1,177 zoekresultaten voor “small molecule inhibitors” in de Publieke website
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Small-molecule inhibitors of bacterial metallo-β-lactamases
The main focus of the thesis is the discovery and development of novel inhibitors of bacterial metallo-β-lactamases (MBLs).
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Small molecule inhibitors of Nicotinamide N-Methyltransferase (NNMT)
NNMT wordt beschouwd als een nieuw potentieel farmacologisch doelwit in de behandeling van een verscheidenheid van kankers, stofwisselingsziekten en andere pathologieën. Het toenemend aantal publicaties waarin de rol van NNMT bij ziekten wordt opgehelderd, heeft op zijn beurt de ontwikkeling van krachtige…
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PhD candidate || Identification and characterization of small molecule inhibitors of type VII protein secretion systems (1.0 fte)
Wiskunde en Natuurwetenschappen, Leids Instituut voor Chemisch Onderzoek (LIC)
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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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Inhibitor Selectivity: Profiling and Prediction
Less than 1 in 10 drug candidates that enter phase 1 clinical trials actually gets approved for human use.
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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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NMR structural studies of protein-small molecule interactions
Promotor: Prof.dr. M. Ubbink, Co-promotor: G. Siegal
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High-throughput profiling of small molecules using mass spectrometry
Promotor: Prof.dr. T. Hankemeier
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Inhibitor discovery of phospholipases and N-acyltransferases
In this thesis an activity-based probe was discovered that could visualize the activity of PLAATs. With an optimized gel-based ABPP assay in hand, screening of a compound library led to the discovery of alpha-ketoamides as a hit for PLAAT3.
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Small-molecule inhibitors of bacterial metallo-β-lactamases
Promotie
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Biophysical characterization of membrane protein-small molecule interactions
Promotor: Prof.dr. M. Ubbink
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Discovery of BUB1 kinase inhibitors for the treatment of cancer
The spindle-assembly checkpoint (SAC) is a safety mechanism which secures accurate chromosome segregation during mitosis.
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Targeting Human Proteasomes: Substrates, Inhibitors and Prodrugs
Large parts of the research described in this Thesis aims at the development of oligopeptide-masked toxins and their in situ immunoproteasome-mediated activation.
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NMR studies of protein-small molecule and protein-peptide interactions
Promotor: M. Ubbink, Co-promotor: G. Siegal
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and its derivatives: synthesis and application as beta-glycosidase inhibitors
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
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Small Molecule Inhibitors of Nicotinamide N-Methyltransferase (NNMT)
Promotie
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Inhibitors and probes targeting endo-glycosidases
The chemical synthesis of inhibitors and probes targeting endo-glycosidases.
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Development of kinase inhibitors and activity-based probes
Promotor: H.S. Overkleeft, J. Neefjes, Co-promotor: M. van der Stelt
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PhD candidate in bio-synthetic chemistry of small-molecule drugs targeting viral RNAs
Wiskunde en Natuurwetenschappen, Leids Instituut voor Chemisch Onderzoek (LIC)
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Cancer chess: molecular insights into PARP inhibitor resistance
The clinical potential of applying synthetic lethality to cancer treatment is famously demonstrated by the BRCA1/PARP1 paradigm: a tumor specific defect in BRCA1 – a component of the DNA double-strand break (DSB) repair pathway homologous recombination (HR) – results in a remarkable sensitivity to PARP1…
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Exploring chemical space in covalent and competitive glycosidase inhibitor design
Glycoside hydrolases (glycosidases/GHs) are widely abundant enzymes in all kingdoms of life and are important biocatalysts that catalyze the hydrolysis of glycosidic linkages in oligo/polysaccharides, glycoproteins and glycolipids with tremendous efficiency
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Iminosugars as glucosylceramide processing enzymes inhibitors: design, synthesis and evaluation
This Thesis describes the design, synthesis and evaluation as glycoprocessing enzyme inhibitors of focused libraries of iminosugars.
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and characterization of inhibitors of carbohydrate modifying enzymes to generate a new type of anti-bacterial molecule (1.0 fte)
Wiskunde en Natuurwetenschappen, Leids Instituut voor Chemisch Onderzoek (LIC)
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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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Single-molecule microscopy in zebrafish embryos
Single-Molecule Microscopy (SMM) techniques constitute a group of powerful imaging tools that enable researchers to study the dynamic behavior of individual molecules.
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identify and characterize inhibitors of carbohydrate modifying enzymes to generate a new type of anti-viral molecule
Wiskunde en Natuurwetenschappen, Leids Instituut voor Chemisch Onderzoek (LIC)
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Nieuwe moleculen ontwerpen
Zelfs een kleine quantumcomputer zou in staat moeten zijn om de eigenschappen en het gedrag van nieuwe moleculen exact te simuleren. Dit zou de chemie naar een nieuw niveau tillen. Betere zonnepanelen, krachtiger batterijen, grote energiebesparingen in de chemische industrie: de toepassingen hebben…
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How Electrostatic Interactions Drive Nucleosome Binding of RNF168 & PSIP1
The studies presented in the work show the potential of the integrative use of biophysical data in defining the structural basis of protein interactions.
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Discovery and development of inhibitors selective for human constitutive proteasome and immunoproteasome active sites
This thesis describes the design and development of subunit‐selective inhibitors of particular catalytically active subunits of human constitutive proteasomes and immunoproteasomes.
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Discovery of novel inhibitors to investigate diacylglycerol lipases and α/β hydrolase domain 16A
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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Design and development of conformational inhibitors and activity-based probes for retaining glycosidases
Glycosidases are essential in fundamental biological processes and are responsible for the degradation of most (oligo)saccharides, glycolipids and glycoproteins.
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Organische moleculen in de ruimte
Dishoeck
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Sequencing biological molecules with graphene
Schneider
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Deciphering the complex paramagnetic NMR spectra of small laccase
Multicopper oxidase, laccase, can efficiently reduce oxygen to water and are mostly used in the enzymatic biofuel cells.
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Unraveling the mechanism of multicopper oxidases: from ensemble to single molecule
Promotores: Prof.dr. G.W. Canters, Prof.dr. T.J. Aartsma
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Plasmonic enhancement of one-photon- and two-photon-excited single-molecule fluorescence by single gold nanorods
This thesis is a collection of experimental attempts to enhance photoluminescence of fluorescent molecules and quantum dots with single gold nanorods (GNRs) and relevant applications.
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Electronic spectroscopy of molecules of astrophysical interest
This thesis revolves around the electronic spectroscopy of molecules in the laboratory and the search for the carriers of the diffuse interstellar bands (DIBs).
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Molecules during stellar formation and death
Promotor: Prof.dr. E. F. van Dishoeck
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Let Them Roar: Small States as Cyber Norm Entrepreneurs
Sinds de United Nations Group of Governmental Experts on the Developments in the Field of Information and Telecommunications in the Context of International Security (UN GGE) elf aanbevelingen heeft gedaan over verantwoordelijk staatsgedrag omtrent cyberspace is er een discussie gaande over internationale…
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Small changes for long term impact: optimization of structure kinetic properties: a case of CCR2 antagonists
Promotor: Prof.dr. A. P. IJzerman, Co-Promotor: L.H. Heitman
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Small scale kinematics of massive star-forming cores
Promotor: Prof.dr. E.F. van Dishoeck, Co-Promotor: M.R. Hogerheijde
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solution and crystallographic studies of the Sso10a2 and human C1 inhibitor protein
Promotor: Prof.dr. J.P. Abrahams, Co-Promotor: N.S. Pannu
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Ab initio molecular dynamics calculations on reactions of molecules with metal surfaces
Promotor: Prof.dr. G.J. Kroes
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The formation of complex organic molecules in dense clouds-Sweet results from laboratory
Large areas of space are filled by molecular clouds that consist of gas and dust grains that are the remnants of dead stars. When these clouds start collapsing, the decreasing temperature and increasing density cause gas particles to start accreting onto dust grain surfaces.
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Charge transport properties of Ru-complex molecules: the influence of humidity
I will give a general introduction to the field of molecular electronics, its history, methods and challenges. I will also introduce the subject of my investigation and provide a brief outlook to the remainder of our thesis.
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Beyond the Born-Oppenheimer Static Surface Model for Molecule- Surface Reactions
Several techniques are explored for going beyond the born-oppenheimer static surface model for molecule-surface reactions.
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Stable single molecules for quantum optics and all-optical switches
Promotor: Prof.dr. M.A.G.J. Orrit
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Two-photon multifocal microscopy for in vivo single-molecule and single-particle imaging
In this thesis we investigated the ability of two-photon multifocal microscopy for single-molecule microscopy in live cells and organisms.
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Management of small-scale -African fisheries: The Case of Elephant Marsh in Malawi
How does the management of Elephant Marsh Fishery in Malawi relate to wider contexts of policies, theories and regions? And how can the current management system be adapted to achieve long-term sustainability of the fishery?
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Nucleosome stacking in chromatin fibers probed with single-molecule force- and torque-spectroscopy
In human cells, a meter-long DNA is condensed inside a micrometer-sized cell nucleus. Simultaneously, the genetic code must remain accessible for its replication and transcription to functional proteins.