83 zoekresultaten voor “kinase inhibitor” in de Publieke website
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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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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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Development of kinase inhibitors and activity based probes
Promotie
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Chemical genetic approaches for target validation
Drug development is a time- and resource-consuming process that starts with the discovery and validation of a (protein) target that contributes to pathogenesis or disease progression.
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Targeted Therapy for Triple-Negative Breast Cancer
The research described in this thesis focused on identifying novel drug targets and synergistic combinations for triple-negative breast cancer (TNBC), a virulent subtype of breast cancer with a dismal prognosis and limited therapeutic options.
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Arabidopsis AGC3 kinases and PIN plasma membrane abundance
The plant hormone auxin plays a central role in the growth and development of plants. Auxin acts in a concentration dependent manner and polar cell-to-cell transport of this hormone determines its distribution in the tissues of plants. This polar auxin transport is mediated by several families of auxin…
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The role of AGC3 kinases and calmodulins in plant growth responses to abiotic signals
Promotor: Prof.dr. P. Hooykaas, Co-promotor: R. Offringa
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Novel factors modulating AGC kinase signaling-controlled polar auxin transport
The PID-directed shift in PIN polarity has been broadly accepted as one of the essential mechanisms for the regulation of auxin transport polarity.
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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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Unieke medicijnstructuren vinden met kunstmatige intelligentie en scheikunde
In de zoektocht naar nieuwe medicijnen tegen onder andere kanker heeft een Leids team een nieuwe werkwijze ontwikkeld. Dit stappenplan combineert kunstmatige intelligentie (AI) met moleculair modelleren en is geschikt om onbekende en vernieuwende medicijnstructuren te vinden, zo bewezen de onderzoek…
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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 FLT3 inhibitors for the treatment of acute myeloid leukemia
Promotie
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Functions of P38 and ERK kinases in zebrafish early development
Promotor: Prof.dr. H.P. Spaink, Co-promotor: Dr. B.E. Snaar
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Uncovering vulnerabilities in triple-negative breast cancer
Triple-negative breast cancer (TNBC) constitutes a small subtype (~15%) of breast cancer, but causes the majority of breast cancer-related deaths.
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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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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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Regulation of the arabidopsis AGC kinase PINOID by PDK1 and the microtubule cytoskeleton
Plants, are sessile organisms, have developed strategies to adapt to changes in their environment, in part by altering their growth and development.
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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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Mario van der SteltWiskunde en Natuurwetenschappen
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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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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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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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Modulating the behaviour of pancreatic tumour cells
Promotores: Prof.dr. M.K. Richardson, Prof.dr. H.P. Spaink. Co-promotor: C.P. Bagowski
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Osteosarcoma: searching for new treatment options
Promotores: B. van de Water; P. Hogendoorn; J. Bovée Co-Promotor: E.H.J. Danen
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Jeroen CodeeWiskunde en Natuurwetenschappen
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Hermen OverkleeftWiskunde en Natuurwetenschappen
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This Week's Discoveries | 12 november 2019
Lezing
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Cyclophellitol analogues for profiling of exo- and endo-glycosidases
To this day, all cyclophellitol-based inhibitors and ABPs have been close analogues of their natural substrate counterparts. As a result, these probes showed high selectivity towards their target glycosidases.
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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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Chemical tools to monitor and control proteasome activities
Promotores: H.S. Overkleeft; G.A. van der Marel Co-Promotor: B.I. Florea
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Direct and two-step activity-based profiling of proteases and glycosidases
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
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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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Fluorescence Polarization Activity-Based Protein Profiling on Retaining Glycosidases
Glycosidases are important enzymes in the turnover of polysaccharides and glycoconjugates, and are involved in a range of human pathologies including genetic disorders such as Gaucher and Pompe disease, but also in various cancers.
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Nieuwe techniek geeft chemici ongekende controle in medicijnonderzoek
Leidse chemici hebben een nieuwe techniek ontwikkeld waarmee ze de rol van kinases – een groep eiwitten – kunnen achterhalen in een levende cel. De techniek maakt het eenvoudiger om nieuwe medicijndoelwitten te vinden voor ziektes als kanker en reuma. Het team publiceerde de bevindingen in het vakblad…
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Precision modeling of breast cancer in the CRISPR era
The molecular mechanisms that instigate a healthy cell to become malignant are fueled by (epi)genetic alterations in so-called driver genes.
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Inhibitor Selectivity: Profiling and Prediction
Promotie
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Targeting Human Proteasomes: Substrates, Inhibitors and Prodrugs
Promotie
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Novel factors modulating AGC kinase signaling-controlled polar auxin transport
Promotie
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Arabidopsis AGC3 kinases and PIN plasma membrane abundance
Promotie
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Samenwerken voor efficiënte medicijnontwikkeling
De keten die patiënten voorziet van nieuwe medicijnen, bestaat uit diverse complexe schakels: van fundamentele wetenschap, tot klinische tests, tot productie. Deze hele keten is aanwezig in Leiden. De universiteit, het Leids Universitair Medisch Centrum (LUMC) en de bedrijven op het Leiden Bio Science…
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The synthesis of mannose-derived bioconjugates and enzyme inhibitors
Promotie
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Iminosugars as glucosylceramide processing enzyme inhibitors: design, synthesis and application
Promotie
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Regulation of the arabidopsis AGC kinase PINOID by PDK1 and the microtubule cytoskeleton
Promotie
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In the Spotlight - Biology Seminars Leiden
Lezing
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Design and development of conformational inhibitors and activity-based probes for retaining glycosidases
Promotie
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Discovery and development of inhibitors selective for human constitutive proteasome and immunoproteasome active sites
Promotie
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Discovery of novel inhibitors to investigate diacylglycerol lipases and α/β hydrolase domain 16A
Promotie
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Activity-based protein profiling in drug discovery
In the last decades, activity-based protein profiling (ABPP) has emerged as a powerful chemical tool that may aid the ever-challenging drug discovery process.
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Activity-based protein profiling of diacylglycerol lipases
Promotor: H.S. Overkleeft, Co-promotor: M. van der Stelt
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Dynamics of a β-lactamase
BlaC is the β-lactamase of Mycobacterium tuberculosis. We show that it can recover from inhibition by clavulanic acid and that phosphate helps it do so.