Scholars@Duke publication: Isolation and structure of antagonists of chemokine receptor (CCR5).

Isolation and structure of antagonists of chemokine receptor (CCR5).

Publication , Journal Article

Jayasuriya, H; Herath, KB; Ondeyka, JG; Polishook, JD; Bills, GF; Dombrowski, AW; Springer, MS; Siciliano, S; Malkowitz, L; Sanchez, M; Guan, Z ...

Published in: J Nat Prod

June 2004

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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.

Duke Scholars

Author Ziqiang Guan Biochemistry

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Published In

J Nat Prod

DOI

10.1021/np049974l

ISSN

0163-3864

Publication Date

June 2004

Volume

Issue

Start / End Page

1036 / 1038

Location

United States

Related Subject Headings

Terpenes
Sesterterpenes
Pyridines
Molecular Structure
Medicinal & Biomolecular Chemistry
Lauraceae
Inhibitory Concentration 50
Humans
HIV Envelope Protein gp120
Fungi

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APA

Chicago

ICMJE

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NLM

Jayasuriya, H., Herath, K. B., Ondeyka, J. G., Polishook, J. D., Bills, G. F., Dombrowski, A. W., … Singh, S. B. (2004). Isolation and structure of antagonists of chemokine receptor (CCR5). J Nat Prod, 67(6), 1036–1038. https://doi.org/10.1021/np049974l

Jayasuriya, Hiranthi, Kithsiri B. Herath, John G. Ondeyka, Jon D. Polishook, Gerald F. Bills, Anne W. Dombrowski, Marty S. Springer, et al. “Isolation and structure of antagonists of chemokine receptor (CCR5).” J Nat Prod 67, no. 6 (June 2004): 1036–38. https://doi.org/10.1021/np049974l.

Jayasuriya H, Herath KB, Ondeyka JG, Polishook JD, Bills GF, Dombrowski AW, et al. Isolation and structure of antagonists of chemokine receptor (CCR5). J Nat Prod. 2004 Jun;67(6):1036–8.

Jayasuriya, Hiranthi, et al. “Isolation and structure of antagonists of chemokine receptor (CCR5).” J Nat Prod, vol. 67, no. 6, June 2004, pp. 1036–38. Pubmed, doi:10.1021/np049974l.

Jayasuriya H, Herath KB, Ondeyka JG, Polishook JD, Bills GF, Dombrowski AW, Springer MS, Siciliano S, Malkowitz L, Sanchez M, Guan Z, Tiwari S, Stevenson DW, Borris RP, Singh SB. Isolation and structure of antagonists of chemokine receptor (CCR5). J Nat Prod. 2004 Jun;67(6):1036–1038.

Published In

J Nat Prod

DOI

10.1021/np049974l

ISSN

0163-3864

Publication Date

June 2004

Volume

Issue

Start / End Page

1036 / 1038

Location

United States

Related Subject Headings

Terpenes
Sesterterpenes
Pyridines
Molecular Structure
Medicinal & Biomolecular Chemistry
Lauraceae
Inhibitory Concentration 50
Humans
HIV Envelope Protein gp120
Fungi