8 research outputs found
Cocaine Esterase Prevents Cocaine-Induced Toxicity and the Ongoing Intravenous Self-Administration of Cocaine in Rats
No full textThermostable Variants of Cocaine Esterase for Long-Time Protection against Cocaine Toxicity
No full textEnhancing cocaine metabolism by administration of cocaine esterase (CocE)
has been recognized as a promising treatment strategy for cocaine overdose and
addiction, because CocE is the most efficient native enzyme for metabolizing
the naturally occurring cocaine yet identified. A major obstacle to the
clinical application of CocE is the thermoinstability of native CocE with a
half-life of only a few minutes at physiological temperature (37°C). Here
we report thermostable variants of CocE developed through rational design
using a novel computational approach followed by in vitro and in vivo studies.
This integrated computational-experimental effort has yielded a CocE variant
with a ∼30-fold increase in plasma half-life both in vitro and in vivo.
The novel design strategy can be used to develop thermostable mutants of any
protein
The Fate of Bacterial Cocaine Esterase (CocE): An In Vivo Study of CocE-Mediated Cocaine Hydrolysis, CocE Pharmacokinetics, and CocE Elimination
No full textThe Ability of Bacterial Cocaine Esterase to Hydrolyze Cocaine Metabolites and Their Simultaneous Quantification Using High-Performance Liquid Chromatography-Tandem Mass Spectrometry
No full textA Thermally Stable Form of Bacterial Cocaine Esterase: A Potential Therapeutic Agent for Treatment of Cocaine Abuse
No full textThe potential benefit of the placebo effect in sham-controlled trials: implications for risk-benefit assessments and informed consent
No full text
