[Frontiers in Bioscience 1, d214-233, September 1, 1996]
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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