Literature DB >> 14501022

Acetylcholinesterase: a multifaceted target for structure-based drug design of anticholinesterase agents for the treatment of Alzheimer's disease.

Harry M Greenblatt1, Hay Dvir, Israel Silman, Joel L Sussman.   

Abstract

The structure of Torpedo californica acetylcholinesterase is examined in complex with several inhibitors that are either in use or under development for treating Alzheimer's disease. The noncovalent inhibitors vary greatly in their structures and bind to different sites of the enzyme, offering many different starting points for future drug design.

Entities:  

Mesh：

Substances：

Year:  2003        PMID： 14501022     DOI： 10.1385/JMN:20:3:369

Source DB:  PubMed          Journal:  J Mol Neurosci        ISSN： 0895-8696            Impact factor:   2.866


  64 in total

1.  Huprine X is a novel high-affinity inhibitor of acetylcholinesterase that is of interest for treatment of Alzheimer's disease.

Authors:  P Camps; B Cusack; W D Mallender; R E El Achab; J Morral; D Muñoz-Torrero; T L Rosenberry
Journal:  Mol Pharmacol       Date:  2000-02       Impact factor: 4.436

2.  Amino acid residues controlling acetylcholinesterase and butyrylcholinesterase specificity.

Authors:  D C Vellom; Z Radić; Y Li; N A Pickering; S Camp; P Taylor
Journal:  Biochemistry       Date:  1993-01-12       Impact factor: 3.162

3.  Structures of recombinant native and E202Q mutant human acetylcholinesterase complexed with the snake-venom toxin fasciculin-II.

Authors:  G Kryger; M Harel; K Giles; L Toker; B Velan; A Lazar; C Kronman; D Barak; N Ariel; A Shafferman; I Silman; J L Sussman
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2000-11

4.  Long chain analogs of physostigmine as potential drugs for Alzheimer's disease: new insights into the mechanism of action in the inhibition of acetylcholinesterase.

Authors:  E Perola; L Cellai; D Lamba; L Filocamo; M Brufani
Journal:  Biochim Biophys Acta       Date:  1997-11-14

5.  Dissection of the human acetylcholinesterase active center determinants of substrate specificity. Identification of residues constituting the anionic site, the hydrophobic site, and the acyl pocket.

Authors:  A Ordentlich; D Barak; C Kronman; Y Flashner; M Leitner; Y Segall; N Ariel; S Cohen; B Velan; A Shafferman
Journal:  J Biol Chem       Date:  1993-08-15       Impact factor: 5.157

Review 6.  Anticholinesterases: medical applications of neurochemical principles.

Authors:  C B Millard; C A Broomfield
Journal:  J Neurochem       Date:  1995-05       Impact factor: 5.372

7.  Conformational analyses and molecular-shape comparisons of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.

Authors:  M G Cardozo; T Kawai; Y Iimura; H Sugimoto; Y Yamanishi; A J Hopfinger
Journal:  J Med Chem       Date:  1992-02-07       Impact factor: 7.446

8.  Identification of amino acid residues involved in the binding of Huperzine A to cholinesterases.

Authors:  A Saxena; N Qian; I M Kovach; A P Kozikowski; Y P Pang; D C Vellom; Z Radić; D Quinn; P Taylor; B P Doctor
Journal:  Protein Sci       Date:  1994-10       Impact factor: 6.725

9.  Role of tyrosine 337 in the binding of huperzine A to the active site of human acetylcholinesterase.

Authors:  Y Ashani; J Grunwald; C Kronman; B Velan; A Shafferman
Journal:  Mol Pharmacol       Date:  1994-03       Impact factor: 4.436

10.  Prediction of the binding site of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine in acetylcholinesterase by docking studies with the SYSDOC program.

Authors:  Y P Pang; A P Kozikowski
Journal:  J Comput Aided Mol Des       Date:  1994-12       Impact factor: 3.686
View more
  26 in total

1.  High throughput enzyme inhibitor screening by functionalized magnetic carbonaceous microspheres and graphene oxide-based MALDI-TOF-MS.

Authors:  Yang Liu; Yan Li; Junyan Liu; Chunhui Deng; Xiangmin Zhang
Journal:  J Am Soc Mass Spectrom       Date:  2011-09-27       Impact factor: 3.109

2.  Structural insights into substrate traffic and inhibition in acetylcholinesterase.

Authors:  Jacques-Philippe Colletier; Didier Fournier; Harry M Greenblatt; Jure Stojan; Joel L Sussman; Giuseppe Zaccai; Israel Silman; Martin Weik
Journal:  EMBO J       Date:  2006-06-08       Impact factor: 11.598

3.  Shoot-and-Trap: use of specific x-ray damage to study structural protein dynamics by temperature-controlled cryo-crystallography.

Authors:  Jacques-Philippe Colletier; Dominique Bourgeois; Benoît Sanson; Didier Fournier; Joel L Sussman; Israel Silman; Martin Weik
Journal:  Proc Natl Acad Sci U S A       Date:  2008-08-13       Impact factor: 11.205

4.  Flexibility of aromatic residues in the active-site gorge of acetylcholinesterase: X-ray versus molecular dynamics.

Authors:  Yechun Xu; Jacques-Philippe Colletier; Martin Weik; Hualiang Jiang; John Moult; Israel Silman; Joel L Sussman
Journal:  Biophys J       Date:  2008-05-23       Impact factor: 4.033

5.  Rapid and label-free screening of enzyme inhibitors using segmented flow electrospray ionization mass spectrometry.

Authors:  Jian Pei; Qiang Li; Robert T Kennedy
Journal:  J Am Soc Mass Spectrom       Date:  2010-02-10       Impact factor: 3.109

Review 6.  Carboxylesterase inhibitors.

Authors:  M Jason Hatfield; Philip M Potter
Journal:  Expert Opin Ther Pat       Date:  2011-05-24       Impact factor: 6.674

7.  Chiral Separation, X-ray Structure, and Biological Evaluation of a Potent and Reversible Dual Binding Site AChE Inhibitor.

Authors:  Marco Catto; Leonardo Pisani; Eugenio de la Mora; Benny Danilo Belviso; Giuseppe Felice Mangiatordi; Andrea Pinto; Annalisa De Palma; Nunzio Denora; Rocco Caliandro; Jacques-Philippe Colletier; Israel Silman; Orazio Nicolotti; Cosimo Damiano Altomare
Journal:  ACS Med Chem Lett       Date:  2020-02-07       Impact factor: 4.345

8.  Aryl acylamidase activity on acetylcholinesterase is high during early chicken brain development.

Authors:  Rathanam Boopathy; Paul G Layer
Journal:  Protein J       Date:  2004-07       Impact factor: 2.371

9.  Flavoring extracts of Hemidesmus indicus roots and Vanilla planifolia pods exhibit in vitro acetylcholinesterase inhibitory activities.

Authors:  Anish Kundu; Adinpunya Mitra
Journal:  Plant Foods Hum Nutr       Date:  2013-09       Impact factor: 3.921

10.  The impact of crystallization conditions on structure-based drug design: A case study on the methylene blue/acetylcholinesterase complex.

Authors:  Orly Dym; Wanling Song; Clifford Felder; Esther Roth; Valery Shnyrov; Yacov Ashani; Yechun Xu; Robbie P Joosten; Lev Weiner; Joel L Sussman; Israel Silman
Journal:  Protein Sci       Date:  2016-03-28       Impact factor: 6.725
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.