Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
Publication
, Journal Article
Herath, KB; Jayasuriya, H; Bills, GF; Polishook, JD; Dombrowski, AW; Guan, Z; Felock, PJ; Hazuda, DJ; Singh, SB
Published in: J Nat Prod
May 2004
HIV-1 integrase is a critical enzyme for replication of HIV, and its inhibition is one of the most promising new drug targets for anti-retroviral therapy with potentially significant advantages over existing therapies. In this Note, the isolation, structure elucidation, and absolute stereochemistry of integrasone, a novel polyketide, derived from an unidentified sterile mycelium have been described. This bicyclic dihydroxy epoxide lactone inhibited the strand transfer reaction of HIV-1 integrase with an IC(50) of 41 microM.
Duke Scholars
Published In
J Nat Prod
DOI
ISSN
0163-3864
Publication Date
May 2004
Volume
67
Issue
5
Start / End Page
872 / 874
Location
United States
Related Subject Headings
- Stereoisomerism
- Nuclear Magnetic Resonance, Biomolecular
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- HIV-1
- HIV Integrase Inhibitors
- HIV Integrase
- Furans
- Fungi
Citation
APA
Chicago
ICMJE
MLA
NLM
Herath, K. B., Jayasuriya, H., Bills, G. F., Polishook, J. D., Dombrowski, A. W., Guan, Z., … Singh, S. B. (2004). Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide. J Nat Prod, 67(5), 872–874. https://doi.org/10.1021/np0340504
Herath, Kithsiri B., Hiranthi Jayasuriya, Gerald F. Bills, Jon D. Polishook, Anne W. Dombrowski, Ziqiang Guan, Peter J. Felock, Daria J. Hazuda, and Sheo B. Singh. “Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.” J Nat Prod 67, no. 5 (May 2004): 872–74. https://doi.org/10.1021/np0340504.
Herath KB, Jayasuriya H, Bills GF, Polishook JD, Dombrowski AW, Guan Z, et al. Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide. J Nat Prod. 2004 May;67(5):872–4.
Herath, Kithsiri B., et al. “Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.” J Nat Prod, vol. 67, no. 5, May 2004, pp. 872–74. Pubmed, doi:10.1021/np0340504.
Herath KB, Jayasuriya H, Bills GF, Polishook JD, Dombrowski AW, Guan Z, Felock PJ, Hazuda DJ, Singh SB. Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide. J Nat Prod. 2004 May;67(5):872–874.
Published In
J Nat Prod
DOI
ISSN
0163-3864
Publication Date
May 2004
Volume
67
Issue
5
Start / End Page
872 / 874
Location
United States
Related Subject Headings
- Stereoisomerism
- Nuclear Magnetic Resonance, Biomolecular
- Molecular Structure
- Medicinal & Biomolecular Chemistry
- Inhibitory Concentration 50
- HIV-1
- HIV Integrase Inhibitors
- HIV Integrase
- Furans
- Fungi