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Isolation and Structure of Antagonists of Chemokine Receptor (CCR5)

descriptionPublicationkeyboard_double_arrow_right Article 13 May 2004Publisher:American Chemical Society (ACS)Journal:Journal of Natural Products, volume 67, pages 1,036-1,038 (issn: 0163-3864, eissn: 1520-6025,

Authors: S J Siciliano; Marty S Springer; Lorraine Malkowitz; Robert P. Borris; Gerald F. Bills; John G. Ondeyka; Ziqiang Guan; +8 Authors

doi: 10.1021/np049974l

pmid: 15217290

Isolation and Structure of Antagonists of Chemokine Receptor (CCR5)

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Abstract

Human CCR5 is a G-coupled receptor that binds to the envelope protein gp120 and CD4 and mediates the HIV-1 viral entry into the cells. The blockade of this binding by a small molecule receptor antagonist could lead to a new mode of action agent for HIV-1 and AIDS. Screening of natural product extracts led to the identification of anibamine (1), a novel pyridine quaternary alkaloid as a TFA salt, from Aniba sp.; ophiobolin C from fermentation extracts of fungi Mollisia sp.; and 19,20-epoxycytochalasin Q from Xylaria sp. Formation of the TFA salt of anibamine is plausibly an artifact of the isolation. The identity of the natural counterion is unknown. Anibamine.TFA competed for the binding of 125I-gp120 to human CCR5 with an IC50 of 1 microM. Ophiobolin C and 19,20-epoxycytochalasin Q exhibited binding IC50) values of 40 and 60 microM, respectively.

Related Organizations

New York Botanical Garden
United States
Merck & Co.
United States

Keywords

Sesterterpenes, Molecular Structure, Pyridines, Terpenes, Fungi, HIV Envelope Protein gp120, Cytochalasins, Inhibitory Concentration 50, Lauraceae, CCR5 Receptor Antagonists, CD4 Antigens, Humans

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3 Research products, page 1 of 1

Comparative Docking Study of Anibamine as the First Natural Product CCR5 Antagonist in CCR5 Homology Models
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