285 search results for “adenosine receptor” in the Public website
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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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Proteochemometrics
Research question
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Binding kinetics
A tantalizing concept that has emerged in our recent research is binding kinetics. An important parameter is residence time (RT), a direct reflection of how long a drug stays bound to its target. This parameter is of crucial importance, because drug action lasts only as long as the receptor-ligand complex…
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Metabolic Characterization of Marine Sponge
Which metabolites of sponge are influenced by individual environmental or biological factors?
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Data-Driven Drug Discovery Network (D4N)
The Data-Driven Drug Discovery Network (D4N) is an initiative by researchers from Leiden University and collaborators to join efforts in applying and developing novel techniques from data science to drug discovery and related topics from bioinformatics.
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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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Julia Hillger wins first prize during FIGON PhD poster competition
Drs. Julia Hillger won the first prize for the category
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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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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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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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Marcel Schaaf
Science
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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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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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Key innate immune components controlling intracellular infection
Promotor: Prof.dr. H.P. Spaink, Co-promotor: Prof.dr. A.H. Meijer
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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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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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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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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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Adriaan IJzerman
Science
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Biophysical characterization of membrane protein-small molecule interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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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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Sensing Transport
Solute carrier (SLC) transporters are a large and diverse class of relatively understudied transmembrane proteins.
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Laura Heitman
Science
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Natalia Ortiz Zacarias
Science
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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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Ad IJzerman wins prestigious Nauta Pharmacochemistry Award
Professor of Pharmacochemistry Ad IJzerman has won the Nauta Award for his years of research into signal processing proteins that are interesting for the development of new medications: G protein coupled receptors. The prize is awarded every two years for services to pharmacochemistry and chemical b…
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The Role of Target Binding Kinetics in Drug Discovery
Source: ChemMedChem (2015)
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Marjolein Soethoudt wins Unilever Research Prize
Marjolein Soethoudt was awarded the Unilever Research Prize 2013 for the University of Leiden. The prize was bestowed upon her because of her thesis about her 9-months Master’s internship that she performed in the department from September 2011 until July 2012, in combination with her other study re…
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Natalia Ortiz awarded for the KNMP Student Prize
Natalia Ortiz, a current PhD student in our department, was awarded the KNMP Student Prize during the last autumn Congress 2014 of the Royal Dutch Pharmacists Association (Koninklijke Nederlandse Maatschappij ter bevordering der Pharmacie, KNMP), held in Utrecht at the beginning of October.
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Dr. Dong Guo won the Dutch Medicinal Chemistry prize 2013-2014
On March 27th, 2015 the biannual Dutch Medicinal Chemistry Prize for the best Dutch Ph.D. thesis in the field was awarded to Dr. Dong Guo, a current postdoc researcher in our lab, by the Section of Medicinal Chemistry of the Royal Netherlands Chemical Society.
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Newly discovered gene regulates balance of ‘bad cholesterol’
In a publication in Science, Noam Zelcer from the Division of Biopharmaceutics describes a previously unrecognized pathway to regulate LDL-cholesterol levels. He is also able to modulate this pathway. This opens the possibility for complementing and improving the efficacy of statins: A class of drugs…
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Pain relief without the high
Researchers at Leiden University led by Mario van der Stelt (Leiden Institute for Chemistry) have set ‘gold standards’ for developing new painkillers based on the medicinal effects of cannabis. Publication in Nature Communications.
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Kinetics for drug discovery – The first step towards an improved drug discovery paradigm
Supervisor: Indira Nederpelt
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Synthetic Methodology Towards ADP-Ribosylation Related Molecular Tools
Phosphorylation affects all four major biomolecules – proteins, lipids, carbohydrates and nucleic acids – and plays a pivotal role in the most fundamental cellular functions.
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Activity-based protein profiling for drug discovery
Activity-based protein profiling (ABPP, also termed chemical proteomics), is one of the pillars of chemical biology, and at LED3 we have taken it to the next level. ABPP allows the assessment of protein function in live cells and tissues, which means that the activity of a complete protein family can…
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The endocannabinoid system in zebrafish larvae
In this thesis, we have studied the potential of the zebrafish larval model in studying the ECS, as a complementary model to the existing rodent models.
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The molecular secrets of medicinal cannabis
Chronic pain, nausea or vomiting due to chemotherapy. If you suffer from such ailments, medicinal cannabis can be a godsend. Though a downside is that it can make patients high. Therefore, Leiden researchers from the Oncode Institute are investigating alternatives that do not make you high. In Nature…
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Cryo Electron Tomography Studies On Bacterial Chemosensory Arrays
Bacterial chemosensory arrays are protein assemblies that are the key structural and functional component for motile bacteria to sense their internal or environmental chemical signals.
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The synthesis of mannose-derived bioconjugates and enzyme inhibitors
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-Promotor: J.D.C. Codee
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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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Towards predictive cardiovascular safety: a systems pharmacology approach
Promotores: Prof.dr. M. Danhof, Prof.dr. D.R. Stanski
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Chemokine signaling mechanisms underlying inflammation and infection control: insights from the zebrafish model
This thesis focuses on the role of chemokine receptors CXCR3 and CCR2 in the inflammatory process and infection control using the zebrafish model.
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Rob van Wijk has won the oral presentations of the National PhD Competition during the FIGON Dutch Medicine Days
He presented his PhD research entitled “Kick-starting drug development; translational systems pharmacology using innovative zebrafish experiments and advanced computational modelling”. During his presentation, Rob highlighted the advancements he made in using zebrafish as model in system pharmacolog…
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Synthesis of well-defined ADP-Ribosylated biomolecules
Promotor: G. A. van der Marel, Co-promotor: D. V. Filippov
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Stem cells as cure
Leiden has a long history in the treatment of blood cell cancer. Research to find better therapies never stands still. One of the potential treatments currently being worked on is a ‘living medicine’.
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Microbial Chemotaxis
In order to gain insight into the structure and function of the molecular complexes involved in chemotaxis, we use electron cryotomography (ECT). This technique allows us to directly study microbes in their native state at resolutions capable of visualizing individual proteins.
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Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
PhD defence
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Evolution of Molecular Resistance to Snake Venom α-Neurotoxins in Vertebrates
We have examined sequences from the ligand-binding domain of the nicotinic acetyl choline receptor (nAChR) in 148 vertebrate species. We are in interested in this receptor because the α-neurotoxins of many venomous snakes binds to this receptor in its location at the neuromuscular junction in all ve…
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LACDR excels at the FIGON Dutch Medicine Days
The Leiden Academic Centre for Drug Research (LACDR) received no less than three awards during the Figon Dutch Medicine Days. Bas Goulooze won the PhD Prize for best PhD candidate, Natalia Ortiz Zacarías and Huub Sijben both received a poster prize. ‘Scientists must be able to communicate their research…