Mutation

Kinetic parameters

Tree Display

AceDB Schema

XML Display

Feedback

Mutation Report for: A199S/S287G/A328W/Y332G_human-BCHE

A199S/S287G/A328W/Y332G_human-BCHE
Gene_Locus|human-BCHE
Mode of mutation|Site directed mutagenesis
Amino Acid change|A199S/S287G/A328W/Y332G
Torpedo number|201//289//330//334//201,289,330,334
Summary|
Comment|p.A199S/S287G/A328W/Y332G Ala199Ser/Ser287Gly/Ala328Trp/Tyr332Gly (p.A227S/S315G/A356W/Y360G Ala227Ser/Ser315Gly/Ala356Trp/Tyr360Gly in primary sequence with 28 amino-acids signal peptide) CocH1 This mutant fused at its C terminus with human serum albumin to improve stability and extend plasma half-life was developed by CoGenesys, Inc. (Rockville, MD, USA). This construct (albuCocH, known as TV-1380 since Teva Pharmaceuticals acquired CoGenesys in 2008)
Kinetic parameters|none


References:
    Title: Kinetic characterization of cholinesterases and a therapeutically valuable cocaine hydrolase for their catalytic activities against heroin and its metabolite 6-monoacetylmorphine
    Kim K, Yao J, Jin Z, Zheng F, Zhan CG
    Ref: Chemico-Biological Interactions, 293:107, 2018 : PubMed

            

    Title: Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects
    Cohen-Barak O, Wildeman J, van de Wetering J, Hettinga J, Schuilenga-Hut P, Gross A, Clark S, Bassan M, Gilgun-Sherki Y and Spiegelstein O <1 more author(s)>
    Ref: Journal of Clinical Pharmacology, 55:573, 2015 : PubMed

            

    Title: Kinetic characterization of high-activity mutants of human butyrylcholinesterase for the cocaine metabolite norcocaine
    Zhan M, Hou S, Zhan CG, Zheng F
    Ref: Biochemical Journal, 457:197, 2014 : PubMed

            

    Title: Pharmacokinetic strategies for treatment of drug overdose and addiction
    Gorelick DA
    Ref: Future Med Chem, 4:227, 2012 : PubMed

            

    Title: Effects of cocaine hydrolase on cocaine self-administration under a PR schedule and during extended access (escalation) in rats
    Carroll ME, Gao Y, Brimijoin S, Anker JJ
    Ref: Psychopharmacology (Berl), 213:817, 2011 : PubMed

            

    Title: Characterization of a high-activity mutant of human butyrylcholinesterase against (-)-cocaine
    Yang W, Xue L, Fang L, Chen X, Zhan CG
    Ref: Chemico-Biological Interactions, 187:148, 2010 : PubMed

            

    Title: Design of high-activity mutants of human butyrylcholinesterase against (-)-cocaine: structural and energetic factors affecting the catalytic efficiency
    Zheng F, Yang W, Xue L, Hou S, Liu J, Zhan CG
    Ref: Biochemistry, 49:9113, 2010 : PubMed

            

    Title: A cocaine hydrolase engineered from human butyrylcholinesterase selectively blocks cocaine toxicity and reinstatement of drug seeking in rats
    Brimijoin S, Gao Y, Anker JJ, Gliddon LA, Lafleur D, Shah R, Zhao Q, Singh M, Carroll ME
    Ref: Neuropsychopharmacology, 33:2715, 2008 : PubMed

            

    Title: Computational redesign of human butyrylcholinesterase for anticocaine medication
    Pan Y, Gao D, Yang W, Cho H, Yang G, Tai HH, Zhan CG
    Ref: Proc Natl Acad Sci U S A, 102:16656, 2005 : PubMed

            




Send your questions or comments to :
Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.
Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
For technical information about these pages see:
ESTHER Home Page and ACEDB Home Page
AcePerl Lincoln Stein Home Page
webmaster

Acknowledgements and disclaimer