Fragment-Based Drug Development: Finding Starting Points for Today’s Drug Targets
Dr. Stijn Gremmen
The development of new drugs is both challenging and highly exciting. Despite the positive impact of the available small-molecule therapies on the lives of patients, drug development still seems a relatively inefficient process, characterized by long timelines, high cost and an immense failure rate.
Studies of the complex underlying mechanisms of disease and resistance to existing therapies constantly reveal new drug targets. The current focus of the pharmaceutical industry is on drug targets and mechanisms that were previously considered to be “undruggable”. In this light, one of the challenges is the search for molecular starting points in today’s drug target space.
ZoBio is one of the early adaptors of fragment-based drug discovery, in which we identify low molecular weight compounds (fragments) as starting points. In the lecture we will discuss the impact of fragment screening and show highlights of our multidisciplinary platform, including protein production, a range of biophysical techniques and chemistry.
Stijn is currently working at ZoBio as Head of Chemistry and is responsible for all medicinal chemistry related matters in projects. His chemistry journey started in the early 90’s at the HLO in Beverwijk. Since then he studied mass spectrometry and bioorganic chemistry, both at the University of Amsterdam, where received his PhD in 2002. After a postdoctoral period at the Radboud University Nijmegen, he joined Mercachem to do chemical research in a commercial setting. During his 13 years at the company, he worked on many multidisciplinary projects for pharmaceutical and agrochemical companies. In this period, he experienced the central role chemists can play in the process of drug discovery. In his current position at ZoBio, he is working in a team of chemists, biologists and physicists and translates results from those very different disciplines into novel molecules for clients in the pharmaceutical industry.