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

ABSTRACT: We report an efficient approach for the chemical synthesis of Rhesus ?-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.

SUBMITTER: Aboye TL

PROVIDER: S-EPMC3590006 | biostudies-literature | 2012 Apr

REPOSITORIES: biostudies-literature

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

Aboye Teshome L TL Li Yilong Y Majumder Subhabrata S Hao Jinfeng J Shekhtman Alexander A Camarero Julio A JA

Bioorganic & medicinal chemistry letters 20120302 8

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 p ...[more]

PMID: 22425570

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