1,892 zoekresultaten voor “optimize drug design” in de Publieke website
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Design of selective inhibitors for human immunoproteasomes
The thesis describes the development, synthesis and biological evaluation of several proteasome inhibitor designs. Mainly, this work focusses on designing proteasome inhibitors that selectively inhibit the immunoproteasome, while leaving the constitutive proteasome mostly, if not completely, untouch…
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Research and design in STEM education
Onderzoeken en ontwerpen zijn twee vaardigheden die steeds belangrijker worden in de vakken O&O (onderzoeken en ontwerpen) en NLT (natuur, leven en technologie). Uit onderzoek van Tessa Vossen (ICLON en Faculteit Wiskunde en Natuurwetenschappen) blijkt dat docenten en leerlingen de relevantie van onderzoeken…
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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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Waarom zijn drugs verslavend?
Een pilletje op een festival, een biertje in de kroeg, of een sigaret bij de koffie. We wéten dat het slecht voor ons is, maar doen het toch. Hoe komt dat?
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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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Algorithm design for mixed-integer black-box optimization problems with uncertainty
The increasing competition in the automotive industry requires the tailored, swift development of technologically sophisticated vehicles. Therefore, the computationally expensive state-of-the-art simulation technologies are combined with optimization algorithms. An example of a real-world optimization…
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Systems pharmacokinetic models to the prediction of local CNS drug concentrations in human
Clinical development of drugs for central nervous system (CNS) disorders has been particularly challenging and still suffers from high attrition rates.
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Quality-driven multi-objective optimization of software architecture design: method, tool, and application
Promotores: Prof.dr. T.H.W. Bäck, Prof.dr. M.R.V. Chaudron, Co-Promotor: M.T.M. Emmerich
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localization of lipid-based nanomedicines for the exploration of targeted drug delivery
Microscopic insight on lipid-based nanomedicine in vivo remains limited to the perception of the knowledge that could be obtained: if we interpret only what we see, then we only believe to know. Although believing to know encapsulates an undefined amount of uncertainty in the exploration of lipid-based…
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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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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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Real-World Expensive Black-Box Optimization with Applications in Vehicle Design
Optimally solving real-world expensive Black-Box Optimization (BBO) problems w.r.t. real-world constraints, such as wall-clock time and computational costs, is extremely difficult and tedious.
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How to scale clearance from adults to children for drugs undergoing hepatic metabolism?
The aim of this thesis is to expedite and ensure the systematic accuracy of clearance scaling from adults to paediatric patients, with a special focus on drugs undergoing hepatic metabolism.
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namic Relationships of Central Nervous Systems Active Dopaminergic Drugs
Discovery and development of Central Nervous System (CNS) drugs is hampered by high attrition rates.
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System-level design for efficient execution of CNNs at the edge
A convolutional neural network (CNN) is a biologically inspired algorithm, highly capable at processing images and videos.
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Design, synthesis, and evaluation of antigenic peptide conjugates containing Toll-like receptor agonists
This thesis describes the design, synthesis, and immunological evaluation of varying (neo)antigenic peptide conjugates containing either a TLR2 or a TLR7 agonist.
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Transforming data into knowledge for intelligent decision-making in early drug discovery
Promotor: A.P.IJzerman Co-promotor: A. Bender
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Designing 'context-specific' regional innovation policy: a study on the role of regional government in six European regions
Whilst government’s ability to design ‘context-specific’ regional innovation policy is generally assumed to depend on the region’s decision-making power, the aim of this study is to investigate how regional government matters. In order to open up the black box of policy design, the study develops a…
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Systems microscopy to unravel cellular stress response signalling in drug induced liver injury
Promotor: B. van de Water
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Design, implementation and evaluation of transnational collaborative programmes in astronomy education and public outreach
Promotores: Prof.dr. G. Miley & Prof.dr. J.M. van den Broek
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Design, synthesis and application of paramagnetic probes for protein structure studies
The main subject of this thesis is the design and synthesis of paramagnetic molecules for protein studies with NMR and EPR spectroscopy.
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The impact of obesity on the pharmacokinetics of drugs in adolescents and adults
Promotores: C.A.J. Knibbe; J.N. van den Anker, Co-promotores: H.P.A. van Dongen; B. van Ramshorst
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Pharmacogenomics in Drug Development: Implementation and Application of PKPD Model Based Approaches
Model based approaches, integrating physiological parameters or linking exposure with response, are powerful tools to quantify and evaluate the impact of genetic differences that are reflected as variability of drug exposure and/or clinical response(s). This thesis “Pharmacogenomics in Drug Development: …
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Personalised pharmacotherapy in paediatric epilepsy : the path to rational drug and dose selection
The path to rational drug and dose selection
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Andrea Herrera JaramilloFaculteit der Wiskunde en Natuurwetenschappen
j.a.herrera.jaramillo@cml.leidenuniv.nl | 071 5272727
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vaccines for immune modulation: from antigen selection to nanoparticle design
Nanoparticles can be used as delivery systems for both small molecules and macromolecules such as proteins, peptides or oligonucleotides. This thesis focuses on the use of liposomes, nanometric vesicles formed by a lipid bilayer enclosing an aqueous core. Liposomes are highly versatile delivery syst…
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Design and synthesis of metal-based chemotherapeutic agents for targeted DNA interactions or DNA repair pathway modulation
The research presented in this thesis explores the chemotherapeutic potential of metal-based compounds as chemotherapy agents, with an initial focus on the synthesis and DNA interaction studies of platinum and palladium compounds utilizing the [Pt(bapbpy)]2+ scaffold. The study identifies intercalation…
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using fluorescent cell models for mechanistic evaluation of adverse drug reactions
Promotie
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Individualization of Drug Clearance Predictions and Dose Regimens in Patients with Obesity Using Pharmacometric Approaches
Promotie
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Designing a sustainable future for the European Healthcare Sector
The project seeks to develop an eco-design framework for single-use medical devices and packaging
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Electoral Systems and Turnout: Evidence From a Regression Discontinuity Design
Electoral Systems and Turnout: Evidence From a Regression Discontinuity Design. In dit artikel, gepubliceerd op de website SAGE research methods, bespreken auteurs Jaroslaw Kantorowicz en Tobias M. Hlobil hoe een Regression Discontinuity Design uitgevoerd kan worden.
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Designing Data protection law: hebben we een beter idee?
Wat is een goede wetgeving inzake gegevensbescherming? Hoe kan een dergelijke wetgeving goed worden ontwikkeld? Is de Europese wetgeving hierover adequaat, en is deze toepasbaar in China?
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system-based pharmacology approach to predict developmental changes in renal drug clearance in children
Promotores: Prof.dr. C.A.J. Knibbe, Prof.dr. M. Danhof, Prof.dr. K. Allegaert (Leuven)
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Gene networks-based mechanistic assessment of drug-induced organ toxicity: a focus on liver and kidney
Drug induced organ toxicity is the main problem of the drug development and drug usage in the clinic. The liver and kidneys are the most sensitive organs towards drug induced toxicity.
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Optimisation of first clinical studies in special populations: towards semi-physiological pharmacokinetic models
M. Danhof, Co-promotores: J. Freijer, A. Yassen
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Multifunctional polypept(o)ide miktoarm star polymers for advanced drug delivery: from the development of versatile synthetic strategies for
With an emphasis on developing novel miktoarm star polymers termed PeptoMiktoStars, this thesis leverages asymmetric polymeric polypept(o)ide frameworks to advance their effectiveness in delivering hydrophobic drugs and nucleic acids.
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Psychedelische drugs hebben mogelijk effect op creativiteit
Promovenda Luisa Prochazkova deed samen met haar collega's van cognitieve psychologie onderzoek naar de effecten van microdoseringen psychedelische drugs op creativiteit. Hun eerste voorzichtige conclusie: je wordt inderdaad creatiever van een klein beetje LSD.
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Semi-partitioned Scheduling and Task Migration in Dataflow Networks
Promotor: Ed F. Deprettere, Co-promotor: Todor P. Stefanov
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Image-based phenotypic screening for breast cancer metastasis drug target discovery
The main aim of this thesis was to unravel the signaling and regulatory networks that drive tumor cell migration during breast cancer metastasis.
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Design and evaluation of video portfolios: reliability, generalizability, and validity of an authentic performance assessment for teachers
In welke mate zijn beoordelingen op basis van een videodossier betrouwbaar, generaliseerbaar en valide?
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Transdisciplinary Perspectives on Validity: Bridging the Gap Between Design and Implementation for Technology-Enhanced Learning Systems
Technologies that help to enhance our educational environments can be found everywhere.
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and flow of data: connecting large datasets with machine learning in a drug discovery envirionment
This thesis focuses on data found in the field of computational drug discovery. New insight can be obtained by applying machine learning in various ways and in a variety of domains. Two studies delved into the application of proteochemometrics (PCM), a machine learning technique that can be used to…
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Development of a Kidney-on-a-Chip Model for Compound Screening and Transport Studies
Pharmaceutical companies, governments and the general public have become increasingly aware that animal models used in drug testing lack vital aspects to serve as an accurate representation of human biology. As models of the human body should become more physiologically relevant, animal models no longer…
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NMR structural studies of protein-small molecule interactions
Promotor: Prof.dr. M. Ubbink, Co-promotor: G. Siegal
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Nusa ZidaricFaculteit der Wiskunde en Natuurwetenschappen
n.zidaric@liacs.leidenuniv.nl | 071 5274799
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Joran LammersFaculteit der Wiskunde en Natuurwetenschappen
j.a.lammers@cml.leidenuniv.nl | 071 5272727
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The LeiCNS-PK3.0 model development and applications: healthy-to-diseased CNS pharmacokinetic translation
Accurate prediction of the unbound drug concentration-time profile at the CNS target site is crucial for the assessment of the right drug concentration-effect relationship. PBPK models have supported the PK prediction of the CNS target sites and the translation of PK data between species and between…
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Lost in Chemical Space, Found in Data
Developing new medicines is one of modern science's most significant hurdles, a process marked by high costs, long timelines, and frequent failures of promising candidates.
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Antibiotic Conjugates and Natural Products as Next-Generation Strategies Against Antimicrobial Resistance
This thesis tackles the urgent challenge of antimicrobial resistance (AMR) through the design of novel antibacterial agents.
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Eindpresentatie Design of Justice
Op 19 mei 2021 heeft de eindpresentatie plaatsgevonden van de cursus Design of Justice: the juvenile court of the future.