Prof. Bernhard Kuster
Chair of the Department of Biosciences and Co-Director of the Bavarian Biomolecular Mass Spectrometry Center at Technische Universitat Munchen
Chemical proteomics reveals the target landscape of clinical kinase inhibitors
Kinase inhibitors have developed into important cancer drugs because de-regulated protein kinases are often driving the disease . Efforts in biotech and pharma have resulted in more than 30 such molecules being approved for use in humans and several hundred are undergoing clinical trials. As most kinase inhibitors target the ATP binding pocket, selectivity among the 500 human kinase is a recurring question. Polypharmacology can be beneficial as well as detrimental in clinical practice, hence, knowing the full target profile of a drug is important but rarely available. We have used a chemical proteomics approach termed kinobeads to profile 240 clinical kinase inhibitors in a dose dependent fashion against a total of 320 protein kinases and some 2,000 other kinobead binding proteins. In this presentation, I will outline how this information can be used to identify molecular targets of toxicity, re-purposing existing drugs or combinations for new indications or provide starting points for new drug discovery campaigns
Bio-sketch
Bernhard Kuster is a chemist by training and obtained is PhD in Biochemistry from the University of Oxford. He went on to do a PostDoc funded by an EMBO long-term fellowship at the EMBL in Heidelberg and the University of Southern Denmark in Odense. After seven years at the biotech firm Cellzome in Heidelberg as Vice President for Analytical Sciences and Informatics, he became Full Professor of Proteomics at the Technical University of Munich in 2007 where he is also the Chair of the Department for Biosciences and Co-Director of the Bavarian Biomolecular Mass Spectrometry Center. Bernhard’s research focuses on mass spectrometry based proteomics, big data informatics and their application to drug discovery as well as chemical and systems biology.
Professor Kuster is recognized as a pioneer in the field of chemical proteomics and his group has generated an extensive draft of the human proteome in 2014. These contributions have been recognized by the Heinz Maier-Leibnitz award of the TUM (2014) and the HUPO Discovery in Proteomic Sciences Award (2015). Bernhard is also an associate editor of the journal Molecular and Cellular Proteomics and a co-founder of the biotech firm OmicScouts.
Date
Date(s) - September 12, 2016
7:00 pm - 10:00 pm
Emplacement / Location
Morris and Rosalind Goodman Agora