Search Results - "Giraldo, Jesús"
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Structural Assessment of Agonist Efficacy in the μ‑Opioid Receptor: Morphine and Fentanyl Elicit Different Activation Patterns
Published in Journal of chemical information and modeling (22-03-2021)“…Over the past two decades, the opioid epidemic in the United States and Canada has evidenced the need for a better understanding of the molecular mechanisms of…”
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Revealing the Mechanism of Agonist-Mediated Cannabinoid Receptor 1 (CB1) Activation and Phospholipid-Mediated Allosteric Modulation
Published in Journal of medicinal chemistry (13-06-2019)“…Cannabinoid receptor 1 (CB1) mediates the functional responses of Δ9-tetrahydrocannabinol. Although progress has been made in understanding cannabinoid binding…”
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3
Pharmacological evidence for a metabotropic glutamate receptor heterodimer in neuronal cells
Published in eLife (29-06-2017)“…Metabotropic glutamate receptors (mGluRs) are mandatory dimers playing important roles in regulating CNS function. Although assumed to form exclusive…”
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Oligomerization in health and disease: from enzymes to G protein-coupled receptors
Published 28-01-2020“…Oligomerization in Health and Disease: From Enzymes to G Protein-Coupled Receptors, Volume 169 in the Progress in Molecular Biology and Translational Science…”
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Allosteric control of an asymmetric transduction in a G protein-coupled receptor heterodimer
Published in eLife (10-08-2017)“…GPCRs play critical roles in cell communication. Although GPCRs can form heteromers, their role in signaling remains elusive. Here we used rat metabotropic…”
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6
Remote local photoactivation of morphine produces analgesia without opioid‐related adverse effects
Published in British journal of pharmacology (01-04-2023)“…Background and Purpose Opioid‐based drugs are the gold standard medicines for pain relief. However, tolerance and several side effects (i.e. constipation and…”
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Evaluating Allosteric Perturbations in Cannabinoid Receptor 1 by In Silico Single-Point Mutation
Published in ACS omega (25-10-2022)“…Cannabinoid receptor 1 (CB1) is a promising drug target involved in many physiological processes. Using atomistic molecular dynamics (MD) simulations, we…”
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Insights into adenosine A2A receptor activation through cooperative modulation of agonist and allosteric lipid interactions
Published in PLoS computational biology (01-04-2020)“…The activation process of G protein-coupled receptors (GPCRs) has been extensively studied, both experimentally and computationally. In particular, Molecular…”
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Selective Protonation of Acidic Residues Triggers Opsin Activation
Published in The journal of physical chemistry. B (30-07-2015)“…Rhodopsin, the visual pigment in the retina, is a Class A G protein-coupled receptor (GPCR) covalently bound to retinal chromophore. In dark conditions,…”
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10
Distinct Dopamine D₂ Receptor Antagonists Differentially Impact D₂ Receptor Oligomerization
Published in International journal of molecular sciences (04-04-2019)“…Dopamine D₂ receptors (D₂R) are known to form transient homodimer complexes, of which the increased formation has already been associated with development of…”
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ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
Published in British journal of pharmacology (02-06-2024)“…G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals…”
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Illuminating Phenylazopyridines To Photoswitch Metabotropic Glutamate Receptors: From the Flask to the Animals
Published in ACS central science (25-01-2017)“…Phenylazopyridines are photoisomerizable compounds with high potential to control biological functions with light. We have obtained a series of…”
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Computational Analysis of Negative and Positive Allosteric Modulator Binding and Function in Metabotropic Glutamate Receptor 5 (In)Activation
Published in Journal of chemical information and modeling (27-05-2014)“…Metabotropic glutamate receptors (mGluRs) are high-profile G-protein coupled receptors drug targets because of their involvement in several neurological…”
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Synthesis toward Bivalent Ligands for the Dopamine D2 and Metabotropic Glutamate 5 Receptors
Published in Journal of medicinal chemistry (27-09-2018)“…In this study, we designed and synthesized heterobivalent ligands targeting heteromers consisting of the metabotropic glutamate 5 receptor (mGluR5) and the…”
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Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator
Published in eLife (11-04-2017)“…Light-operated drugs constitute a major target in drug discovery, since they may provide spatiotemporal resolution for the treatment of complex diseases (i.e…”
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16
Characterization of the Calcium-mediated Response to Alkaline Stress in Saccharomyces cerevisiae
Published in The Journal of biological chemistry (15-10-2004)“…Exposure of the yeast Saccharomyces cerevisiae to alkaline stress resulted in adaptive changes that involved remodeling the gene expression. Recent evidence…”
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Follow-Up Genotoxic Study: Chromosome Damage Two and Six Years after Exposure to the Prestige Oil Spill
Published in PloS one (29-07-2015)“…The north-west coast of Spain was heavily contaminated by the Prestige oil spill, in 2002. Individuals who participated in the clean-up tasks showed increased…”
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Persistence of Breakage in Specific Chromosome Bands 6 Years after Acute Exposure to Oil
Published in PloS one (01-08-2016)“…The identification of breakpoints involved in chromosomal damage could help to detect genes involved in genetic disorders, most notably cancer. Until now, only…”
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Genomewide Screen for Tolerance to Cationic Drugs Reveals Genes Important for Potassium Homeostasis in Saccharomyces cerevisiae
Published in Eukaryotic Cell (01-09-2011)“…Potassium homeostasis is crucial for living cells. In the yeast Saccharomyces cerevisiae, the uptake of potassium is driven by the electrochemical gradient…”
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Shining Light on an mGlu5 Photoswitchable NAM: A Theoretical Perspective
Published in Current neuropharmacology (01-07-2016)“…Metabotropic glutamate receptors (mGluRs) are important drug targets because of their involvement in several neurological diseases. Among mGluRs, mGlu5 is a…”
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