Publications by authors named "M Gomez-Canas"
This chapter aims to elucidate an example of the drug development process for a G protein-coupled receptor (GPCR), focusing specifically on the cannabinoid receptors CB and CB. Various techniques can be employed for different purposes when characterizing a new compound targeting these receptors.Initially, the compound affinity for both cannabinoid receptors is assessed through binding competition assays.
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- GPR55 is a unique G-protein coupled receptor with limited known ligands, which hampers further research into its functions.
- Research focused on developing new compounds based on a previously identified antagonist, ML192, using a thienopyrimidine structure.
- The new compounds were tested for their ability to inhibit GPR55 activity, showing some promising candidates that selectively targeted GPR55 without affecting CB1 and CB2 cannabinoid receptors.
Cannabis plant has been used from ancient times with therapeutic purposes for treating human pathologies, but the identification of the cellular and molecular mechanisms underlying the therapeutic properties of the phytocannabinoids, the active compounds in this plant, occurred in the last years of the past century. In the late 1980s and early 1990s, seminal studies demonstrated the existence of cannabinoid receptors and other elements of the so-called endocannabinoid system. These G protein-coupled receptors (GPCRs) are a key element in the functions assigned to endocannabinoids and appear to serve as promising pharmacological targets.
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- Cannabinoids, especially through CB receptors and GPR55, have shown neuroprotective effects in preclinical models of neurodegenerative diseases, sparking significant research interest.
- The study tested a compound called VCE-006.1, which acts on GPR55, and found it effective in reversing motor defects and neuron loss in models of Parkinson's disease, although it had limited effects on inflammatory reactions.
- Despite showing some protective benefits in models of neurodegeneration, the compound did not alter GPR55 expression levels, potentially explaining its varied effectiveness in different experimental setups.