273 search results for “g protein-coupled receptor” in the Public website
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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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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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Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors
Supervisor: Xue Yang
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The 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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Allosteric modulation by sodium ions and amilorides of G protein-coupled receptors
Promotor: A.P. IJzerman
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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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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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Novel receptor concepts
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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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Receptor Residence Time
Research question
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Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
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Receptor Pharmacology
In this research group, headed by Laura Heitman, novel receptor concepts in drug discovery are studied, aiming to increase the effectivity of medicines. Many drugs act via so-called G protein-coupled receptors (GPCRs) and therefore our research is mainly focused on understanding and improving drug-receptor…
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Adriaan IJzermanScience
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The ins and outs of ligand binding to CCR2
Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: Dr. L.H. Heitman
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Laura HeitmanScience
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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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investigating kinetic interactions between drug, endogenous neuropeptides and receptor
Promotor: A.P. IJzerman Co-promotor: L.H. Heitman
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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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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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Clavis Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands
Promotores: A.P. IJzerman, H.W.T. van Vlijmen
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Allosteric modulation by sodium ions and amilorides of G protein- coupled receptors
Promotor: A.P. IJzerman
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Biophysical characterization of membrane protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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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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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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A chemical biology approach for targeting of ligand-drug conjugates
Promotores: Prof.dr. H. S. Overkleeft, Prof.dr. G. A. van der Marel
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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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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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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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Intracellular allosteric modulators for human CC chemokine receptors
Supervisor: Natalia Ortiz Zacarías
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The Role of Target Binding Kinetics in Drug Discovery
Source: ChemMedChem (2015)
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The activation mechanisms of G protein-coupled receptors
PhD Defence
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Proteins in harmony: Tuning selectivity in early drug discovery
This thesis describes the importance of being able to control the selectivity of potential drug candidates.
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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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Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
PhD Defence
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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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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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Kinetic profiling of positive allosteric modulators of the mGlu2 receptor
Supervisor: Maarten Doornbos
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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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Kinetics for Drug Discovery: a Case for the Adenosine A3 receptor
Supervisor: Lizi Xia
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G TavillaFaculteit Geneeskunde
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G Jukema
Faculteit Geneeskunde
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G Kleiverda
Faculteit Geneeskunde
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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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G van Drunen
Faculteit Geneeskunde
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G Trimbos-Kemper
Faculteit Geneeskunde
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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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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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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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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?