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

Authors

  • Dr. Andreas Brust,

    Corresponding author
    1. 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,

    1. Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)
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  • Prof. Norelle L. Daly,

    1. 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,

    1. Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)
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  • Mahsa Sadeghi,

    1. Discipline of Pharmacology, University of Sydney (Australia)
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  • Prof. Macdonald J. Christie,

    1. Discipline of Pharmacology, University of Sydney (Australia)
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  • Prof. Richard J. Lewis,

    1. Institute of Molecular Bioscience, The University of Queensland, St Lucia QLD 4072 (Australia)
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  • Dr. Mehdi Mobli,

    Corresponding author
    1. 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
    1. 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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  • We acknowledge financial support by NHMRC (Program Grant No. 351446).

Abstract

original image

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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