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Molecules 2016, 21(2), 152; doi:10.3390/molecules21020152

Design of a MCoTI-Based Cyclotide with Angiotensin (1-7)-Like Activity

1
Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, Los Angeles, CA 90089-9121, USA
2
Department of Chemistry, State University of New York, Albany, NY 12222, USA
3
Department of Chemistry, University of Southern California, Los Angeles, CA 90089-9121, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 28 December 2015 / Revised: 20 January 2016 / Accepted: 22 January 2016 / Published: 26 January 2016
View Full-Text   |   Download PDF [2826 KB, uploaded 26 January 2016]   |  

Abstract

We report for the first time the design and synthesis of a novel cyclotide able to activate the unique receptor of angiotensin (1-7) (AT1-7), the MAS1 receptor. This was accomplished by grafting an AT1-7 peptide analog onto loop 6 of cyclotide MCoTI-I using isopeptide bonds to preserve the α-amino and C-terminal carboxylate groups of AT1-7, which are required for activity. The resulting cyclotide construct was able to adopt a cyclotide-like conformation and showed similar activity to that of AT1-7. This cyclotide also showed high stability in human serum thereby providing a promising lead compound for the design of a novel type of peptide-based in the treatment of cancer and myocardial infarction. View Full-Text
Keywords: cyclotide; MAS1 receptor; angiotensin cyclotide; MAS1 receptor; angiotensin
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MDPI and ACS Style

Aboye, T.; Meeks, C.J.; Majumder, S.; Shekhtman, A.; Rodgers, K.; Camarero, J.A. Design of a MCoTI-Based Cyclotide with Angiotensin (1-7)-Like Activity. Molecules 2016, 21, 152.

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