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Grifonin-1: A Small HIV-1 Entry Inhibitor Derived from the Algal Lectin, Griffithsin

Micewicz, Ewa D. and Cole, Amy L. and Jung, Chun-Ling and Luong, Hai and Phillips, Martin L and Pratikhya, Pratikhya and Sharma, Shantanu and Waring, Alan J. and Cole, Alexander M. and Ruchala, Piotr (2010) Grifonin-1: A Small HIV-1 Entry Inhibitor Derived from the Algal Lectin, Griffithsin. PLoS ONE, 5 (12). Art. No. e14360. ISSN 1932-6203. PMCID PMC3002932.

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Background: Griffithsin, a 121-residue protein isolated from a red algal Griffithsia sp., binds high mannose N-linked glycans of virus surface glycoproteins with extremely high affinity, a property that allows it to prevent the entry of primary isolates and laboratory strains of T- and M-tropic HIV-1. We used the sequence of a portion of griffithsin's sequence as a design template to create smaller peptides with antiviral and carbohydrate-binding properties. Methodology/Results: The new peptides derived from a trio of homologous β-sheet repeats that comprise the motifs responsible for its biological activity. Our most active antiviral peptide, grifonin-1 (GRFN-1), had an EC50 of 190.8±11.0 nM in in vitro TZM-bl assays and an EC50 of 546.6±66.1 nM in p24gag antigen release assays. GRFN-1 showed considerable structural plasticity, assuming different conformations in solvents that differed in polarity and hydrophobicity. Higher concentrations of GRFN-1 formed oligomers, based on intermolecular β-sheet interactions. Like its parent protein, GRFN-1 bound viral glycoproteins gp41 and gp120 via the N-linked glycans on their surface. Conclusion: Its substantial antiviral activity and low toxicity in vitro suggest that GRFN-1 and/or its derivatives may have therapeutic potential as topical and/or systemic agents directed against HIV-1.

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Additional Information:© 2010 Micewicz et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Received July 2, 2010; Accepted November 22, 2010; Published December 16, 2010. Editor: Cheryl A. Stoddart, University of California San Francisco, United States of America. Funding: These studies were supported, in part, by funds from the Adams and Burnham endowments provided by the Dean’s Office of the David Geffen School of Medicine at University of California at Los Angeles (PR) and by National Institutes of Health grants #AI-052017 and #AI082623 (to AMC). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript. We thank Dr. Robert I. Lehrer for critical reading of the manuscript and helpful discussions. Author Contributions: Conceived and designed the experiments: PPR. Performed the experiments: EDM ALC CLJ HL MLP PP SS AJW AMC PPR. Analyzed the data: EDM ALC CLJ HL MLP PP SS AJW AMC PPR. Contributed reagents/materials/analysis tools: AMC PPR. Wrote the paper: EDM PPR.
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University of California Los Angeles (UCLA)UNSPECIFIED
Issue or Number:12
PubMed Central ID:PMC3002932
Record Number:CaltechAUTHORS:20110125-105140147
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Official Citation:Micewicz ED, Cole AL, Jung C-L, Luong H, Phillips ML, et al. (2010) Grifonin-1: A Small HIV-1 Entry Inhibitor Derived from the Algal Lectin, Griffithsin. PLoS ONE 5(12): e14360. doi:10.1371/journal.pone.0014360
Usage Policy:No commercial reproduction, distribution, display or performance rights in this work are provided.
ID Code:21879
Deposited By: Tony Diaz
Deposited On:25 Jan 2011 21:59
Last Modified:03 Oct 2019 02:30

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