University of Groningen
Discovery of Inhibitors by Combinatorial-Chemistry Approaches
van der Vlag, Ramon
DOI:
10.33612/diss.146091529
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Publication date: 2020
Link to publication in University of Groningen/UMCG research database
Citation for published version (APA):
van der Vlag, R. (2020). Discovery of Inhibitors by Combinatorial-Chemistry Approaches. University of Groningen. https://doi.org/10.33612/diss.146091529
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Discovery of Inhibitors by
Combinatorial-Chemistry Approaches
Ramon van der Vlag
The work described in this thesis was carried out at the Stratingh Institute for Chemistry, University of Groningen, The Netherlands.
The work was financially supported by the Netherlands Organization for Scientific Research (NWO, VIDI grant 723.014.008).
Cover Design by R. van der Vlag: protein structures 1GCZ, 1LOX and 1YCR from the RCSB Protein Data Bank were visualized using SeeSAR 10.1 (BioSolveIT GmbH).
Discovery of Inhibitors by
Combinatorial‐Chemistry Approaches
Proefschrift
ter verkrijging van de graad van doctor aan de Rijksuniversiteit Groningen
op gezag van de
rector magnificus prof. dr. C. Wijmenga en volgens besluit van het College voor Promoties.
De openbare verdediging zal plaatsvinden op
vrijdag 27 november 2020 om 14:30 uur
door
Ramon van der Vlag
geboren op 8 december 1991 te Stadskanaal
Promotores Prof. dr. A. K. H. Hirsch Prof. dr. F. J. Dekker Beoordelingscommissie Prof. dr. M. R. Groves Prof. dr. G. J. Poelarends Prof. dr. R. W. Hartmann
Table of contents
Chapter 1
Analytical Methods in Protein-Templated Dynamic Combinatorial Chemistry
1
Chapter 2
A Combinatorial Approach for the Discovery of Drug-Like Inhibitors of 15-Lipoxygenase-1
41
Chapter 3
Replacement of an Indole Scaffold Targeting Human 15 Lipoxygenase-1 Using Combinatorial Chemistry
67
Chapter 4
Optimized Inhibitors of MDM2 via an Attempted Protein-Templated Reductive Amination
85
Chapter 5
Inhibition and Labeling of Macrophage Migration Inhibitory Factor (MIF) 111
Chapter 6
Summary and Future Perspectives 145
Chapter 7
Samenvatting en Toekomstperspectief 151
Chapter 8
Acknowledgments 157
