Inhibition of HIV Fusion with Multivalent Gold Nanoparticles

The design and synthesis of a multivalent gold nanoparticle therapeutic is presented. SDC-1721, a fragment of the potent HIV inhibitor TAK-779, was synthesized and conjugated to 2.0 nm diameter gold nanoparticles. Free SDC-1721 had no inhibitory effect on HIV infection; however, the (SDC-1721)−gold...

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Bibliographic Details
Published in:Journal of the American Chemical Society 2008-06, Vol.130 (22), p.6896-6897
Main Authors: Bowman, Mary-Catherine, Ballard, T. Eric, Ackerson, Christopher J, Feldheim, Daniel L, Margolis, David M, Melander, Christian
Format: Article
Language:English
Subjects:
Amides - chemistry
Amides - pharmacology
Gold - chemistry
Gold - pharmacology
HIV Fusion Inhibitors - chemistry
HIV Fusion Inhibitors - pharmacology
HIV Infections - drug therapy
HIV-1 - physiology
Human immunodeficiency virus
Metal Nanoparticles - chemistry
Metal Nanoparticles - therapeutic use
Quaternary Ammonium Compounds - chemistry
Quaternary Ammonium Compounds - pharmacology
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Summary:The design and synthesis of a multivalent gold nanoparticle therapeutic is presented. SDC-1721, a fragment of the potent HIV inhibitor TAK-779, was synthesized and conjugated to 2.0 nm diameter gold nanoparticles. Free SDC-1721 had no inhibitory effect on HIV infection; however, the (SDC-1721)−gold nanoparticle conjugates displayed activity comparable to that of TAK-779. This result suggests that multivalent presentation of small molecules on gold nanoparticle surfaces can convert inactive drugs into potent therapeutics.
ISSN:0002-7863
1272-7863
1520-5126
DOI:10.1021/ja710321g