title: Efficient one-pot cyclization/folding of Rhesus θ-defensin-1 (RTD-1).
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.
authors.affiliation: Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, Los Angeles, CA 90033, USA.
authors.forename: Teshome L
authors.initials: TL
authors.lastname: Aboye
authors.forename: Yilong
authors.initials: Y
authors.lastname: Li
authors.forename: Subhabrata
authors.initials: S
authors.lastname: Majumder
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Hao
authors.forename: Alexander
authors.initials: A
authors.lastname: Shekhtman
authors.forename: Julio A
authors.initials: JA
authors.lastname: Camarero
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D020650:Combinatorial Chemistry Techniques; D003500:Cyclization; D023082:Defensins / Q000138:chemical synthesis* / Q000737:chemistry*; D008253:Macaca mulatta; D008969:Molecular Sequence Data; D010455:Peptides / Q000737:chemistry; D017510:Protein Folding; D060327:Solid-Phase Synthesis Techniques / Q000379:methods*
chemical_list: D023082:Defensins; D010455:Peptides; C450142:theta-defensin