123 zoekresultaten voor “receptor” in de Publieke website
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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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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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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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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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Drug-target residence time: a case for the adenosine A1 and A2A receptors
Promotor: A.P.IJzerman, Co-Promotor: L.H. Heitman
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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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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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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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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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mutations and identification of a selectivity hotspot in adenosine receptor
G protein-coupled receptors (GPCRs), one of the largest families of membrane proteins, are responsive to a diverse set of physiological endogenous ligands including hormones and neurotransmitters.
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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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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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Functie receptor voor goed HDL cholesterol in mens ontmaskerd
HDL staat bekend als het ‘goede cholesterol’: het verlaagt de kans op hart- en vaatziekten. Sommige families hebben van nature veel HDL in het bloed. Onderzoek naar hun erfelijk materiaal kan bijdragen aan de ontwikkeling van nieuwe medicijnen die HDL verhogen.
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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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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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A chemical biology approach for targeting of ligand-drug conjugates
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-Promotor: R.G. Boot
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The ins and outs of ligand binding to CCR2
Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: L.H. Heitman
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Key innate immune components controlling intracellular infection
Promotor: H.P. Spaink, Co-Promotor: A.H. Meijer
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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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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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Clavis Aurea? Structure-enabled approaches of identifying and optimizing GPCR ligands
Promotores: A.P. IJzerman, H.W.T. van Vlijmen
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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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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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Biophysical characterization of membrane protein-small molecule interactions
Promotor: Prof.dr. M. Ubbink
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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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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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De moleculaire geheimen van medicinale cannabis
Chronische pijn, misselijkheid of braken door chemotherapie. Als je er last van hebt, kan medicinale cannabis een uitkomst zijn. Het nadeel is alleen wel dat patiënten er high van kunnen worden. Leidse onderzoekers van het Oncode Instituut doen daarom onderzoek naar alternatieven waar je dat niet van…
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Corpora Non Agunt Nisi Fixata: Ligand Receptor Binding Kinetics in G Protein-Coupled Receptors
Promotie
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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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Sensing Transport
Solute carrier (SLC) transporters are a large and diverse class of relatively understudied transmembrane proteins.
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Synthetic carbohydrate ligands for immune receptors
Promotie
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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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Leidse onderzoekers brengen eiwit in beeld met hoogste resolutie ooit
Nog nooit was een kristalstructuur van een menselijk eiwitmolecuul in een celwand zo kristalhelder. De Leidse onderzoekers Ad IJzerman en Laura Heitman maakten samen met Amerikaanse collega’s de meest gedetailleerde kristalstructuur ooit van een doeleiwit voor geneesmiddelen. De onderzoekers publiceerden…
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Carcinogenicity of insulin analogues
Promotor: Prof.dr. B. van de Water
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Nieuw ontdekt gen reguleert balans ‘slecht cholesterol’
In een publicatie in Science beschrijft Noam Zelcer van het LACDR een tot nu toe onbekend mechanisme om de hoeveelheid LDL-cholesterol te reguleren. Hij kan dit mechanisme ook beïnvloeden. Dit biedt kansen op aanvulling en verbetering van de werking van zogenoemde statines: medicijnen om ‘slecht cholesterol’…
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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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Discovery of Reversible Monoacylglycerol Lipase Inhibitors
Monoacylglycerol lipase (MAGL) is the principal enzyme responsible for hydrolysis of the endocannabinoid 2-arachidonoylglycerol (2-AG). MAGL inhibition provides several potential therapeutic opportunities, including anti-nociceptive, anti-inflammatory and anti-cancer activity.
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Chemical tools to study the cannabinoid receptor type 2
Promotie
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LACDR in de prijzen bij FIGON Dutch Medicine Days
Tijdens de Dutch Medicine Days viel het Leiden Academic Centre for Drug Research (LACDR) maar liefst drie keer in de prijzen. Bas Goulouze won de PhD Prize voor beste promovendus, Natalia Ortiz Zacarías en Huub Sijben mochten beiden een posterprijs in ontvangst nemen. 'Wetenschappers moeten in staat…
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Discovery of FLT3 inhibitors for the treatment of acute myeloid leukemia
The disease acute myeloid leukemia (AML) is characterized by fast progression and low survival rates.
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Biotic ligand models
Description of Biotic ligand models: making an inventory of available models & assessment of the variability of the predicted HC5 using the BLMs in different Dutch water types (2005 - 2007)
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Pijnstilling zonder high te zijn
Onderzoekers van de Universiteit Leiden onder leiding van Mario van der Stelt (Leids Instituut voor de Chemie) wijzen ‘gouden standaarden’ aan om nieuwe pijnstillers te ontwikkelen die gebaseerd zijn op de medicinale werking van cannabis. Publicatie in Nature Communications.
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Using insertional mutagenesis to identify breast cancer drivers and therapy resistance genes in mice
In this thesis, we used genetically engineered mouse models to identify genes and pathways that are involved in ILC formation and in the development of resistance to FGFR-targeted therapy.
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Selective autophagy in host defense against mycobacterial infection
The effective treatment of tuberculosis (TB) remains a major challenge to global health.