Article
Constitutive activity and inverse agonism at the alpha1adrenoceptors.
Biochemical pharmacology - 15 Apr 2007
Cotecchia Susanna
Abstract excerpt
Mutations of G protein-coupled receptors (GPCR) can increase their constitutive (agonist-independent) activity. Some of these mutations have been artificially introduced by site-directed mutagenesis, others occur spontaneously in human diseases. The alpha(1B)adrenoceptor was the first GPCR in which point mutations were shown to trigger receptor activation. This article briefly summarizes some of the findings...
Topics
- Adrenergic alpha-1 Receptor Antagonists
- Adrenergic alpha-Antagonists
- Amino Acid Sequence
- Animals
- COS Cells
- Chlorocebus aethiops
- Cricetinae
- GTP-Binding Proteins
- Humans
- Models, Molecular
- Molecular Sequence Data
- Mutation
- Protein Conformation
- Protein Structure, Secondary
- Receptors, Adrenergic, alpha-1
- Receptors, G-Protein-Coupled