Macromolecules·Hossein AshrafianRizwan Hasan Khan
Oct 4, 2020·Archives of Biochemistry and Biophysics·Amit Mitra, Nandini Sarkar
Sep 10, 2021·Future Medicinal Chemistry·Nibedita Ghosh, Lal Mohan Kundu

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