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MOLECULAR BIOLOGY OF THE GABAA RECEPTOR: FUNCTIONAL DOMAINS
IMPLICATED BY MUTATIONAL ANALYSIS
Martin Davies1, Alan N. Bateson1,2 and Susan M. J. Dunn1,2
1 Department of Pharmacology
2Division of Neuroscience,
Faculty of Medicine, University of Alberta, Edmonton, Alberta,
Canada T6G 2H7
Received 07/16/96; Accepted 07/22/96; On-line 09/01/96
TABLE OF CONTENTS
- 1. Abstract
- 2. Introduction
- 3. Mutational analysis of ligand-gated ion channels: General
considerations
- 4. Mutational analysis of ligand binding domains in the GABAA
receptor
- 4.1.The nicotinic acetylcholine receptor: A receptor prototype
- 4.2.GABA recognition site(s)
- 4.2.1. Residues implicated in GABA binding
- 4.2.2. Investigation of a role for a conserved disulfide
loop
- 4.2.3. A role for aromatic and hydroxylated amino acid residues
- 4.2.4. Other GABA binding proteins
- 4.3. Benzodiazepine recognition site(s)
- 4.3.1. Importance of the alpha subunit(s)
- 4.3.2. Importance of the gamma subunit(s)
- 4.4. Identification of a single residue conferring high affinity
loreclezole binding
- 5. Mutational analysis of the channel forming region of the
GABAA receptor
- 6. Mutational analysis of post-translational modifications
of the GABAA receptor
- 6.1. Phosphorylation sites
- 6.2. Glycosylation sites
- 7. Recent models of GABAA receptor structure and function
- 8. Conclusions
- 9. Acknowledgments
- 10. References
- 11. Entire manuscript
Keywords: molecular pharmacology; brain; ligand-gated ion channels;
GABAA receptor; mutagenesis
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