Volume 125, Issue 46 pp. 12242-12245
Zuschrift

Vicinal Disulfide Constrained Cyclic Peptidomimetics: a Turn Mimetic Scaffold Targeting the Norepinephrine Transporter

Dr. Andreas Brust

Corresponding Author

Dr. Andreas Brust

Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

Andreas Brust, Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

Mehdi Mobli, Centre for Advanced Imaging, The University of Queensland, St Lucia 4072 QLD (Australia)

Paul F. Alewood, Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

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Dr. Ching-I. A. Wang

Dr. Ching-I. A. Wang

Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

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Prof. Norelle L. Daly

Prof. Norelle L. Daly

Norelle Daly Centre for Biodiscovery and Molecular Development of Therapeutics, School of Pharmacy and Molecular Sciences, James Cook University, Cairns (Australia)

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Joe Kennerly

Joe Kennerly

Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

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Mahsa Sadeghi

Mahsa Sadeghi

Discipline of Pharmacology, University of Sydney (Australia)

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Prof. Macdonald J. Christie

Prof. Macdonald J. Christie

Discipline of Pharmacology, University of Sydney (Australia)

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Prof. Richard J. Lewis

Prof. Richard J. Lewis

Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

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Dr. Mehdi Mobli

Corresponding Author

Dr. Mehdi Mobli

Centre for Advanced Imaging, The University of Queensland, St Lucia 4072 QLD (Australia)

Andreas Brust, Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

Mehdi Mobli, Centre for Advanced Imaging, The University of Queensland, St Lucia 4072 QLD (Australia)

Paul F. Alewood, Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

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Prof. Paul F. Alewood

Corresponding Author

Prof. Paul F. Alewood

Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

Andreas Brust, Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

Mehdi Mobli, Centre for Advanced Imaging, The University of Queensland, St Lucia 4072 QLD (Australia)

Paul F. Alewood, Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)

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First published: 24 September 2013
Citations: 9

We acknowledge financial support by NHMRC (Program Grant No. 351446).

Graphical Abstract

Peptid mit Schleifchen: Peptidschleifen-Mimetika des klinisch relevanten Norepinephrin-Wiederaufnahmehemmers wurden mithilfe einer Hochdurchsatz-Synthese entwickelt, bei der Peptidthioester zunächst erzeugt und anschließend unter nativer chemischer Ligation cyclisiert werden. Die abgebildeten cyclischen Disulfid-Peptidmimetika sind in Struktur und Funktion dem Stammpeptid sehr ähnlich, aber deutlich stoffwechselbeständiger.

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