Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge.
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Yuan-Ping Pang | Joel L Sussman | Israel Silman | J. Sussman | E. H. Rydberg | I. Silman | P. Carlier | Y. Pang | H. Greenblatt | B. Brumshtein | D. Shaya | Boris Brumshtein | Harry M Greenblatt | Paul R Carlier | Dawn M Wong | Edwin H Rydberg | David Shaya | Larry D Williams | L. D. Williams | D. M. Wong | D. Wong
[1] Jan Kroon,et al. STRATEGY: a program to optimize the starting spindle angle and scan range for X-ray data collection , 1997 .
[2] E A Merritt,et al. Raster3D: photorealistic molecular graphics. , 1997, Methods in enzymology.
[3] Joel L Sussman,et al. The complex of a bivalent derivative of galanthamine with torpedo acetylcholinesterase displays drastic deformation of the active-site gorge: implications for structure-based drug design. , 2004, Journal of the American Chemical Society.
[4] J L Sussman,et al. Structure of acetylcholinesterase complexed with (−)‐galanthamine at 2.3 Å resolution , 1999, FEBS letters.
[5] Z. Otwinowski,et al. Processing of X-ray diffraction data collected in oscillation mode. , 1997, Methods in enzymology.
[6] V. Andrisano,et al. beta-Amyloid aggregation induced by human acetylcholinesterase: inhibition studies. , 2003, Biochemical pharmacology.
[7] Collaborative Computational,et al. The CCP4 suite: programs for protein crystallography. , 1994, Acta crystallographica. Section D, Biological crystallography.
[8] Yuan-Ping Pang,et al. Prediction of the binding sites of huperzine A in acetylcholinesterase by docking studies , 1994, J. Comput. Aided Mol. Des..
[9] H. Fibiger,et al. Chapter 49: Role of forebrain cholinergic systems in learning and memory: relevance to the cognitive deficits of aging and Alzheimer's dementia , 1993 .
[10] S. French,et al. On the treatment of negative intensity observations , 1978 .
[11] S. Brimijoin,et al. Highly Potent, Selective, and Low Cost Bis-tetrahydroaminacrine Inhibitors of Acetylcholinesterase , 1996, The Journal of Biological Chemistry.
[12] B. P. Doctor,et al. A monoclonal antibody against acetylcholinesterase inhibits the formation of amyloid fibrils induced by the enzyme. , 1997, Biochemical and biophysical research communications.
[13] Claudia Linker,et al. Acetylcholinesterase Accelerates Assembly of Amyloid-β-Peptides into Alzheimer's Fibrils: Possible Role of the Peripheral Site of the Enzyme , 1996, Neuron.
[14] D. Drachman,et al. Human memory and the cholinergic system. A relationship to aging? , 1974, Archives of neurology.
[15] I. Ivorra,et al. The acetylcholinesterase inhibitor BW284c51 is a potent blocker of Torpedo nicotinic AchRs incorporated into the Xenopus oocyte membrane , 2005, British journal of pharmacology.
[16] I B WILSON,et al. The inhibitory effect of stilbamidine, curare and related compounds and its relationship to the active groups of acetylcholine esterase; action of stilbamidine upon nerve impulse conduction. , 1950, Biochimica et biophysica acta.
[17] D. Humphrey,et al. Ambenonium is a rapidly reversible noncovalent inhibitor of acetylcholinesterase, with one of the highest known affinities. , 1992, Molecular Pharmacology.
[18] N. Greig,et al. Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine. , 2005, Journal of medicinal chemistry.
[19] E. Giacobini,et al. Cholinesterase inhibitors: new roles and therapeutic alternatives. , 2004, Pharmacological research.
[20] Ettore Novellino,et al. Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. , 2005, Journal of medicinal chemistry.
[21] I Silman,et al. A structural motif of acetylcholinesterase that promotes amyloid beta-peptide fibril formation. , 2001, Biochemistry.
[22] Yvain Nicolet,et al. Crystal Structure of Human Butyrylcholinesterase and of Its Complexes with Substrate and Products* , 2003, Journal of Biological Chemistry.
[23] G. Campiani,et al. Conformational flexibility in the peripheral site of Torpedo californica acetylcholinesterase revealed by the complex structure with a bifunctional inhibitor. , 2006, Journal of the American Chemical Society.
[24] A. Goldman,et al. Atomic structure of acetylcholinesterase from Torpedo californica: a prototypic acetylcholine-binding protein , 1991, Science.
[25] H. Fibiger,et al. Role of forebrain cholinergic systems in learning and memory: relevance to the cognitive deficits of aging and Alzheimer's dementia. , 1993, Progress in brain research.
[26] Axel T. Brunger,et al. Free R value: cross-validation in crystallography. , 1997 .
[27] Zoran Radić,et al. In situ selection of lead compounds by click chemistry: target-guided optimization of acetylcholinesterase inhibitors. , 2005, Journal of the American Chemical Society.
[28] Zoran Radić,et al. Freeze-frame inhibitor captures acetylcholinesterase in a unique conformation. , 2004, Proceedings of the National Academy of Sciences of the United States of America.
[29] J. Sussman,et al. Acetylcholinesterase: 'classical' and 'non-classical' functions and pharmacology. , 2005, Current opinion in pharmacology.
[30] E. Perry,et al. CHANGES IN BRAIN CHOLINESTERASES IN SENILE DEMENTIA OF ALZHEIMER TYPE , 1978, Neuropathology and applied neurobiology.
[31] P. Carlier,et al. Development of bivalent acetylcholinesterase inhibitors as potential therapeutic drugs for Alzheimer's disease. , 2004, Current pharmaceutical design.
[32] P. Carlier,et al. Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions. , 1999, Journal of medicinal chemistry.
[33] J. Sussman,et al. Acetylcholinesterase: a multifaceted target for structure-based drug design of anticholinesterase agents for the treatment of Alzheimer's disease. , 2003, Journal of molecular neuroscience : MN.
[34] R. Bartus,et al. The cholinergic hypothesis of geriatric memory dysfunction. , 1982, Science.
[35] P. Taylor,et al. Click chemistry in situ: acetylcholinesterase as a reaction vessel for the selective assembly of a femtomolar inhibitor from an array of building blocks. , 2002, Angewandte Chemie.
[36] L. Austin,et al. Two selective inhibitors of cholinesterase. , 1953, The Biochemical journal.
[37] D. Boehr,et al. Analysis of the pi-pi stacking interactions between the aminoglycoside antibiotic kinase APH(3')-IIIa and its nucleotide ligands. , 2002, Chemistry & biology.
[38] J L Sussman,et al. Conversion of acetylcholinesterase to butyrylcholinesterase: modeling and mutagenesis. , 1992, Proceedings of the National Academy of Sciences of the United States of America.
[39] Vincenza Andrisano,et al. Rational approach to discover multipotent anti-Alzheimer drugs. , 2005, Journal of medicinal chemistry.
[40] W. Delano. The PyMOL Molecular Graphics System , 2002 .
[41] Yuan-Ping Pang,et al. Crystal packing mediates enantioselective ligand recognition at the peripheral site of acetylcholinesterase. , 2005, Journal of the American Chemical Society.
[42] R J Read,et al. Crystallography & NMR system: A new software suite for macromolecular structure determination. , 1998, Acta crystallographica. Section D, Biological crystallography.
[43] Ming-tao Li,et al. Novel Dimeric Acetylcholinesterase Inhibitor Bis(7)-tacrine, but Not Donepezil, Prevents Glutamate-induced Neuronal Apoptosis by Blocking N-Methyl-d-aspartate Receptors* , 2005, Journal of Biological Chemistry.
[44] P. Watkins,et al. Hepatotoxic effects of tacrine administration in patients with Alzheimer's disease. , 1994, JAMA.
[45] M Farlow,et al. A controlled trial of tacrine in Alzheimer's disease. The Tacrine Study Group. , 1992, JAMA.
[46] A T Brünger,et al. Crystallographic refinement by simulated annealing: methods and applications. , 1997, Methods in enzymology.
[47] A. Cavalli,et al. 3-(4-[[Benzyl(methyl)amino]methyl]phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: a dual function lead for Alzheimer's disease therapy. , 2003, Journal of medicinal chemistry.
[48] E. Perry,et al. Butyrylcholinesterase: impact on symptoms and progression of cognitive impairment , 2005, Expert review of neurotherapeutics.
[49] W. Jencks,et al. Binding energy, specificity, and enzymic catalysis: the circe effect. , 2006, Advances in enzymology and related areas of molecular biology.
[50] D. Neary,et al. Biochemical Assessment of Serotonergic and Cholinergic Dysfunction and Cerebral Atrophy in Alzheimer's Disease , 1983, Journal of neurochemistry.
[51] D E McRee,et al. XtalView/Xfit--A versatile program for manipulating atomic coordinates and electron density. , 1999, Journal of structural biology.
[52] S. Wodak,et al. Effect of mutations within the peripheral anionic site on the stability of acetylcholinesterase. , 1999, Molecular pharmacology.
[53] J. Sussman,et al. Quaternary ligand binding to aromatic residues in the active-site gorge of acetylcholinesterase. , 1994, Proceedings of the National Academy of Sciences of the United States of America.
[54] P. Carlier,et al. Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis. , 1999, Bioorganic & medicinal chemistry.