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Bioorg Med Chem Lett. 2012 Apr 15;22(8):2823-6. doi: 10.1016/j.bmcl.2012.02.080. Epub 2012 Mar 2.

Efficient one-pot cyclization/folding of Rhesus θ-defensin-1 (RTD-1).

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  • 1Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, Los Angeles, CA 90033, USA.

Abstract

We report an efficient approach for the chemical synthesis of Rhesus θ-defensin-1 (RTD-1) using Fmoc-based solid-phase peptide synthesis in combination with an intramolecular version of native chemical ligation. The corresponding linear thioester precursor was cyclized and folded in a one-pot reaction using reduced glutathione. The reaction was extremely efficiently yielding natively folded RTD-1 with minimal or no purification at all. This approach is fully compatible with the high throughput production of chemical libraries using this peptide scaffold.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
22425570
[PubMed - indexed for MEDLINE]
PMCID:
PMC3590006
Free PMC Article
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