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.

journal_name

Bioorg Med Chem Lett

authors

Aboye TL,Li Y,Majumder S,Hao J,Shekhtman A,Camarero JA

doi

10.1016/j.bmcl.2012.02.080

subject

Has Abstract

pub_date

2012-04-15 00:00:00

pages

2823-6

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00281-8

journal_volume

22

pub_type

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