Vicinal disulfide constrained cyclic peptidomimetics: a turn mimetic scaffold targeting the norepinephrine transporter

Brust, Andreas, Wang, Ching-I.A., Daly, Norelle L., Kennerly, Joe, Sadeghi, Mahsa, Christie, Macdonald J., Lewis, Richard J., Mobli, Mehdi, and Alewood, Paul F. (2013) Vicinal disulfide constrained cyclic peptidomimetics: a turn mimetic scaffold targeting the norepinephrine transporter. Angewandte Chemie International Edition, 52 (46). pp. 12020-12023.

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Abstract

Loopy peptides: Peptide turn mimetics of a clinically relevant norepinephrine reuptake inhibitor were developed employing a high-throughput synthesis approach to generate peptide thioesters, with subsequent cyclization through native chemical ligation. The vicinal disulfide constrained cyclic peptidomimetics show high structural and functional similarity to the parent peptide, though with superior metabolic stability.

Item ID: 32111
Item Type: Article (Research - C1)
ISSN: 1521-3773
Keywords: biological activity; cyclic peptides; combinatorial chemistry; drug discovery; peptidomimetics
Date Deposited: 25 May 2014 23:50
FoR Codes: 03 CHEMICAL SCIENCES > 0304 Medicinal and Biomolecular Chemistry > 030401 Biologically Active Molecules @ 100%
SEO Codes: 97 EXPANDING KNOWLEDGE > 970103 Expanding Knowledge in the Chemical Sciences @ 100%
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