Title: Design of a Novel Cyclotide-Based CXCR4 Antagonist with Anti-Human Immunodeficiency Virus (HIV)-1 Activity
Authors: Aboye, Teshome L ×
Ha, Helen
Majumder, Subhabrata
Christ, Frauke
Debyser, Zeger
Shekhtman, Alexander
Neamati, Nouri
Camarero, Julio A #
Issue Date: Nov-2012
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:55 issue:23 pages:10729-10734
Abstract: Herein, we report for the first time the design and synthesis of a novel cyclotide able to efficiently inhibit HIV-1 viral replication by selectively targeting cytokine receptor CXCR4. This was accomplished by grafting a series of topologically modified CVX15 based peptides onto the loop 6 of cyclotide MCoTI-I. The most active compound produced in this study was a potent CXCR4 antagonist (EC(50) ≈ 20 nM) and an efficient HIV-1 cell-entry blocker (EC(50) ≈ 2 nM). 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 anticancer and anti-HIV-1 therapeutics.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Virology and Gene Therapy
× corresponding author
# (joint) last author

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