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Selectively N‐Methylated Soluble IAPP Mimics as Potent IAPP Receptor Agonists and Nanomolar Inhibitors of Cytotoxic Self‐Assembly of Both IAPP and Aβ40
Author(s) -
Yan LiMei,
Velkova Aleksandra,
TatarekNossol Marianna,
Rammes Gerhard,
Sibaev Andrei,
Andreetto Erika,
Kracklauer Michael,
Bakou Maria,
Malideli Eleni,
Göke Burkhard,
Schirra Jörg,
Storr Martin,
Kapurniotu Aphrodite
Publication year - 2013
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201302840
Subject(s) - chemistry , cytotoxic t cell , amyloid (mycology) , peptide , islet , biochemistry , receptor , amylin , cytotoxicity , in vitro , biology , endocrinology , insulin , inorganic chemistry
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).