A5043012246- Cannabis and Cannabinoid Research
- Receptor Mechanisms and Signaling
- Monoclonal and Polyclonal Antibodies Research
- Computational Drug Discovery Methods
- Chemokine receptors and signaling
- Neurotransmitter Receptor Influence on Behavior
- Neuroscience and Neuropharmacology Research
- Diet and metabolism studies
- Genomics and Rare Diseases
- Neuroscience of respiration and sleep
- Biotin and Related Studies
- Pharmacological Effects and Assays
- Epilepsy research and treatment
- Sleep and Wakefulness Research
- Cytokine Signaling Pathways and Interactions
- Chemical Synthesis and Analysis
- Protein purification and stability
- Drug Transport and Resistance Mechanisms
- Boron Compounds in Chemistry
- Neurogenetic and Muscular Disorders Research
- Pharmacological Receptor Mechanisms and Effects
- Neuropeptides and Animal Physiology
- Biochemical effects in animals
- Hereditary Neurological Disorders
University of the Basque Country
2021-2025
University of Nottingham
2021-2025
University of Birmingham
2021-2025
University of California, San Diego
2023-2025
Palobiofarma (Spain)
2025
University of Montana
2025
Centro de Investigación Biomédica en Red de Salud Mental
2021
Queen's Medical Centre
2021
Allosteric modulation of cannabinoid receptor type 1 (CB1R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs). Currently, CB1R allosteric modulators (AMs) are characterized based on their ability modulate binding or functional response OLs, preventing isolation individual contributions by and ligands. Herein, we develop the first fluoroprobe attendant FRET‐based assay allowing for direct profiling AMs without coincubation with an OL. Our...
Allosteric modulation of cannabinoid receptor type 1 (CB1R) offers a promising alternative to conventional therapeutic approaches using orthosteric ligands (OLs). Currently, CB1R allosteric modulators (AMs) are characterized based on their ability modulate binding or functional response OLs, preventing isolation individual contributions by and ligands. Herein, we develop the first fluoroprobe attendant FRET‐based assay allowing for direct profiling AMs without coincubation with an OL. Our...
CC chemokine receptor (CCR) 5 promotes inflammatory responses by driving cell migration and scavenging chemokine. A CCR5 inhibitor Maraviroc has been approved for blocking HIV entry; however, inhibitors the treatment of other diseases have had limited success, likely because complexity pharmacology biology. is activated natural engineered chemokines that elicit distinct signaling trafficking responses, including sequestration inside cell. Intracellular may be therapeutically exploitable as a...
The kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important optimization parameter in drug discovery. Traditional radioligand assays are labor-intensive, preventing their application at the early stages Fluorescence-based offer several advantages, including a possibility develop homogeneous format, continuous data collection, and higher throughput. This study sought fluorescence-based assay investigate ligand-binding human cannabinoid type 1 2 (CB1R CB2R). We...
The cannabinoid receptor 2 (CB2R) is of considerable therapeutic and scientific interest. Hence, the discovery novel molecules that target modulate this receptor, ideally selectively over its closest relative, 1, great importance. In study, we aimed to discover ligands targeting CB2R using large library in silico docking screens. However, since binding site difficult with methods due hydrophobic nature, used a variety screening approaches, including placement water predicted sites site,...
Abstract G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism ligands that bind them. Ligands exert their action via interactions in ligand binding pocket. We hypothesized there a common set receptor made by diverse structures mediate and among large dataset different ligands, functionally important will be over‐represented. computationally docked ~2700...
The transient receptor potential vanilloid 1 (TRPV1) is a non-selective ligand-gated cation channel involved in synaptic transmission, plasticity, and brain pathology. In the hippocampal dentate gyrus, TRPV1 localizes to dendritic spines dendrites postsynaptic excitatory synapses molecular layer (ML). At these same synapses, cannabinoid CB (CB R) activated by exogenous endogenous cannabinoids presynaptic terminals. Hence, as both receptors are anandamide, co-localize, mediate long-term...
Specific and selective anti-CB1 antibodies are among the most powerful research tools to unravel complex biological processes mediated by CB1 receptor in both physiological pathological conditions. However, low performance of remains a major source inconsistency between results from different laboratories. Using variety techniques, including some commonly accepted ones for antibody specificity testing, we identified three five commercial against regions as best choice specific end-use...
CC chemokine receptor 5 (CCR5) promotes inflammatory responses by driving cell migration and scavenging to shape directional gradients. A CCR5 inhibitor has been approved for blocking HIV entry into cells. However, targeting the treatment of other diseases had limited success, likely because complexity pharmacology biology. is activated natural engineered chemokines that elicit distinct signaling trafficking responses, including sequestration inside cell. Intracellular may be therapeutically...
Abstract By driving monocyte chemotaxis, the chemokine receptor CCR2 shapes inflammatory responses and formation of tumor microenvironments. This makes it a promising target in inflammation immuno-oncology; however, despite extensive efforts, there are no FDA-approved CCR2-targeting therapeutics. Cited challenges include redundancy system, suboptimal properties compound candidates, species differences that confound translation results from animals to humans. Structure-based drug design can...
Abstract Background Replacement of radioligand binding assays with antibody-antigen interaction-based approaches for quantitative analysis G protein-coupled receptor (GPCR) levels requires the use purified protein standards containing antigen. GPCRs in general and cannabinoid CB 1 particular show a progressive tendency to aggregate precipitate aqueous solution outside their biological context due low solubility that hydrophobic nature imprinted by seven transmembrane domains. This renders...
<b>Abstract ID 131403</b> <b>Poster Board 569</b> Chemokine receptors 2 and 5 (CCR2 CCR5, respectively) are highly homologous G-protein coupled on the surface of select immune cells with distinct functions endogenous agonists but shared antagonists. These chemokine promising targets for small molecule therapeutics in treatment various cancers autoimmune diseases, despite only one currently approved therapeutic CCR5. Rational design future relies a structural understanding determinants...
Abstract INTRODUCTION The kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important determining factor in the preclinical evaluation a molecule. Therefore, efforts should be made measure this property as part any drug development plan. original assays used assess were developed using radioligands. However, these types are very labor-intensive, limiting their application later phases discovery process. Recently, fluorescence-based have been for multiple GPCRs,...
Alboko esklerosi amiotrofikoa (AEA) gaixotasun neurodegeneratibo heterogeneo eta sendaezina da. Goiko beheko neurona motorren endekapena bizkarmuineko alboko kordoiaren esklerosia dira zigilu histopatologiko nagusiak. Adierazpen klinikoetan aldakortasun handia dagoen arren, ahultasun orokorra, faszikulazioak espasmoak gertatzen endekapenaren muskulu-atrofiaren ondorioz, baita portaera- kognizio-asaldurak ere garuneko kalte zabala dela eta. Mutazio genetikoek gaixotasunaren bi adierazpen...
Abstract G protein coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism ligands which bind them. Ligands exert their action via interactions in ligand binding pocket. We hypothesised that there a common set receptor made by diverse structures mediate and among large dataset different ligands, functionally important will be over-represented. computationally docked...