Antibiotic and anti-parasitic agents that modulate class II fructose 1,6-bisphosphate aldolase

This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivat...

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Hauptverfasser: AHRENDT KATERI, PEGAN SCOTT DUSAN, COWEN BRYAN, CAPODAGLI GLENN C
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creator AHRENDT KATERI
PEGAN SCOTT DUSAN
COWEN BRYAN
CAPODAGLI GLENN C
description This invention provides a family of compounds that inhibit Class II fructose 1,6-bisphosphate aldolase (FBA), which is implicated in the pathogenic activity of a broad range of bacterial and parasitic agents. The compounds were identified by empirical testing, and provide a basis for further derivatization and optimization of 8-hydroxyquinoline-2-carboxylic acid and related compounds. Crystal structure shows that the compounds don't bind directly to the catalytic site of the enzyme, and so are not defined simply as substrate analogs. Instead, they create a pocket by induced fit, resulting a powerful and specific inhibitory effect on FBA activity.
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subjects AGRICULTURE
ANIMAL HUSBANDRY
BEER
BIOCHEMISTRY
BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES
CHEMISTRY
COMPOSITIONS OR TEST PAPERS THEREFOR
CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES
ENZYMOLOGY
FISHING
FORESTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HUNTING
INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES
MEASURING
MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS
METALLURGY
MICROBIOLOGY
MUTATION OR GENETIC ENGINEERING
ORGANIC CHEMISTRY
PEST REPELLANTS OR ATTRACTANTS
PHYSICS
PLANT GROWTH REGULATORS
PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF
PROCESSES OF PREPARING SUCH COMPOSITIONS
SPIRITS
TESTING
TRAPPING
VINEGAR
WINE
title Antibiotic and anti-parasitic agents that modulate class II fructose 1,6-bisphosphate aldolase
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