306 search results for “g protein-coupled receptor” in the Public website
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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?
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Kinetics for drug discovery – The first step towards an improved drug discovery paradigm
Supervisor: Indira Nederpelt
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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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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 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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Inverse Agonism and Constitutive Activity
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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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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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Jose G. Vallarino
PhD at Molecular Biology and Biochemistry Department, University of Malaga - Spain
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Erica G. Wilson
PhD at the Natural Products Laboratory, Institute of Biology, Leiden University - the Netherlands
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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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space smarter: Artificial intelligence in drug design for G protein-coupled receptors
PhD Defence
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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…
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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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Prof. G. Rozenberg
LIACS prof. Grzegorz Rozenberg is one of the world leaders in research on Theoretical Computer Science and Natural Computing. He is often called the guru of Natural Computing.
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Prof. G. Rozenberg
LIACS prof. Grzegorz Rozenberg is one of the world leaders in research on Theoretical Computer Science and Natural Computing. He is often called the guru of Natural Computing.
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Johannes (Hans) G.E.M. Fraaije
Science
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Physicochemical analysis of allosteric binding pockets
Supervisor: Gerard van Westen
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Natalia Ortiz Zacarias
Science
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Personalized Medicine
Getting personal
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Political Ideas of B.G. Tilak
On 12 April 2022 Alok Oak successfully defended a doctoral thesis and graduated.
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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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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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G.F. Stout and the Psychological Origins of Analytic
The philosopher and psychologist G.F. Stout was the teacher of Moore and Russell around 1894. This book shows that Stout's ideas have played a role in Moore and Russell's development from their early idealism towards analytic realism, where Stout's ideas often find their origin in early phenomenolog…
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Molecular 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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Targeting of antigen-presenting cells with mannosylated conjugates
This thesis describes the development of a variety of mannosylated conjugates. Antigen presenting cells bear mannoside recognizing receptors that actively transport antigen into the cell. This thesis exploits this feature for the development of improved vaccines.
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Self adjuvanting immunopeptides: Design and synthesis
Chapter 2 describes a post-synthetic methodology to introduce a fluorescent label in highly lipophilic, Pam3Cys based conjugates.
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Movements of steroid receptors inside the cell nucleus unraveled
Advanced fluorescence microscopy techniques have revealed how steroid receptors move inside the nucleus. The results were published by a team from Leiden University and the Erasmus Medical Center in Rotterdam, led by IBL-researcher Marcel Schaaf.
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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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Marcel Schaaf
Science
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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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Towards a mechanistic understanding of nanoparticle behavior using zebrafish
The work described in this dissertation contributes to a better mechanistic understanding of nanoparticles in vivo. To achieve that goal, we used the zebrafish as a highly predictive pre-screening model of nanoparticles.
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Key innate immune components controlling intracellular infection
Promotor: Prof.dr. H.P. Spaink, Co-promotor: Prof.dr. A.H. Meijer
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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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Islam at 250: Studies in Memory of G.H.A. Juynboll
Islam at 250: Studies in Memory of G.H.A. Juynboll is a collection of original articles on the state of Islamic sciences and Arabic culture in the early phases of their crystallization.
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KNMP student prize for Bio-Pharmaceutical Sciences student Jacqueline Gerritsen
During the congress of the Royal Dutch Association for the Advancement of Pharmacy (Koninklijke Nederlandse Maatschappij ter bevordering der Pharmacie, KNMP) Jacqueline Gerritsen, former student Bio-Pharmaceutical Sciences at Leiden University, was awarded the KNMP student prize.
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Two young female Leiden researchers join Oncode
The Oncode Institute is a new international network organisation that focuses on making sure that new scientific findings on cancer are implemented in patients as rapidly as possible. Two young female researchers at Leiden University have been selected to join Oncode: Laura Heiman (Leiden Academic…
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Benelux Nuclear Receptor Meeting
Conference
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Synthesis of cyclic peptides as bioconjugation platforms
Cyclic peptides are investigated as a platform to induce different orientations between various ligands.
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Targeting the adenosinergic system
Adenosine is an endogenous ligand which exerts its action by activating adenosine receptors (ARs), while its circulating levels are controlled via a variety of mechanism and proteins, amongst others the equilibrative nucleoside transporters (ENTs).
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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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Daniëlle Hamstra
Faculteit der Sociale Wetenschappen
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Chemokine signaling in Tuberculosis and Salmonella infection
Who benefits from CXCR/CXCL chemokine signaling during infection: host or pathogen?
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Innate immune defence against intracellular pathogens
What are the host immune defence mechanisms that control intracellular infections and how are these subverted by pathogens?
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Focus on kinetics for better drug development
Potential drugs that seem promising in the lab, but don’t show any activity in a person: they cost the industry an incredible amount of time and money. That’s why Indira Nederpelt focuses on a more efficient search for new drugs in her PhD, by determining the kinetics of a potential drug earlier on…
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Computational Drug Discovery
Research in this group, headed by Gerard van Westen, focusses on computational methods integrated in different parts of the drug discovery process. More specifically, topics include innovative treatments for cancer, selectivity modeling, translational research, allosteric modulation, drug resistance…
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Laura Heitman appointed as Professor of Molecular Pharmacology
As of 1 November, Laura Heitman has been appointed full Professor of Molecular Pharmacology at the Leiden Academic Centre for Drug Research (LACDR). Heitman has been working on the understanding and improvement of drug-receptor interactions in early drug discovery. ‘My ultimate aim is to make medicines…