2,933 search results for “gpcrs g protein” in the Public website
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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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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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Biophysical characterization of membrane protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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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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Advances in GPCR Modeling Evaluated by the GPCR Dock 2013 Assessment: Meeting New Challenges
Source: Structure , Volume 22, Issue 8, pp. 1120-1139 (2014)
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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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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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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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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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Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors
Supervisor: Xue Yang
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Towards improved drug 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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In silico characterization of a GPCR focused library
Supervisor: Gerard van Westen
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The advantages and disadvantages of bioorthogonal proteins
This thesis describes the use of bioorthogonal proteins in immunological settings. It provides an introduction towards the field of protein modification, which was used throughout the thesis for the expression of proteins containing unnatural amino acids.
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Time is of the essence: investigating kinetic interactions between drug, endogenous neuropeptides and receptor
Promotor: A.P. IJzerman Co-promotor: L.H. Heitman
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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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Protein Facility
The Protein Centre can supply you with purified proteins that are essential for many experiments, ranging from in vitro inhibitor screening and enzymatic analysis to manipulation of life cells.
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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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NMR studies of protein-small molecule and protein-peptide interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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NMR structural studies of protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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Spin-label EPR Approaches to Protein Interactions
Promotor: Prof.dr. E.J.J. Groenen
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Unravelling proteins by touch
How can we develop a new microscope that can distinguish individual atoms in proteins?
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Morphogenesis and protein production in Aspergillus niger
Promotor: Prof.dr. C.A.M.J.J. van den Hondel, Dr. ir. V. Meyer, Co-promotor: Dr. A.F.J. Ram
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Oxidation of Therapeutic Proteins and Peptides: Structural and Biological Consequences
Oxidation is a common degradation pathway that affects therapeutic proteins and peptides during production, purification, formulation, transportation, storage and handling of solid and liquid preparations. In the present work we review the scientific literature about structural and biological consequences…
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solvent free supercritical fluid spray drying process for producing dry protein formulations
In this study, we evaluated the influence of supercritical carbon dioxide (scCO2) spray drying conditions, in the absence of organic solvent, on the ability to produce dry protein/trehalose formulations at 1:10 and 1:4 (w/w) ratios.
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The road 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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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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Molecular engineering of plant development using Agrobacterium-mediated protein translocation
Supervisor: P.J.J. Hooykaas Co-Supervisor: R. Offringa
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Pharmaceutical Aspects of Subvisible Particles in Protein Formulations
Promotor: W. Jiskoot, Co-promotor: A. Hawe
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Activity-based protein profiling of diacylglycerol lipases
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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G TavillaFaculteit Geneeskunde
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G Kleiverda
Faculteit Geneeskunde
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G Jukema
Faculteit Geneeskunde
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Visualization of effector protein translocation from Agrobacterium tumefaciens into host cells
In our research protein translocation from Agrobacterium into yeast and plant cells is studied to obtain fundamental insights in the translocation process
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Activity-based protein profiling in drug discovery
In the last decades, activity-based protein profiling (ABPP) has emerged as a powerful chemical tool that may aid the ever-challenging drug discovery process.
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Fluorescence Polarization Activity-Based Protein Profiling on Retaining Glycosidases
Glycosidases are important enzymes in the turnover of polysaccharides and glycoconjugates, and are involved in a range of human pathologies including genetic disorders such as Gaucher and Pompe disease, but also in various cancers.
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Activity-based protein profiling of glucosidases, fucosidases and glucuronidases
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-promotor: B.I. Florea
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Protein motions revealed by paramagnetic NMR spectroscopy
Hass
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Efficient targeting of the Trichoderma genome for industrial protein engineering
The research is aimed at development of an efficient gene targeting method that allows controlled integration of DNA at a preselected site in the Trichoderma genome.
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CRISPR Cas-induced targeted mutagenesis with Agrobacterium mediated protein delivery
The RNA guided endonuclease based on the CRISPR/Cas system of Streptococcus pyogenus is a potent new tool for genome engineering in plants.
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Bioorthogonal Chemistry: Applications in Activity-Based Protein Profiling
The close interaction between organic chemi stry and biology goes back to the late 18th century, when the modern natural sciences began to take shape. After synthetic organic chemistry arose as a discipline, organic chemists almost immediately began to pursue the synthesis of naturally occurring compounds,…
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G van Drunen
Faculteit Geneeskunde
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G Trimbos-Kemper
Faculteit Geneeskunde
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Supercritical carbon dioxide spray drying for the production of stable dried protein formulations
Promotor: W. Jiskoot, Co-promotor: H.A. Every
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In vivo tracking and biodistribution of protein aggregates
Therapeutic proteins have revolutionized the treatment of many severe diseases like multiple sclerosis, haemophilia, diabetes and many more. Unfortunately, even recombinant proteins with structures (almost) identical to those of their endogenous counterparts often induce the formation of anti drug antibodies…
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Activity-based protein profiling reveals off-target proteins of the FAAH inhibitor BIA 10-2474, SCIENCE, 2017
The drug BIA 10-2474 inhibits fatty acid amide hydrolase (FAAH), a lipase that degrades a specific endocannabinoid. On the basis of this activity, BIA 10-2474 was being developed as a potential treatment for anxiety and pain. In a phase 1 trial of the drug, one subject died, and four others suffered…
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Making the invisible visible: paramagnetic NMR and the transient protein complex
Promotor: Prof.dr. M. Ubbink
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Innovative analytical approaches for protein aggregates and other particulate matter impurities
Developing robust and comprehensive analytical methods to size and quantify subvisible particles in biopharmaceutical products.
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Agrobacterium-mediated protein therapy for genome editing
Is translocation of nucleases possible via Agrobacterium T4SS and is it efficient enough for mutagenesis?