New Families of Beta-Lactamase Inhibitors
Item
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Title
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New Families of Beta-Lactamase Inhibitors
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Identifier
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d_2009_2013:6ec59c78d61e:11024
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identifier
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11385
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Creator
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Gonzalez, Janet,
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Contributor
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Manfred Philipp
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Date
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2011
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Language
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English
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Publisher
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City University of New York.
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Subject
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Biochemistry | Pharmacology | beta-lactamase | enzyme | inhibitors
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Abstract
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A traditional approach to improving the efficacy of beta-lactam antibiotics has been to modify natural antibiotics by modifying the nucleus and adding various side chains. It is generally believed that beta-lactam based antibiotics have a limited future given increased resistance demonstrated by many strains of bacteria. Therefore the lack of performance among commonly used antibiotics against the rise of resistant bacterial strains has propelled researchers to look for novel types of antimicrobial agents and enzyme inhibitors as tools to combat this serious and growing threat. The focus of this research is to investigate novel small-molecules from different families with antibacterial properties such as peptides, aromatic ketones, biphenyl and stilbene compounds and boronic acids that demonstrate an inhibitory effect on class A beta-lactamase. Some of these inhibitors were found by screening natural products other were found by screening libraries of compounds and yet others were found by computational approaches involving molecular docking. Of all the compounds tested as long as the molecule was within hydrogen bonding distance of Ser84, Lys87 Ser142, Asn186, Gly252, Glu182 or Asp142, they demonstrated inhibitory effect which demonstrates that docking for this class of compounds is highly correlated with successful experimental inhibition.
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Type
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dissertation
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Source
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2009_2013.csv
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degree
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Ph.D.
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Program
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Biochemistry
