title: Influence of the point mutation alpha-1-H101R on the assembly of gamma-aminobutyric acid type A receptors.
abstract: The point mutation H101R in the alpha1-subunit of gamma-aminobutyric acid type A receptors is known to abolish effects by benzodiazepine diazepam. This mutation and homologous mutations in other alpha-subunits have been used to quantify receptor pentamers containing two different alpha-subunit isoforms, and to study the role of alpha-subunit isoforms in the response of mice to diazepam. Both types of study assumed implicitly or explicitly that this mutation strongly affects assembly with the gamma2-subunit. Here, we investigated the assembly properties of mutated in comparison with wild-type subunits, and demonstrate that alpha1H101R has similar assembly properties as wild-type alpha1.
authors.affiliation: Department of Pharmacology, University of Bern, Bern, Switzerland.
authors.forename: Roland
authors.initials: R
authors.lastname: Baur
authors.forename: Erwin
authors.initials: E
authors.lastname: Sigel
mesh_terms: D000818:Animals; D003975:Diazepam / Q000494:pharmacology; D018757:GABA Modulators / Q000494:pharmacology; D015640:Ion Channel Gating / Q000235:genetics* / Q000502:physiology*; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D016296:Mutagenesis; D009865:Oocytes / Q000502:physiology; D018408:Patch-Clamp Techniques; D017354:Point Mutation; D021122:Protein Subunits / Q000235:genetics / Q000502:physiology; D051381:Rats; D011963:Receptors, GABA-A / Q000235:genetics* / Q000502:physiology*; D014982:Xenopus laevis
chemical_list: D018757:GABA Modulators; D021122:Protein Subunits; D011963:Receptors, GABA-A; D003975:Diazepam