GPCR photopharmacology

@article{RicartOrtega2019GPCRP,
  title={GPCR photopharmacology},
  author={Maria Ricart-Ortega and Joan Font and Amadeu Llebaria},
  journal={Molecular and Cellular Endocrinology},
  year={2019},
  volume={488},
  pages={36-51}
}
11 Citations
Mechanistic Insights into Light-Driven Allosteric Control of GPCR Biological Activity.
TLDR
It is concluded that photoisomerization can take place inside and outside the ligand binding pocket, and this leads to a reversible loss in affinity, in part, due to changes in dissociation rates from the receptor.
Photoswitchable antagonists for a precise spatiotemporal control of β2-adrenoceptors.
TLDR
This work introduces Photoazolol-1-3, a series of photoswitchable azobenzene β2-AR antagonists that can be reversibly controlled with light and provides a molecular rationale for the interaction of the different photoisomers with the receptor.
A toolbox of molecular photoswitches to modulate the CXCR3 chemokine receptor with light
TLDR
Investigations of positional and substituent effects reveal that halogen substituents on the ortho-position of the outer ring are preferred for conferring partial agonism on the cis form of the ligands, which can aid in new photopharmacology studies of CXCR3 signaling.
Optical Control of Adenosine-Mediated Pain Modulation
TLDR
The results demonstrate that a photoswitchable adenosine derivative can be used to map the contribution of ARs mediating analgesia in vivo and suggest a major role for A1R and A3R in peripheral-mediated pain sensitization.
"Photo-Rimonabant": Synthesis and Biological Evaluation of Novel Photoswitchable Molecules Derived from Rimonabant Lead to a Highly Selective and Nanomolar "Cis-On" CB1R Antagonist.
TLDR
It is established that 16a is highly selective for hCB1R over hCB2R, which can be valuable molecular tools for optical modulation of CBRs and better understanding of disorders associated with the endocannabinoid system.
Triggered azobenzene-based prodrugs and drug delivery systems.
...
1
2
...

References

SHOWING 1-10 OF 84 REFERENCES
A Photoswitchable Dualsteric Ligand Controlling Receptor Efficacy.
TLDR
BQCAAI proved to be an unprecedented molecular tool; it is the first photoswitchable dualsteric ligand, and its activity can be regulated by light, and it was applied to investigate the time course of several receptor activation processes.
In Vivo Photopharmacology.
TLDR
An overview of photopharmacology using synthetic switches that have been applied in vivo, i.e., in living cells and organisms is provided.
Emerging Targets in Photopharmacology.
TLDR
A critical overview of the different pharmacological targets in various organs and a survey of organ systems in the human body that can be addressed in a non-invasive manner are presented.
Specificity and Speed: Tethered Photopharmacology.
TLDR
Genetically encoded, tethered photopharmacology is a variant of optogenetics and could even play a role in medicine wherever gene therapy is viable if sufficiently selective tethering strategies that operate on wild-type receptors can be developed.
Optical Control of Dopamine Receptors Using a Photoswitchable Tethered Inverse Agonist.
TLDR
The results indicate that DARs can be chemically engineered for selective remote control by light and provide a template for precision control of Family A GPCRs.
Optical control of endogenous receptors and cellular excitability using targeted covalent photoswitches
TLDR
Targeted covalent photoswitches constitute a new class of light-regulated drugs and act as prosthetic molecules that photocontrol the activity of GluK1-expressing neurons, and restore photoresponses in degenerated retina.
Optogenetic pharmacology for control of native neuronal signaling proteins
TLDR
This work has shown that covalently attaching photoswitch molecules to genetically tagged proteins, the newly emerging methodology of optogenetic pharmacology allows biochemically precise control in targeted subsets of neurons.
...
1
2
3
4
5
...