Structural determinants of the multifunctional profile of dual binding site acetylcholinesterase inhibitors as anti-alzheimer agents
Dual binding site acetylcholinesterase inhibitors have recently emerged as a new class of anti-Alzheimer agents with potential to positively modify the course of the disease. These compounds exhibit a multifunctional pharmacological profile arising from interaction with several biological targets in...
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Bentham Science Publishers B.V.
2010
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| LEADER | 33366caa a22026177a 4500 | ||
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| 003 | AR-BaUEN | ||
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| 008 | 190411s2010 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-77957932175 | |
| 024 | 7 | |2 cas |a acetylcholine, 51-84-3, 60-31-1, 66-23-9; acetylcholinesterase, 9000-81-1; amyloid beta protein, 109770-29-8; cholinesterase, 9001-08-5; decamethonium, 1420-40-2, 156-74-1, 3198-38-7, 541-22-0; donepezil, 120011-70-3, 120014-06-4, 142057-77-0; galantamine, 1953-04-4, 357-70-0; gallamine, 153-76-4; huperzine A, 102518-79-6, 92138-20-0; physostigmine, 57-47-6, 64-47-1; propidium iodide, 25535-16-4; tacrine, 1684-40-8, 3198-41-2, 321-64-2; thioflavine, 2390-54-7 | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
| 030 | |a CPDEF | ||
| 100 | 1 | |a Galdeano, C. | |
| 245 | 1 | 0 | |a Structural determinants of the multifunctional profile of dual binding site acetylcholinesterase inhibitors as anti-alzheimer agents |
| 260 | |b Bentham Science Publishers B.V. |c 2010 | ||
| 270 | 1 | 0 | |m Muñoz-Torrero, D.; Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Diagonal 643, E-08028, Barcelona, Spain; email: dmunoztorrero@ub.edu |
| 506 | |2 openaire |e Política editorial | ||
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| 520 | 3 | |a Dual binding site acetylcholinesterase inhibitors have recently emerged as a new class of anti-Alzheimer agents with potential to positively modify the course of the disease. These compounds exhibit a multifunctional pharmacological profile arising from interaction with several biological targets involved upstream and downstream in the neurodegenerative cascade of Alzheimer's disease (AD). The primary target of these compounds is the enzyme acetylcholinesterase (AChE). Interaction of dual binding site AChE inhibitors with AChE results in a potent inhibitory activity of AChE and AChE-induced β-amyloid peptide (Aβ) aggregation. Some dual binding site AChE inhibitors take on added value a significant ability to additionally inhibit the enzymes butyrylcholinesterase and BACE-1, involved in the co-regulation of the hydrolysis of the neurotransmitter acetylcholine and in Aβ formation, respectively. The structural determinants which mediate the interaction of dual binding site AChE inhibitors with these three important enzymes for AD treatment are herein re-viewed. © 2010 Bentham Science Publishers Ltd. |l eng | |
| 593 | |a Laboratori de Química Farmacèutica (Unitat Associada al CSIC), Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Diagonal 643, E-08028, Barcelona, Spain | ||
| 593 | |a Laboratorio de Modelado Molecular, Química Inorgánica, Analítica y Química Física, INQUIMAE (CONICET), Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria - Pabellón II 1piso, C1428EHA, Buenos Aires, Argentina | ||
| 593 | |a Departament de Fisicoquímica, Facultat de Farmàcia, and Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Diagonal 643, E-08028, Barcelona, Spain | ||
| 690 | 1 | 0 | |a ACETYLCHOLINESTERASE |
| 690 | 1 | 0 | |a BACE-1 |
| 690 | 1 | 0 | |a BUTYRYLCHOLINESTERASE |
| 690 | 1 | 0 | |a DRUG-TARGET INTERACTIONS |
| 690 | 1 | 0 | |a STRUCTURE-BASED DRUG DESIGN |
| 690 | 1 | 0 | |a 8 ( 2,6 DIMETHYLMORPHOLINO)OCTYLCARBAMOYLESEROLINE |
| 690 | 1 | 0 | |a ACETYLCHOLINE |
| 690 | 1 | 0 | |a ACETYLCHOLINESTERASE |
| 690 | 1 | 0 | |a AMINOPYRIDINE DERIVATIVE |
| 690 | 1 | 0 | |a AMYLOID BETA PROTEIN |
| 690 | 1 | 0 | |a AP 2238 |
| 690 | 1 | 0 | |a BETA SECRETASE |
| 690 | 1 | 0 | |a BETA SECRETASE INHIBITOR |
| 690 | 1 | 0 | |a BUTYRYLCHOLINESTERASE 1 |
| 690 | 1 | 0 | |a CHOLINESTERASE |
| 690 | 1 | 0 | |a CHOLINESTERASE INHIBITOR |
| 690 | 1 | 0 | |a DECAMETHONIUM |
| 690 | 1 | 0 | |a DONEPEZIL |
| 690 | 1 | 0 | |a GALANTAMINE |
| 690 | 1 | 0 | |a GALLAMINE |
| 690 | 1 | 0 | |a HUPERZINE A |
| 690 | 1 | 0 | |a HUPRINE X |
| 690 | 1 | 0 | |a MF 268 |
| 690 | 1 | 0 | |a NEUROMUSCULAR DEPOLARIZING AGENT |
| 690 | 1 | 0 | |a NF 595 |
| 690 | 1 | 0 | |a NOOTROPIC AGENT |
| 690 | 1 | 0 | |a PEPTIDOMIMETIC AGENT |
| 690 | 1 | 0 | |a PHYSOSTIGMINE |
| 690 | 1 | 0 | |a PHYSOSTIGMINE DERIVATIVE |
| 690 | 1 | 0 | |a PROPIDIUM IODIDE |
| 690 | 1 | 0 | |a PYRIMIDINE DERIVATIVE |
| 690 | 1 | 0 | |a SULFONAMIDE |
| 690 | 1 | 0 | |a TACRINE |
| 690 | 1 | 0 | |a THIOFLAVINE |
| 690 | 1 | 0 | |a TRIAZOLE DERIVATIVE |
| 690 | 1 | 0 | |a UNCLASSIFIED DRUG |
| 690 | 1 | 0 | |a UNINDEXED DRUG |
| 690 | 1 | 0 | |a XANTHOSTIGMINE |
| 690 | 1 | 0 | |a ALZHEIMER DISEASE |
| 690 | 1 | 0 | |a ARTICLE |
| 690 | 1 | 0 | |a CATALYSIS |
| 690 | 1 | 0 | |a COMPLEX FORMATION |
| 690 | 1 | 0 | |a CRYSTAL STRUCTURE |
| 690 | 1 | 0 | |a DEGENERATIVE DISEASE |
| 690 | 1 | 0 | |a DISEASE COURSE |
| 690 | 1 | 0 | |a DRUG BINDING SITE |
| 690 | 1 | 0 | |a DRUG INHIBITION |
| 690 | 1 | 0 | |a DRUG POTENCY |
| 690 | 1 | 0 | |a ENZYME ACTIVITY |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a HYDROLYSIS |
| 690 | 1 | 0 | |a IC 50 |
| 690 | 1 | 0 | |a NEUROTRANSMISSION |
| 690 | 1 | 0 | |a NONHUMAN |
| 690 | 1 | 0 | |a OLIGOMERIZATION |
| 690 | 1 | 0 | |a PRIORITY JOURNAL |
| 690 | 1 | 0 | |a X RAY CRYSTALLOGRAPHY |
| 653 | 0 | 0 | |a ap 2238; mf 268; nf 595 |
| 700 | 1 | |a Viayna, E. | |
| 700 | 1 | |a Arroyo, P. | |
| 700 | 1 | |a Bidon-Chanal, A. | |
| 700 | 1 | |a Blas, J.R. | |
| 700 | 1 | |a Muñoz-Torrero, D. | |
| 700 | 1 | |a Luque, F.J. | |
| 773 | 0 | |d Bentham Science Publishers B.V., 2010 |g v. 16 |h pp. 2818-2836 |k n. 25 |p Curr. Pharm. Des. |x 13816128 |t Current Pharmaceutical Design | |
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| 856 | 4 | 0 | |u https://doi.org/10.2174/138161210793176536 |y DOI |
| 856 | 4 | 0 | |u https://hdl.handle.net/20.500.12110/paper_13816128_v16_n25_p2818_Galdeano |y Handle |
| 856 | 4 | 0 | |u https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_13816128_v16_n25_p2818_Galdeano |y Registro en la Biblioteca Digital |
| 961 | |a paper_13816128_v16_n25_p2818_Galdeano |b paper |c PE | ||
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| 999 | |c 68531 | ||