Cocrystallization studies of full-length recombinant butyrylcholinesterase (BChE) with cocaine.
Acta Crystallogr Sect F Struct Biol Cryst Commun
; 67(Pt 4): 434-7, 2011 Apr 01.
Article
em En
| MEDLINE
| ID: mdl-21505234
ABSTRACT
Human butyrylcholinesterase (BChE; EC 3.1.1.8) is a 340â
kDa tetrameric glycoprotein that is present in human serum at about 5â
mgâ
l(-1) and has well documented therapeutic effects on cocaine toxicity. BChE holds promise as a therapeutic that reduces and finally eliminates the rewarding effects of cocaine, thus weaning an addict from the drug. There have been extensive computational studies of cocaine hydrolysis by BChE. Since there are no reported structures of BChE with cocaine or any of the hydrolysis products, full-length monomeric recombinant wild-type BChE was cocrystallized with cocaine. The refined 3â
Å resolution structure appears to retain the hydrolysis product benzoic acid in sufficient proximity to form a hydrogen bond to the active-site Ser198.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Butirilcolinesterase
/
Cocaína
Limite:
Humans
Idioma:
En
Revista:
Acta Crystallogr Sect F Struct Biol Cryst Commun
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos