Introducing lasso peptides as molecular scaffolds for drug design: Engineering of an integrin antagonist

Thomas A. Knappe; Florian Manzenrieder; Carlos Mas-Moruno; Uwe Linne; Florenz Sasse; Horst Kessler; Xiulan Xie; Mohamed A. Marahiel

doi:10.1002/anie.201102190

Introducing lasso peptides as molecular scaffolds for drug design: Engineering of an integrin antagonist

Thomas A. Knappe, Florian Manzenrieder, Carlos Mas-Moruno, Uwe Linne, Florenz Sasse, Horst Kessler, Xiulan Xie, Mohamed A. Marahiel

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Abstract

Tightening the noose: Lasso peptides are a class of stable bacterial peptides with unique characteristics that encourage their application in drug design. Epitope grafting of the integrin binding motif RGD onto the lasso structure of microcin J25 converts the knotted peptide into a nanomolar integrin antagonist (see picture). Engineered lasso peptides can therefore be used for pharmacophore presentation.

Original language	English
Pages (from-to)	8714-8717
Number of pages	4
Journal	Angewandte Chemie International Edition in English
Volume	50
Issue number	37
DOIs	https://doi.org/10.1002/anie.201102190
State	Published - 5 Sep 2011

Keywords

drug design
epitope grafting
integrin inhibitors
lasso peptides
molecular scaffolds

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10.1002/anie.201102190

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abstract = "Tightening the noose: Lasso peptides are a class of stable bacterial peptides with unique characteristics that encourage their application in drug design. Epitope grafting of the integrin binding motif RGD onto the lasso structure of microcin J25 converts the knotted peptide into a nanomolar integrin antagonist (see picture). Engineered lasso peptides can therefore be used for pharmacophore presentation.",

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AU - Linne, Uwe

AU - Sasse, Florenz

AU - Kessler, Horst

AU - Xie, Xiulan

AU - Marahiel, Mohamed A.

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KW - molecular scaffolds

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Introducing lasso peptides as molecular scaffolds for drug design: Engineering of an integrin antagonist

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Keywords

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