Share This Author
Oxytocin and Vasopressin Agonists and Antagonists as Research Tools and Potential Therapeutics
We recently reviewed the status of peptide and nonpeptide agonists and antagonists for the V1a, V1b and V2 receptors for arginine vasopressin (AVP) and the oxytocin receptor for oxytocin (OT). In the…
Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents.
Time-resolved FRET between GPCR ligands reveals oligomers in native tissues.
A time-resolved FRET strategy based on receptor labeling with selective fluorescent ligands was developed and applied to native tissues and succeeded in demonstrating the presence of oxytocin receptor dimers and/or oligomers in mammary gland.
Inhibition of oxytocin receptor function by direct binding of progesterone
These findings provide the first evidence for a direct interaction between a steroid hormone and a G-protein-coupled receptor and define a new level of crosstalk between the peptide- and steroid-hormone signalling pathways.
The Binding Site of Neuropeptide Vasopressin V1a Receptor
The experimental results suggest that AVP could be completely buried into a 15-20-Å deep cleft defined by the transmembrane helices of the receptor and interact with amino acids located within this region, which indicates a different binding mode for agonists and antagonists in the vasopressin receptor.
Desensitization, phosphorylation and palmitoylation of the human dopamine D1 receptor.
Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor.
It is shown that Arg8 is crucial for high affinity binding of AVP to the rat V1a receptor and when Tyr115 is replaced by an Asp and a Phe, the amino acids naturally occurring in the V2 and in the OT receptor subtypes, the agonist selectivity of the V 1a receptor switches accordingly.
Structural bases of vasopressin/oxytocin receptor function.
Recent studies suggest that the vasopressin V1b receptor may serve additional and unknown functions in the brain and at the periphery, and a great number of molecular probes have been developed, including agonists and antagonists, and radiolabelled, fluorescent or photosensitive ligands.
Oxytocin and vasopressin V1a and V2 receptors form constitutive homo- and heterodimers during biosynthesis.
The finding that immature forms of the receptor can be immunoprecipitated as homo- and heterodimers and the detection by BRET of such oligomer in endoplasmic reticulum-enriched fractions suggest that the oligomerization processes take place early during biosynthesis.
THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview
The Concise Guide to PHARMACOLOGY 2017/18 is the third in this series of biennial publications. This version provides concise overviews of the key properties of nearly 1800 human drug targets with an…