Detail
Článek
Článek online
FT
Medvik - BMČ
  • Je něco špatně v tomto záznamu ?

Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase

A. Kostelnik, A. Cegan, M. Pohanka,

. 2017 ; 2017 (-) : 2532764. [pub] 20170713

Jazyk angličtina Země Spojené státy americké

Typ dokumentu časopisecké články

Perzistentní odkaz   https://www.medvik.cz/link/bmc18024757

Biperiden is a drug used in Parkinson disease treatment and it serves also as an antiseizures compound in organophosphates poisoning. It acts as antagonist of muscarinic receptor activated by acetylcholine while the enzyme acetylcholinesterase (AChE) cleaves acetylcholine in synaptic junction into choline and acetic acid. This enzyme is inhibited by various compounds; however there has not been proposed evidence about interaction with biperiden molecule. We investigated this interaction using standard Ellman's assay and experimental findings were critically completed with an in silico prediction by SwissDock docking software. Uncompetitive mechanism of action was revealed from Dixon plot and inhibition constant (Ki ) was calculated to be 1.11 mmol/l. The lowest predicted binding energy was -7.84 kcal/mol corresponding to H-bond between biperiden molecule and Tyr 341 residuum in protein structure of AChE. This interaction seems to be further stabilized by π-π interaction with Tyr 72, Trp 286, and Tyr 341. In conclusion, biperiden appears as a very weak inhibitor but it can serve as a lead structure in a pharmacological research.

Citace poskytuje Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc18024757
003      
CZ-PrNML
005      
20180711095901.0
007      
ta
008      
180709s2017 xxu f 000 0|eng||
009      
AR
024    7_
$a 10.1155/2017/2532764 $2 doi
035    __
$a (PubMed)28785576
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a xxu
100    1_
$a Kostelnik, Adam $u Faculty of Chemical Technology, University of Pardubice, Studentska 95, 53210 Pardubice, Czech Republic. Faculty of Military Health Sciences, University of Defence, Trebesska 1575, 50001 Hradec Kralove, Czech Republic.
245    10
$a Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase / $c A. Kostelnik, A. Cegan, M. Pohanka,
520    9_
$a Biperiden is a drug used in Parkinson disease treatment and it serves also as an antiseizures compound in organophosphates poisoning. It acts as antagonist of muscarinic receptor activated by acetylcholine while the enzyme acetylcholinesterase (AChE) cleaves acetylcholine in synaptic junction into choline and acetic acid. This enzyme is inhibited by various compounds; however there has not been proposed evidence about interaction with biperiden molecule. We investigated this interaction using standard Ellman's assay and experimental findings were critically completed with an in silico prediction by SwissDock docking software. Uncompetitive mechanism of action was revealed from Dixon plot and inhibition constant (Ki ) was calculated to be 1.11 mmol/l. The lowest predicted binding energy was -7.84 kcal/mol corresponding to H-bond between biperiden molecule and Tyr 341 residuum in protein structure of AChE. This interaction seems to be further stabilized by π-π interaction with Tyr 72, Trp 286, and Tyr 341. In conclusion, biperiden appears as a very weak inhibitor but it can serve as a lead structure in a pharmacological research.
650    _2
$a acetylcholinesterasa $x metabolismus $7 D000110
650    _2
$a biperiden $x chemie $x farmakologie $x terapeutické užití $7 D001712
650    _2
$a cholinesterasové inhibitory $x chemie $x farmakologie $x terapeutické užití $7 D002800
650    _2
$a enzymatické testy $7 D057075
650    _2
$a lidé $7 D006801
650    _2
$a molekulární modely $7 D008958
650    _2
$a Parkinsonova nemoc $x farmakoterapie $x enzymologie $7 D010300
650    _2
$a substrátová specifita $x účinky léků $7 D013379
655    _2
$a časopisecké články $7 D016428
700    1_
$a Cegan, Alexander $u Faculty of Chemical Technology, University of Pardubice, Studentska 95, 53210 Pardubice, Czech Republic.
700    1_
$a Pohanka, Miroslav $u Faculty of Military Health Sciences, University of Defence, Trebesska 1575, 50001 Hradec Kralove, Czech Republic.
773    0_
$w MED00182164 $t BioMed research international $x 2314-6141 $g Roč. 2017, č. - (2017), s. 2532764
856    41
$u https://pubmed.ncbi.nlm.nih.gov/28785576 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y a $z 0
990    __
$a 20180709 $b ABA008
991    __
$a 20180711100152 $b ABA008
999    __
$a ok $b bmc $g 1316888 $s 1021678
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2017 $b 2017 $c - $d 2532764 $e 20170713 $i 2314-6141 $m BioMed research international $n Biomed Res Int $x MED00182164
LZP    __
$a Pubmed-20180709

Najít záznam

Citační ukazatele

Možnosti archivace