Molecular Pharmacology of G protein-coupled receptors (MolPharmGPCR)
G protein-coupled receptors (GPCRs) constitute a principal family of therapeutic targets in many disease areas. We study specific members of this receptor family with the aim of deciphering novel aspects of their pharmacology and signalling that could potentially lead to improved therapies. We focus on GPCRs that constitute well-validated therapeutic targets in diseases with unmet medical need, as well as on poorly explored GPCRs that emerge as of potential physio-pathologically relevance, with particular interest in Central Nervous System diseases.
Among our specific aims are to identify and characterize small-molecule ligands and mechanisms of action for pharmacological modulation of GPCR function leading to specific cellular responses. We carry out in vitro and cell-based pharmacological assays involving biochemistry, cell and molecular biology, and biomolecular imaging techniques. Much of our research is done in collaboration with biocomputational and medicinal chemistry groups. Our final goal is to advance the knowledge in the field of GPCR pharmacology to open pads to more efficacious and safer drugs targeting this receptor family.
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Líneas de investigación
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Líneas de investigación
- Investigation of novel mechanisms of pharmacological modulation of GPCR function such as allosterism and biased signalling. We carried out this research particularly on targets on which the group accumulates expertise, and for which we can count on medicinal chemistry and structural support. We believe the exploration of new aspects of GPCR pharmacology not exploited by current drugs might result therapeutically advantageous both on emerging as well as on well-validated, historical GPCR therapeutic targets.
- Elucidation of components of the intracellular signalling of GPCRs leading to specific cell response, and potentially susceptible of selective pharmacological modulation. We aim at integrating basic and molecular pharmacological findings into the context of specific cellular responses. For this we study aspects of intracellular signalling such as kinetics and subcellular location with temporal and spatial resolution using biosensors/imaging and disruption strategies among other approaches.
- Sustained surveillance on potential innovative GPCR targets in areas of unmet medical need. We undertake basic research on emerging targets combined with expansion of their small-molecule pharmacology toolbox to gather knowledge and provide pharmacological probes for speeding up target validation/valorisation.
Miembros
Publicaciones seleccionadas
Allosteric modulation of dopamine D2L receptor in complex with Gi1 and Gi2 proteins: the effect of subtle structural and stereochemical ligand modifications
Knowledge-Based Design of Long-Chain Arylpiperazine Derivatives Targeting Multiple Serotonin Receptors as Potential Candidates for Treatment of Autism Spectrum Disorder
Synthesis, pharmacological and structural studies of 5-substituted-3-(1-arylmethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as multi-target ligands of aminergic GPCRs
Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It
Resultados seleccionados
Alianzas
