Enhancement of Anti-HIV-1 Activity by Hot Spot Evolution of RANTES-Derived Peptides

Secchi, Massimiliano and Longhi, Renato and Vassena, Lia and Sironi, Francesca and Grzesiek, Stephan and Lusso, Paolo and Vangelista, Luca. (2012) Enhancement of Anti-HIV-1 Activity by Hot Spot Evolution of RANTES-Derived Peptides. Chemistry & Biology, 19 (12). pp. 1579-1588.

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Official URL: http://edoc.unibas.ch/dok/A6070333

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CCR5, the major HIV-1 coreceptor, is a primary target for HIV-1 entry inhibition strategies. CCL5/RANTES, a natural CCR5 ligand, is one of the most potent HIV-1 entry inhibitors and, therefore, an ideal candidate to derive HIV-1 blockers. Peptides spanning the RANTES N-loop/β1-strand region act as specific CCR5 antagonists, with their hydrophobic N- and C termini playing a crucial role in virus blockade. Here, hydrophobic surfaces were enhanced by tryptophan substitution of aromatic residues, highlighting position 27 as a critical hot spot for HIV-1 blockade. In a further molecular evolution step, C-terminal engraftment of RANTES 40' loop produced a peptide with the highest solubility and anti-HIV-1 activity. These modified peptides represent leads for the development of effective HIV-1 inhibitors and microbicides.
Faculties and Departments:05 Faculty of Science > Departement Biozentrum > Structural Biology & Biophysics > Structural Biology (Grzesiek)
UniBasel Contributors:Grzesiek, Stephan
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Cell Press
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:23 Nov 2017 15:41
Deposited On:01 Mar 2013 11:09

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