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Antimicrobial Agents and Chemotherapy, February 2004, p. 663-665, Vol. 48, No. 2
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.2.663-665.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

Bifunctional Anti-Human Immunodeficiency Virus Type 1 Small Molecules with Two Novel Mechanisms of Action

Li Huang,1 Xiong Yuan,1 Christopher Aiken,2 and Chin Ho Chen1*

Department of Surgery, Duke University Medical Center, Durham, North Carolina 27710,1 Department of Microbiology and Immunology, Vanderbilt University School of Medicine, Nashville, Tennessee 372322

Received 25 July 2003/ Returned for modification 25 September 2003/ Accepted 4 November 2003

A class of betulinic acid derivatives was synthesized to target two critical steps in the human immunodeficiency virus type 1 (HIV-1) replication cycle, entry and maturation. Each mechanism of HIV-1 inhibition is distinct from clinically available anti-HIV therapeutics. The viral determinants of the antientry and antimaturation activities are the bridging sheet of HIV-1 gp120 and the P24/p2 cleavage site, respectively.

* Corresponding author. Mailing address: Duke University Medical Center, Surgical Oncology Research Facility, LaSalle Street Extension, Durham, NC 27710. Phone: (919) 684-3819. Fax: (919) 684-3878. E-mail: chc{at}acpub.duke.edu.

Antimicrobial Agents and Chemotherapy, February 2004, p. 663-665, Vol. 48, No. 2
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.2.663-665.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.





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Copyright © 2004 by the American Society for Microbiology. All rights reserved.