Selectively N‐Methylated Soluble IAPP Mimics as Potent IAPP Receptor Agonists and Nanomolar Inhibitors of Cytotoxic Self‐Assembly of Both IAPP and Aβ40

Limei Yan, Aleksandra Velkova, Marianna Tatarek‐Nossol, Gerhard Rammes, Andrei Sibaev, Erika Andreetto, Michael Kracklauer, Maria Bakou, Eleni Malideli, Burkhard Göke,

Angewandte Chemie International Edition · 2013 · 53 citations · 25 references

Concepts

Abstract

The selective incorporation of N-methyl groups in the highly amyloidogenic and cytotoxic sequence of the type 2 diabetes islet amyloid polypeptide (IAPP) generates a unique class of soluble and nontoxic IAPP mimics. These polypeptides combine potent IAPP receptor agonism with nanomolar-affinity inhibitory potential on the amyloid formation and cell-damaging effects of both IAPP and the Alzheimer's β-amyloid peptide (Aβ40).

References

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