Design of a MCoTI-Based Cyclotide with Angiotensin (1-7)-Like Activity
| Autor: | Alexander Shekhtman, Subhabrata Majumder, Christopher J. Meeks, Teshome Leta Aboye, Kathleen E. Rodgers, Julio A. Camarero |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Protein Folding cyclotide Stereochemistry Cell Survival Protein Conformation Myocardial Infarction Pharmaceutical Science Peptide Cyclotides CHO Cells Proto-Oncogene Mas Article Analytical Chemistry Receptors G-Protein-Coupled lcsh:QD241-441 03 medical and health sciences MAS1 receptor angiotensin Protein structure Cricetulus lcsh:Organic chemistry Neoplasms Proto-Oncogene Proteins Drug Discovery Animals Humans Physical and Theoretical Chemistry Receptor Plant Proteins chemistry.chemical_classification Peptide analog biology Chemistry Protein Stability Organic Chemistry biology.organism_classification Peptide Fragments 3. Good health Cyclotide 030104 developmental biology Biochemistry Chemistry (miscellaneous) Molecular Medicine Protein folding Angiotensin I |
| Zdroj: | Molecules, Vol 21, Iss 2, p 152 (2016) Molecules; Volume 21; Issue 2; Pages: 152 Molecules (Basel, Switzerland) |
| ISSN: | 1420-3049 |
| Popis: | 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 AT 1–7 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. |
| Databáze: | OpenAIRE |
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