Literature DB >> 22627701

Covalent attachment of antagonists to the α7 nicotinic acetylcholine receptor: synthesis and reactivity of substituted maleimides.

Joseph I Ambrus1, Jill I Halliday, Nicholas Kanizaj, Nathan Absalom, Kasper Harpsøe, Thomas Balle, Mary Chebib, Malcolm D McLeod.   

Abstract

The 3-methylmaleimide congeners of the natural product methyllycaconitine (MLA) and an analogue covalently attach to functional cysteine mutants of the α7 nicotinic acetylcholine receptor (nAChR).

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Year:  2012        PMID： 22627701     DOI： 10.1039/c2cc32442c

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  2 in total

1.  Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.

Authors:  Tue Heesgaard Jepsen; Anders A Jensen; Mads Henrik Lund; Emil Glibstrup; Jesper Langgaard Kristensen
Journal:  ACS Med Chem Lett       Date:  2014-05-20       Impact factor: 4.345

2.  Covalent trapping of methyllycaconitine at the α4-α4 interface of the α4β2 nicotinic acetylcholine receptor: antagonist binding site and mode of receptor inhibition revealed.

Authors:  Nathan L Absalom; Gracia Quek; Trevor M Lewis; Taima Qudah; Ida von Arenstorff; Joseph I Ambrus; Kasper Harpsøe; Nasiara Karim; Thomas Balle; Malcolm D McLeod; Mary Chebib
Journal:  J Biol Chem       Date:  2013-07-26       Impact factor: 5.157
  2 in total

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