Integracides: tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium sp |
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Authors: | Singh Sheo B Zink Deborah L Dombrowski Anne W Polishook Jon D Ondeyka John G Hirshfield Jorden Felock Peter Hazuda Daria J |
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Affiliation: | Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. sheo_singh@merck.com |
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Abstract: | HIV-1 integrase is a critical enzyme in the replication of HIV-1. It is absent in the host cells and therefore is a good target for treatment of HIV-1 infections. Integracides are members of the tetracyclic triterpenoids family that were isolated from the fermentation broth of a Fusarium sp. Integracide A, a sulfated ester, exhibited significant inhibitory activity against strand transfer reaction of HIV-1 integrase. The discovery, structure elucidation including single crystal X-ray structure and HIV-1 inhibitory activity of these compounds are described. |
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