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

Joseph I Ambrus; Jill I Halliday; Nicholas Kanizaj; Nathan Absalom; Kasper Harpsøe; Thomas Balle; Mary Chebib; Malcolm D McLeod

doi:10.1039/c2cc32442c

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

Chem Commun (Camb). 2012 Jul 7;48(53):6699-701. doi: 10.1039/c2cc32442c. Epub 2012 May 25.

Authors

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

Affiliation

¹ Research School of Chemistry, Australian National University, Canberra, ACT 0200, Australia.

PMID: 22627701
DOI: 10.1039/c2cc32442c

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).

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Maleimides / chemical synthesis*
Maleimides / chemistry
Maleimides / pharmacology
Models, Biological
Molecular Structure
Nicotinic Antagonists / chemical synthesis*
Nicotinic Antagonists / chemistry
Nicotinic Antagonists / pharmacology
Rats
Receptors, Nicotinic* / chemistry
Receptors, Nicotinic* / drug effects
alpha7 Nicotinic Acetylcholine Receptor

Substances

Chrna7 protein, rat
Maleimides
Nicotinic Antagonists
Receptors, Nicotinic
alpha7 Nicotinic Acetylcholine Receptor