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MSSI Research Forum June 7

MSSI Research Forum June 7

Dr Ulrich Hassiepen, Centre for Proteomic Chemistry, Novartis Institutes for BioMedical Research (NIBR), Switzerland

PRESENTATION TITLE  Facing the Challenges of Drug Discovery


Drug discovery has historically developed from a serendipity driven approach to a comprehensive, target rationale driven, multidisciplinary, industrialized process, contested in a highly competitive environment. Hence, pharmaceutical companies are striving to optimize their processes in research towards increased productivity. One response to this challenge has been the formation of expertise groups focusing their efforts on just one target class, e.g., on enzymes such as kinases or proteases. This so-called platform approach facilitates the integration of several target-based drug discovery steps and therefore enables their efficient streamlining. The compilation of literature-known enzyme inhibitors allows for target validation and potentially the identification of first starting points (hits) for Medicinal Chemistry efforts. During the hit-to-lead and lead optimization phases, drug discovery is mainly characterized by iterative cycles of compound synthesis, testing of such compounds in in vitro assays, analysis of binding to the target by X-ray, and feedback of results to be used for starting the next cycle of compound synthesis and characterization with the aim to improve their desirable properties. The combination of state-of-the-art assay technologies with a high degree of lab automation, enables the selectivity profiling of enzyme inhibitors on the target and against a large panel of counter-targets, i.e., generating results required for compound optimization towards on target potency and selectivity against counter targets.  The platform approach results in decreased turnaround times for such cycles by closely linking the three core competencies of In Vitro Biology, Medicinal Chemistry and Structural Science. This talk will provide insights into various aspects of modern drug discovery in pre-clinical research, ranging from target identification/validation, through to hit finding/validation and assay technologies employed for lead optimization.


Dr Hassiepen studied chemistry at the University of Technology (RWTH) Aachen, Germany, where he received his PhD in 1997. In 1998 he joined the Lead Finding Unit in the Core Technology Area of Novartis Pharma AG in Basel, Switzerland. Here he was working on novel assay technologies for high-throughput screening, the main focus being on miniaturized formats for biochemical assays, fluorescence correlation spectroscopy and liquid-handling in the nanoliter range. In 2002 he joined the Biology Unit of the Expertise Platform Proteases at Novartis where he contributed to novel therapeutic approaches for the treatment of, e.g., primary hypertension (renin inhibitors), type 2 diabetes (DPP IV inhibitors), skin diseases (kallikrein 7 inhibitors) and HVC infections (HCV NS3 protease inhibitors) mainly by supporting interdisciplinary teams with his expertise in assay technologies, compound screening and enzymology. Part of his efforts was the successful introduction of novel assay formats for de-ubiqutinating enzyme (DUBs) and developing a workable solution for the use of fluorescence lifetime-based assays for routine compound profiling. For more than three years he was heading a drug discovery program on a target in the field of cardio-vascular diseases. In mid 2015 he joined the Hit Finding Group at the Centre for Proteomic Chemistry where he is responsible for running an open access lab space, supporting a variety of drug discovery programs by developing and adapting assays for high- and medium-throughput screening as well as for desk-top applications, and performing Mode-of-Action studies on compound-target interactions.

DATE:           Tuesday, 7 June 2016

TIME:            10h00

VENUE:        MSG-025 MSSI Building Extension


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