459 zoekresultaten voor “cannabinoid receptor 2” in de Publieke website
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Chemical tools to study the cannabinoid receptor type 2
The cannabinoid receptor type 2 (CB2R) is associated with several inflammatory diseases with an unmet medical need (e.g. Alzheimers, multiple sclerosis, reumatoid arthritis). Development of new chemical biology strategies to study this protein is essential to aid future development of drugs for these…
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Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
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Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
The present thesis focuses on the pharmacological concept of drug-target interaction, which dates back to the beginning of modern pharmacology.
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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity, Nat. Commun., 2017
The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB2R, their selectivity, molecular mode of action and pharmacokinetic properties have…
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Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines
Source: Biosens Bioelectron, Volume 74, pp. 233-42 (2015)
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Pain relief without the high
Researchers at Leiden University led by Mario van der Stelt (Leiden Institute for Chemistry) have set ‘gold standards’ for developing new painkillers based on the medicinal effects of cannabis. Publication in Nature Communications.
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Synthetic carbohydrate ligands for immune receptors
One of the main challenges in the development of an effective anti-cancer vaccine is the generation of an adequate and directed cellular immune response.
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Novel receptor concepts
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Receptor Residence Time
Research question
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biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2)
Source: Bioorg Med Chem, Volume 23, Issue 14, pp. 4034-49 (2015)
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activation mechanisms of G protein-coupled receptors: the case of the adenosine A2B and HCA2/3 receptors
Promotor: A.P. IJzerman
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Physiological significance of the glucocorticoid and mineralocorticoid receptor signaling in the innate immune system
Does the mineralocorticoid receptor play a role in the effects of cortisol and synthetic glucocorticoids on the immune response?
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Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors
Supervisor: Xue Yang
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Liver X receptor: therapeutic targeting of common pathways in Psoriasis and Cardiovascular co-morbidities
Both psoriasis and atheroslcerosis are diseases characterized by a chronic and systemic inflammatory profile with local lipid disturbances that alter the barrier function of the skin (psoriasis) and cause the development of atherosclerotic plaques (atherosclerosis).
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Quantitative live cell imaging of glucocorticoid receptor dynamics in the nucleus
In this thesis, the focus lies on studying glucocorticoid receptor dynamics in living cells with the aim of understanding how this transcription factor finds its DNA target sites to regulate transcription.
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More effective blocking of CCR2 receptor
The discovery of new medicines is a tedious and lengthy process. On average, over 10,000 molecules need to be studied for one to become a drug and reach the patient. Part of that process are the very costly clinical trials in humans, and candidate drugs often fail due to side effects or lack of efficacy.…
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Chemical tools to study the cannabinoid receptor type 2
Promotie
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Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists
Structure-affinity relationship (SAR) and structure-kinetics relationship (SKR) studies were combined to investigate a series of biphenyl anthranilic acid agonists for the HCA2 receptor.
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Drug-target residence time: a case for the adenosine A1 and A2A receptors
Promotor: Prof.dr. A.P. IJzerman, Co-Promotor: Dr. L.H. Heitman
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Better ligands for G Protein-Coupled Receptors
The receptor nomenclature committee of IUPHAR, the International Union of Pharmacology, has several subgroups. Among these are a few that our division is involved in, those for adenosine, nicotinic acid, and GnRH receptors.
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Intracellular allosteric modulators for human CC chemokine receptors
Supervisor: Natalia Ortiz Zacarías
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Sodium ion binding pocket mutations and adenosine A2A receptor function
Source: Mol Pharmacol, Volume 87, Issue 2, pp. 305-13 (2015)
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The Function of Toll-like receptor 2 in Infection and Inflammation
The function of TLRs in innate immunity has aroused worldwide attention soon after its discovery. Because of the broad functions of TLR2 in innate immunity, the drive for the development of TLR2-targeted vaccines or therapeutic treatments has accelerated in the last decades.
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to insurmountability: Novel avenues to better target CC Chemokine receptors
This thesis explores different avenues to develop insurmountable antagonists for CC Chemokine Receptors, such as CCR1, CCR2 and CCR5.
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Kinetic profiling of positive allosteric modulators of the mGlu2 receptor
Supervisor: Maarten Doornbos
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Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists
Source: Eur J Med Chem, Volume 101, pp. 681-91 (2015)
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screening method to decipher the interaction between the adenosine A2B receptor and the C-terminus of different G protein α-subunits.
Source: Purinergic Signal., Volume 10, Issue 3, pp. 441-53 (2014)
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Kinetics for Drug Discovery: a Case for the Adenosine A3 receptor
Supervisor: Lizi Xia
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Allosteric modulation by sodium ions and amilorides of G protein-coupled receptors
Promotor: A.P. IJzerman
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Allosteric modulation by sodium ions and amilorides of G protein- coupled receptors
Promotor: A.P. IJzerman
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investigating kinetic interactions between drug, endogenous neuropeptides and receptor
Promotor: A.P. IJzerman Co-promotor: L.H. Heitman
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action : target binding kinetics and functional efficacy at the mGlu2 receptor
During the course of drug discovery translational steps are made.
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role of the NPxxY(x)(5,6)F motif and helix 8 of the adenosine A(2B) receptor in G protein coupling
Source: Biochem Pharmacol, Volume 95, Issue 4, pp. 290-300 (2015)
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Agonists for the Adenosine A1 Receptor with Tunable Residence Time. A Case for Nonribose 4-Amino-6-aryl-5-cyano-2-thiopyrimidines
Source: J Med Chem, Volume 57, Issue 8, pp. 3213-22 (2014)
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Cannabinoid receptor 2 agonists on their way to clinics – How industrial drug discovery and academic research can cross-fertilize each other
Lezing, Van Leeuwenhoek Lecture on BioScience
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Indanes-Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors
The indane (2,3-dihydro-1H-indene) ring system is an attractive scaffold for biologically active compounds due to the combination of aromatic and aliphatic properties fused together in one rigid system.
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As High-Affinity and Long-Residence-Time Antagonists for the CCR2 Receptor
Animal models suggest that the chemokine ligand 2/CC-chemokine receptor 2 (CCL2/CCR2) axis plays an important role in the development of inflammatory diseases. However, CCR2 antagonists have failed in clinical trials because of a lack of efficacy.
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Toll-like receptor signaling in the innate immune system of zebrafish larvae
Promotor: H.P. Spaink, A.H. Meijer Co-promotor: R. Marin-Juez
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smarter: Artificial intelligence in drug design for G protein-coupled receptors
Over several decades, a variety of computational methods for drug discovery have been proposed and applied in practice. With the accumulation of data and the development of machine learning methods, computational drug design methods have gradually shifted to a new paradigm, i.e. deep learning methods…
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Determining the structure of a chemotaxis kinase complex with receptor mimetics and cryo-EM
Can we determine the 3D structure of a chemotaxis core complex using single-particle reconstructions via cryo-EM?
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relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists
Source: Org Biomol Chem, Volume 13, Issue 8, pp. 2407-22 (2015)
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Personalized Medicine
Getting personal
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A₃ adenosine receptor allosteric modulator induces an anti-inflammatory effect: in vivo studies and molecular mechanism of action
Source: Mediators Inflamm (2014)
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The endocannabinoid system in zebrafish larvae
In this thesis, we have studied the potential of the zebrafish larval model in studying the ECS, as a complementary model to the existing rodent models.
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Optogenetic activation of intracellular adenosine A2A receptor signaling in the hippocampus is sufficient to trigger CREB phosphorylation and
Source: Mol Psychiatry (2015)
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When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as
Source: Eur J Med Chem (2015)
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Affinity
Designing and synthesizing high-affinity ligands for a given drug target have always been among the more important challenges in the drug discovery process.
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EUFEPS congres
EUFEPS Women in Pharmaceutical Sciences Award for Jara Bouma
- Russian 2
- Persian 2