Aricept Complexed with Acetylcholinesterase (Russian)

spinqualitylabelsall models PDB ID 1eve Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image
1eve, resolution 2.50Å ()
Ligands:	,
Activity:	Acetylcholinesterase, with EC number 3.1.1.7
Structural annotation: Resources: CATH : 1Eve000 InterPro : Ipr000908, Ipr002018, Ipr000997 Pfam : PF00135 SCOP : d1eve__ UniProt : P04058
Functional annotation: Cellular component: synapse cell junction membrane Biological process: neurotransmitter catabolic process acetylcholine catabolic process in synaptic cleft Molecular function: cholinesterase activity hydrolase activity GPI anchor binding acetylcholinesterase activity
Evolutionary conservation: Toggle Conservation Colors: Rows = identical sequences: Further Information: Caveats, Explanation, Complete Results at ConSurfDB
Resources:	FirstGlance, OCA, RCSB, PDBsum
Coordinates:	save as pdb, mmCIF, xml

Трёхмерная структура Арицепта, лекарства против болезни Алцгеймера, в комплексе с ацетилхолинэстеразой (см. также Бивалентные ингибиторы ацетилхолинэстеразы (Часть II))

ВведениеВведение

Несколько ингибиторов ацетилхолинэстеразы применяются в симптоматическом лечении болезни Алцгеймера, либо находятся на завершающих этапах клинических исследований. E2020, распространяемый под названием Арицепт (Aricept) является представителем большой семьи ингибиторов фермента ацетилхолинэстеразы (АЦХа).

E2020, marketed as Aricept, is a member of a large family of N-benzylpiperidine-based acetylcholinesterase (AChE) inhibitors, developed, synthesized and evaluated by the Eisai Company in Japan. These inhibitors were designed on the basis of QSAR studies prior to elucidation of the 3D structure of Torpedo californica AChE (TcAChE) (1ea5). It significantly enhances performance in animal models of cholinergic hypofunction and has a high affinity for AChE, binding to both electric eel and mouse AChE in the nanomolar range.