627 zoekresultaten voor “liver x receptors” in de Publieke website
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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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Dyslipidemia at the crossroad of the skin barrier and the arterial wall
The research described in this thesis shows that hypercholesterolemia, a well-established risk factor for atherosclerosis, can impact skin lipid pool and barrier function already at young age. In the field of atherosclerosis, we showed that the small peptide Lyp-1 can be used as a targeting molecule…
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Polymers in the Liver: Metabolism and Regulation
Metabolic diseases are a burden on the European population and health care system. It is increasingly recognised that individual differences with respect to history, lifestyle, and genetic make-up affect disease progression and treatment response. A Systems Medicine approach, based on computational…
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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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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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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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Novel receptor concepts
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Receptor Residence Time
Research question
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yeast system delineates the 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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High throughput microscopy of mechanism-based reporters in druginduced liver injury
Promotor: B. van de Water
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X. LiWiskunde en Natuurwetenschappen
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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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3rd International Workshop on Klinefelter Syndrome, Trisomy X, and XYY
Congres/symposium, Workshop
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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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Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
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Improving survival prediction models for liver transplantation candidates
Promotie
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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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PHD candidate, Mathematical modeling for prediction of liver toxicity
Wiskunde en Natuurwetenschappen, Leiden Academic Centre for Drug Research (LACDR)
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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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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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cellular stress pathways for mechanistic understanding of chemical-induced liver injury
Cellular stress response pathways are activated upon exposure to chemicals and help organisms deal with various molecular dangers (e.g. oxidative stress). When these pathways become hyper-activated an adverse response takes place and cells die, which may lead to organism-level toxicity such as drug-induced…
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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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microscopy to unravel cellular stress response signalling in drug induced liver injury
Promotor: B. van de Water
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Volume X 2016
Perspectives on Terrorism 2016
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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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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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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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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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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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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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3rd International Workshop on Klinefelter Syndrome, Trisomy X and XYY,
Congres/symposium
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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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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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The Old Observatory x DOORS: Innovating Audience Engagement
Announcement
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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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Neurodevelopmental risks in young children with an extra X or Y chromosome
This longitudinal study is focused on neurodevelopmental problems in young children with XXY, XXX and XYY, aged 1 to 6 years.
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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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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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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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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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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?