Literature DB >> 15050619

Contemporary paradigms for cholinergic ligand design guided by biological structure.

Palmer Taylor1, Scott B Hansen, Todd T Talley, Ryan E Hibbs, Zoran Radić.   

Abstract

The identification of the various nicotinic receptor subtypes, when coupled with the recent development of three-dimensional structures of surrogate extracellular receptor domains, offers new opportunities to design nicotinic ligands. Conformation and fluctuations in receptor structure are critical to ligand selectivity, and we present here how a flexible receptor template can be used in the development of selective ligands affecting cholinergic neurotransmission.

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Year:  2004        PMID： 15050619      PMCID： PMC3191913          DOI： 10.1016/j.bmcl.2003.10.072

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  13 in total

1.  Crystal structure of rhodopsin: A G protein-coupled receptor.

Authors:  K Palczewski; T Kumasaka; T Hori; C A Behnke; H Motoshima; B A Fox; I Le Trong; D C Teller; T Okada; R E Stenkamp; M Yamamoto; M Miyano
Journal:  Science       Date:  2000-08-04       Impact factor: 47.728

2.  A glia-derived acetylcholine-binding protein that modulates synaptic transmission.

Authors:  A B Smit; N I Syed; D Schaap; J van Minnen; J Klumperman; K S Kits; H Lodder; R C van der Schors; R van Elk; B Sorgedrager; K Brejc; T K Sixma; W P Geraerts
Journal:  Nature       Date:  2001-05-17       Impact factor: 49.962

3.  Structural insights into ligand interactions at the acetylcholinesterase peripheral anionic site.

Authors:  Yves Bourne; Palmer Taylor; Zoran Radić; Pascale Marchot
Journal:  EMBO J       Date:  2003-01-02       Impact factor: 11.598

4.  Click chemistry in situ: acetylcholinesterase as a reaction vessel for the selective assembly of a femtomolar inhibitor from an array of building blocks.

Authors:  Warren G Lewis; Luke G Green; Flavio Grynszpan; Zoran Radić; Paul R Carlier; Palmer Taylor; M G Finn; K Barry Sharpless
Journal:  Angew Chem Int Ed Engl       Date:  2002-03-15       Impact factor: 15.336

5.  On the reaction of cells and of nerve-endings to certain poisons, chiefly as regards the reaction of striated muscle to nicotine and to curari.

Authors:  J N Langley
Journal:  J Physiol       Date:  1905-12-30       Impact factor: 5.182

6.  Use of a snake venom toxin to characterize the cholinergic receptor protein.

Authors:  J P Changeux; M Kasai; C Y Lee
Journal:  Proc Natl Acad Sci U S A       Date:  1970-11       Impact factor: 11.205

7.  Reversibly bound and covalently attached ligands induce conformational changes in the omega loop, Cys69-Cys96, of mouse acetylcholinesterase.

Authors:  J Shi; A E Boyd; Z Radic; P Taylor
Journal:  J Biol Chem       Date:  2001-08-21       Impact factor: 5.157

8.  Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity.

Authors:  Marie-Louise Lunn; Anders Hogner; Tine B Stensbøl; Eric Gouaux; Jan Egebjerg; Jette S Kastrup
Journal:  J Med Chem       Date:  2003-02-27       Impact factor: 7.446

9.  Tryptophan fluorescence reveals conformational changes in the acetylcholine binding protein.

Authors:  Scott B Hansen; Zoran Radic'; Todd T Talley; Brian E Molles; Tom Deerinck; Igor Tsigelny; Palmer Taylor
Journal:  J Biol Chem       Date:  2002-09-13       Impact factor: 5.157

10.  Nanosecond dynamics of the mouse acetylcholinesterase cys69-cys96 omega loop.

Authors:  Jianxin Shi; Kaihsu Tai; J Andrew McCammon; Palmer Taylor; David A Johnson
Journal:  J Biol Chem       Date:  2003-05-19       Impact factor: 5.157
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  1 in total

Review 1.  Structural answers and persistent questions about how nicotinic receptors work.

Authors:  Gregg B Wells
Journal:  Front Biosci       Date:  2008-05-01
  1 in total

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