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Structure-based design, synthesis and biological evaluation of novel ligands targeting galectin-8

Sjors van Klaveren

Sjors van Klaveren completed a bachelor’s degree in Organic Chemistry with a thesis in the group of Dr Robin Bon at the University of Leeds in 2014. This thesis focussed on the synthesis of activated click-groups for bioorthogonal immobilisation of proteins on self-assembled monolayers.

His master’s degree was obtained from the Vrije Universiteit Amsterdam in 2017. The thesis work was performed in the group of Prof. Rob Leurs and focussed on synthesising inhibitors for parasitic phosphodiesterases aiming to treat the neglected disease Trypanosomiasis.

This PhD4Glycodrug project is carried out at the University of Ljubljana and Lund University under the supervision of  both Assoc. Prof. Tihomir Tomašič and Prof. Ulf J. Nilsson. Combining computational design and organic synthesis, Sjors aims to produce glycomimetic ligands with high selectivity for individual galectins in order to address immune disorders and cancer development.

Publications

  1. Mujtaba Hassan, Sjors van Klaveren, Maria Håkansson, Carl Diehl, Rebeka Kovačič, Floriane Baussière, Anders P. Sundin, Jaka Dernovšek, Björn Walse, Fredrik Zetterberg, Hakon Leffler, Marko Anderluh, Tihomir Tomašič, Žiga Jakopin, Ulf J. Nilsson. Benzimidazole–galactosides bind selectively to the Galectin-8 N-Terminal domain: Structure-based design and optimisation, European Journal of Medicinal Chemistry 2021223, 113664. doi: 10.1016/j.ejmech.2021.113664.
  2. Sjors Van Klaveren, Anders Sundin, Žiga Jakopin, Marko Anderluh, Hakon Leffler, Ulf Nilsson, Tihomir Tomašič. Selective galectin-8N ligands: the design and synthesis of phthalazinone-D-galactals. ChemMedChem2021, doi:  10.1002/cmdc.202100575.
  3. Benedetta Girardi, Martina Manna, Sjors Van Klaveren,  Tihomir Tomašič, Žiga Jakopin, Hakon Leffler, Ulf Nilsson, Daniel Ricklin, Janez Mravljak, Oliver Schwardt, Marko Anderluh. Selective monovalent galectin-8 ligands based on 3-lactoylgalactoside. ChemMedChem 2021, doi: 10.1002/cmdc.202100514.