Vicinal Disulfide Constrained Cyclic Peptidomimetics: a Turn Mimetic Scaffold Targeting the Norepinephrine Transporter
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Open Access
Type
ArticleAuthor/s
Brust, AndreasWang, Ching-I. A.
Daly, Norelle L.
Kennerly, Joe
Sadeghi, Mahsa
Christie, Macdonald J.
Lewis, Richard J.
Mobli, Mehdi
Alewood, Paul F.
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 (see scheme) show high structural and functional similarity to the parent peptide, though with superior metabolic stability.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 (see scheme) show high structural and functional similarity to the parent peptide, though with superior metabolic stability.
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Date
2013-09-24Publisher
WileyDepartment, Discipline or Centre
Discipline of PharmacologyCitation
Brust, A., Wang, C., Daly, N., Kennerly, J., Sadeghi, M., Christie, M., Lewis, R., Mobli, M., Alewood, P. (2013). Vicinal Disulfide Constrained Cyclic Peptidomimetics: a Turn Mimetic Scaffold Targeting the Norepinephrine Transporter. Angewandte Chemie (International Edition), 52(46), 12020-1202Share