Medicinal Chemistry in Belgium: Innovation and Success Stories
Annual One-Day Meeting on Medicinal Chemistry of SRC & KVCV
Liege, Belgium November 27, 2020
Modulating Protein-Protein Interactions by Means of Rigidified Peptidomimetics
Prof. Steven BALLET
VRIJE UNIVERSITEIT BRUSSEL, Brussels, Belgium Read more
Prof. Steven BALLET
Dr Steven Ballet completed his PhD at the Vrije Universiteit Brussel (VUB, Brussels, Belgium) in 2007. Directly following his PhD training, Dr Ballet went for a first postdoctoral stay in Australia at the University of Adelaide with Professor Andrew Abell. During this stay he applied ring closing and cross metathesis reactions on amino acid and peptide substrates. As such, dimeric but also ring closed peptide scaffolds could be obtained. More specifically, RCM was used to stabilize ('staple') the helical conformation of alpha and beta peptides. As a second postdoctoral training, Dr Ballet went to the Institut de Recherches Cliniques de Montréal (IRCM, Montreal, Canada) for a specialized training in the opioid peptide field. Together with Prof. Peter W. Schiller, he designed bifunctional opioid ligands with dual MOR/DOR agonist profiles and hybrid opioid/non-opioid multitarget ligands. Since 2010 Dr Ballet is appointed as a faculty member at his alma mater, where he pursues his efforts in the peptide and peptidomimetic field. The main research topics involve injectable peptide hydrogels for sustained release of bioactive peptides, the synthesis of turn/helix/loop mimetics as receptor ligands or PPI modulators, and transition metal-catalyzed derivatization of peptides in aqueous media.
Dr Gilles BERGER
ULB, Brussels, Belgium
Dr Dan BROOKINGS
UCB, Slough, United Kingdom
Development of Positive Allosteric Modulators for Glutamate Ionotropic Receptors
Pierre Francotte is a pharmacist (University of Liège) and completed a Mastère in Drug Design at the Ecole Supérieure de Chimie de Lille & University of Lille 2. He worked on the development of AMPA potentiators in collaboration with the industry and obtained his PhD in Biomedical and Pharmaceutical Sciences (University of Liège).
He achieved his postdoc at the University of Copenhagen in Prof. Bente Frølund’s team where he was involved in the development of pharmacological tools targeting the GABAA receptors. After this research stay, he came back in Liège where he is now Assistant Professor in the Lab. of Medicinal Chemistry (Prof. B. Pirotte).
His research interests include the design/synthesis of AMPA/KA modulators but also the optimization of natural products using total synthesis approach.
Prof. Raphaël FREDERICK
UCLOUVAIN, Brussels-Woluwe, Belgium
Purines and Trypanosomatids – a Neglected Match for New Therapeutics?
Dr Hulpia is a pharmacist by training, and obtained his PhD in Pharmaceutical Sciences in 2018. Currently, he is a postdoctoral fellow at Ghent University in the laboratory for Medicinal Chemistry. One of his research interests include infectious disease drug discovery, more particularly neglected tropical diseases.
Discovery of GLPG2451, a novel Potentiator for the Treatment of Cystic Fibrosis
After obtaining my masters degree in chemistry in 2007, I started a PhD in organic chemistry at the KULeuven in the group of prof. Wim Dehaen. My research focussed mainly on supramolecular chemistry (helicenes) which allowed me to build up a solid basis in terms of heterocyclic chemistry. During this period I was also able to broaden my knowledge in the field by working for 4 months in China in the group of prof. Xi Zhang (Tsinghua University, Beijing). Soon after obtaining my PhD I started working at Galapagos NV as a Scientist on the Cystic Fibrosis program in 2013, and currently I’m working there as Team Leader in the chemistry department.
Step by Step Towards Fully Modified Aptamers’
Prof. Eveline LESCRINIER
REGA INSTITUTE - KU LEUVEN, Leuven, Belgium Read more
Prof. Eveline LESCRINIER
Eveline Lescrinier (°1972) is a pharmacist (KULeuven, 1995). In 1999, she obtained her PhD in Pharmaceutical Sciences supported by the Flemish Fund for Scientific Research (FWO) with a thesis entitled ‘Structure determination of a HNA-RNA duplex by NMR spectroscopy’.
In 2005, she became responsible for the ‘Impulse Financing’ of the Flemish government to start up an interfaculty center for biomolecular research using NMR spectroscopy at KU Leuven (BioMacs) which launched in 2006. Since then, several students have started a PhD under her supervision. In 2016, she became the head of the laboratory for Medicinal Chemistry of KU Leuven, a multidisciplinary laboratory including bio-organic chemistry, molecular modeling, mass spectrometry, NMR spectroscopy and synthetic biology.
Her general research interest is on structure determination of (modified) oligonucleotides and their interaction with nucleic acid processing enzymes. Obtained results of this fundamental research are applied in the development of folded xenobiotic nucleic acids that bind a specific target (XNA aptamers).
ConfoBody Technology Suite: Unleashing the Full Therapeutic Potential of GPCR Targets
Christel joined Confo Therapeutics as CSO in 2016. She previously was Director of Medicinal Chemistry at Galapagos from 2014 to 2016. Christel was one of the first chemists at Galapagos in 2005. She is the inventor of filgotinib and under her leadership it was moved forward to pre-clinical development (today filgotinib has successfully completed Phase III for rheumatoid arthritis and is explored in several other indications). She also played a key role in a number of other projects and advanced several compounds into preclinical phase.
Christel started her professional career as a Medicinal Chemist at Evotec in 2002. She then joined Faust Pharmaceuticals in 2004, today called Domain Therapeutics, a biotech company specializing in GPCR drug discovery. She is an inventor on more than 25 patent applications.
Christel completed a PhD in Organic Chemistry at the University of Manchester (UK) in Prof Jonathan Clayden’s lab.
Scaffold Development for the Inhibition of FXIIa, a Promising Therapeutic Target.
Lionel Pochet is an associate professor at the University of Namur. He obtained his Ph.D. degree in Pharmaceutical Sciences at the University of Namur and was Post-Doctoral Fellow at the Laboratory of Biomolecular Analysis at the VU University of Amsterdam.
His research interests include medicinal chemistry in the field of serine proteases inhibitors for antithrombotic therapy and the development of analytical methodologies for biological screening.