The bivalent ligand approach as a tool for improving the in vitro anti-alzheimer multitarget profile of dimebon

Autor:	Maria Laura Bolognesi, Ian R. Mellor, José Marco-Contelles, Elena Simoni, Michela Rosini, Barbara Monti, Vincenza Andrisano, Manuela Bartolini, David W. McClymont, Elena Soriano, Birgit Hutter-Paier, Manfred Windisch
Přispěvatelé:	Michela Rosini, Elena Simoni, Manuela Bartolini, Elena Soriano, José Marco-Contelle, Vincenza Andrisano, Barbara Monti, Manfred Windisch, Birgit Hutter-Paier, David W. McClymont, Ian R. Mellor, Maria Laura Bolognesi
Rok vydání:	2013
Předmět:	Indoles dual binding inhibitor Apoptosis Pharmacology Ligands Receptors N-Methyl-D-Aspartate Biochemistry NMDA receptors Bivalent (genetics) Aetylcholinesterase chemistry.chemical_compound Alzheimer Disease Drug Discovery Animals Humans General Pharmacology Toxicology and Pharmaceutics Butyrylcholinesterase Amyloid aggregation Neurons Amyloid beta-Peptides Binding Sites Anti alzheimer Dual binding inhibitors Organic Chemistry acetylcholinesterase NMDA receptor Acetylcholinesterase Peptide Fragments Recombinant Proteins In vitro Protein Structure Tertiary Molecular Docking Simulation chemistry Molecular Medicine Cholinesterase Inhibitors Chickens Alzheimer’s disease
Zdroj:	Digital.CSIC. Repositorio Institucional del CSIC instname
ISSN:	1860-7179 1860-7187
Popis:	Inspired by the concept of bivalent ligands, we prepared a small set of analogues of the drug candidate dimebon. They were shown to inhibit AChE, Aβ42 aggregation, and NMDA receptor activation to a greater extent than dimebon. Some of these compounds also enhanced the survival of chicken neurons under apoptosis-inducing conditions.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e511551adcbeb4d24a671bca5a2b2138 http://hdl.handle.net/10261/114915 Zobrazit plný text záznamu Plný text