2767 search results for “g protein-coupled receptor” in the Public website
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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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Allosteric modulation by sodium ions and amilorides of G protein- coupled receptors
Promotor: A.P. IJzerman
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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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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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Adriaan IJzermanWiskunde en Natuurwetenschappen
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Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors
Supervisor: Xue Yang
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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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Clavis Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands
Promotores: A.P. IJzerman, H.W.T. van Vlijmen
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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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Biophysical characterization of membrane protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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Laura HeitmanWiskunde en Natuurwetenschappen
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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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Natalia Ortiz ZacariasWiskunde en Natuurwetenschappen
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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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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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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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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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Tailored medicines
Medicines do not follow the one size fits all principle, because genetic differences can influence their efficiency. That is what research by PhD candidate Julia Hillger shows. She defends her PhD dissertation Take it Personal on Thursday 7 December.
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The activation mechanisms of G protein-coupled receptors
PhD Defence
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Allosteric modulation by sodium ions and amilorides of G protein- coupled receptors
PhD Defence
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Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
PhD Defence
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Binding mode characterization using free energy perturbations
Supervisors: Bart Lenselink (Leiden University) / Willem Jespers (Uppsala University)
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The Role of Target Binding Kinetics in Drug Discovery
Source: ChemMedChem (2015)
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Novel receptor concepts
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Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
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Mutating GPCRs
Supervisors: Willem Jespers (Uppsala University), Gerard van Westen (LACDR), David Gloriam (Copenhagen University)
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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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Inverse Agonism and Constitutive Activity
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Division of Drug Discovery & Safety
We are interested in the efficacy and safety of new drugs and novel means to decipher these aspects. Hence, we employ advanced imaging and high-throughput screening techniques next to computational approaches such as chem- and bioinformatics.
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Receptor Residence Time
Research question
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Schmidt Lab
Intrigued by the way cells autonomously regulate their fate, we strive to understand and visualize cellular processes as the basis of Cell Signaling.
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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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Receptor bioinformatics and pharmacogenomics
Research question
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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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Kinetics for drug discovery – The first step towards an improved drug discovery paradigm
Supervisor: Indira Nederpelt
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Research
The current projects of the Molecular Physiology group focus on kinases and proteins of the endocannabinoid system.
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Drug Discovery & Safety
In the research programme Drug Discovery & Safety, we are interested in the efficacy and safety of new drugs and novel means to decipher these aspects. Hence, we employ advanced imaging and high-throughput screening techniques next to computational approaches such as chem- and bioinformatics.
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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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Prediction of binding Kinetics
Supervisor: Gerard van Westen
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Research
The research conducted at the Leiden Academic Centre for Drug Research is clustered within the divisions of BioTherapeutics, Drug Discovery & Safety and Systems Biomedicine and Pharmacology.
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Publications
Here you can find our most recent research publications
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Allosteric Modulation
Allosteric modulation has long been recognized as a general and widespread mechanism for the control of protein function. Modulators bind to regulatory sites distinct from the active site on the protein, resulting in conformational changes that may profoundly influence protein function. This concept…
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Physicochemical analysis of allosteric binding pockets
Supervisor: Gerard van Westen
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Dong Guo won two poster prizes at the FIGON Dutch Medicines Days
Dong Guo was awarded two poster prizes for his poster ‘Molecular Mechanism of Allosteric modulation at G protein-coupled Receptors: Insight from a Binding Kinetics Study at the Human A1 Adenosine Receptor’ at the FIGON Dutch Medicines Days, October 6th-8th this year.
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Medicinal Chemistry
The mission in this research group, headed by Ad IJzerman, is to design and synthesize novel and better ligands for drug targets. Drug discovery is a lengthy but inspiring adventure. It is often an interplay between academic institutes and pharmaceutical industry, in which scientists at university develop…
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Personalized Medicine
Getting personal
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Why Leiden University?
We are committed to provide you with meaningful, rigorous and quality graduate experiences in a personalized environment with a cutting edge research infrastructure and internationally renowned supervisors.
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Dr. Gerard van Westen receives VENI grant
Gerard van Westen (LACDR/division of medicinal chemistry) has been awarded with a VENI grant from NWO, the Dutch Research Council.
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Allosterism
The recognition that there may be more, so-called allosteric binding sites on a given receptor has also fueled our synthetic efforts. Over the last few years we have focused on many drug targets (adenosine A1, A2A and A3 receptors, the mGlu2 receptor and a classic ‘anti-target’, the hERG channel) to…