HIV-1 protease inhibitory activity of L-694,746, a novel metabolite of L-689,502

L-689,502 is a potent inhibitor of HIV-1 protease activity in vitro. Microbial biotransformations of L-689,502 by cultures belonging to the genus Streptomyces sp. were performed. Extracts of culture broths were examined for the production of metabolites of L-689,502 that could inhibit HIV-1 protease...

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Published inBiochemical and biophysical research communications Vol. 181; no. 3; pp. 1456 - 1461
Main Authors Lingham, Russell B., Arison, Byron H., Colwell, Lawerence F., Hsu, Amy, Dezeny, Georgette, Thompson, Wayne J., Garrity, George M., Gagliardi, Magda M., Hartner, Frederick W., Darke, Paul L., Balani, Suresh K., Pitzenberger, Steven M., Murphy, Joan S., Ramjit, Harri G., Inamine, Edward S., Treiber, Laszlo R.
Format Journal Article
LanguageEnglish
Published San Diego, CA Elsevier Inc 31.12.1991
Elsevier
Subjects
AIDS/HIV
Amino Acid Sequence
Analytical, structural and metabolic biochemistry
Biological and medical sciences
Biotransformation
Chromatography, High Pressure Liquid
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
HIV Protease Inhibitors
HIV-1 - enzymology
human immunodeficiency virus 1
Hydrolases
inhibition
Kinetics
L-694,746
Molecular Sequence Data
Molecular Structure
Morpholines - metabolism
Morpholines - pharmacology
Oligopeptides - chemical synthesis
Oligopeptides - metabolism
Pepstatins - pharmacology
Peptides - metabolism
Peptides - pharmacology
Protease Inhibitors - pharmacology
proteinase
Streptomyces - metabolism
Virus
Enzymatic activity
HIV-1 virus
Enzyme
Biotransformation
Proteinase
Retroviridae
Lentivirinae
Human immunodeficiency virus
Inhibition
In vitro
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Summary:L-689,502 is a potent inhibitor of HIV-1 protease activity in vitro. Microbial biotransformations of L-689,502 by cultures belonging to the genus Streptomyces sp. were performed. Extracts of culture broths were examined for the production of metabolites of L-689,502 that could inhibit HIV-1 protease activity. One culture, MA 6804 ( Streptomyces lavendulae, ATCC 55095), produced L-694,746 that, while being structurally related to L-689,502, is a novel metabolite and a potent inhibitor of HIV-1 protease.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0006-291X
1090-2104
DOI:10.1016/0006-291X(91)92103-Q