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Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors.
G-protein-coupled receptors (GPCRs) represent one of the largest gene families in the animal genome. These receptors can be classified into several groups based on the sequence similarity of theirExpand
Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization
Cell-surface proteins are important in cell-cell communication. They assemble into heterocomplexes that include different receptors and effectors. Elucidation and manipulation of such proteinExpand
The Non-competitive Antagonists 2-Methyl-6-(phenylethynyl)pyridine and 7-Hydroxyiminocyclopropan[b]chromen-1a-carboxylic Acid Ethyl Ester Interact with Overlapping Binding Pockets in the
We have investigated the mechanism of inhibition and site of action of the novel human metabotropic glutamate receptor 5 (hmGluR5) antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP), which isExpand
CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding.
Metabotropic glutamate receptors (mGluRs) are a family of G protein-coupled receptors characterized by a large, extracellular N-terminal domain comprising the glutamate-binding site. In the currentExpand
Activation mechanism of the heterodimeric GABA(B) receptor.
The GABA(B) receptor was the first heteromeric G-protein coupled receptor (GPCR) identified. Indeed, both GABA(B1) and GABA(B2) subunits appear necessary to get a functional GABA(B) receptor. SoonExpand
Agonist-independent activation of metabotropic glutamate receptors by the intracellular protein Homer
G-protein-coupled receptors (GPCRs) transduce signals from extracellular transmitters to the inside of the cell by activating G proteins. Mutation and overexpression of these receptors have revealedExpand
Allosteric interactions between GB1 and GB2 subunits are required for optimal GABAB receptor function
Recent studies on G‐protein‐coupled receptors revealed that they can dimerize. However, the role of each subunit in the activation process remains unclear. The γ‐amino‐n‐butyric acid type B (GABAB)Expand
C-Terminal Interaction Is Essential for Surface Trafficking But Not for Heteromeric Assembly of GABAB Receptors
Assembly of fully functional GABAB receptors requires heteromerization of the GABAB(1) and GABAB(2)subunits. It is thought that GABAB(1) and GABAB(2) undergo coiled-coil dimerization in theirExpand
Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors
  • C. Goudet, F. Gaven, +6 authors J. Pin
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences…
  • 22 December 2003
Although agonists bind directly in the heptahelical domain (HD) of most class-I rhodopsin-like G protein coupled receptors (GPCRs), class-III agonists bind in the extracellular domain of theirExpand
Changes in the carboxyl-terminal domain of metabotropic glutamate receptor 1 by alternative splicing generate receptors with differing agonist-independent activity.
The metabotropic glutamate receptors (mGluRs) share no sequence homology and show different structural features compared with most other G protein-coupled receptors (GPCRs). In particular, someExpand