Session 3: Chemical Biology Meets Biophysics for Drug Discovery
Dr Sandra JACOB
NOVARTIS, Basel, Switzerland
Illuminating the Path to New E3-Ligases for Targeted Protein Degradation (IL05)
Ms Hannah LITHGOW
UNIVERSITY OF STRATHCLYDE & GSK, Glasgow, United Kingdom
Hannah Lithgow is a final year industrial PhD student at GlaxoSmithKline in collaboration with the University of Strathclyde. Her PhD has focussed on developing novel PROTACs for targeted protein degradation. She has drawn on both high throughput chemical techniques and phenotypic screening to enable new E3 ligase discovery. Throughout her PhD she has won her multiple awards, including the prestigious Salter’s Centenary Prize and she has also been recognised for being an exceptional woman in a STEM career. She will continue her career at GSK after her PhD as a senior scientist in medicinal chemistry, in the high throughput chemistry department enabling rapid drug discovery.
The Development and Biophysical Characterisation of Click-Tagged, Reversible Probes to Measure Target Occupancy of ERK1/2 Kinase Inhibitors (OC07)
Dr Chiara Rosa VALENZANO
ASTEX PHARMACEUTICALS, Cambridge, United Kingdom
Chiara is a senior research associate at Astex Pharmaceuticals in Cambridge. Chiara completed her studies in synthetic organic chemistry in Italy, to then move to the USA to pursue a PhD at Brown University, centred on studying the biosynthesis of polyketide antibiotics. In 2011, she was awarded a Marie Curie International Incoming fellowship to work at the University of Cambridge with professor Chris Abell on fragment-based drug discovery methods to identify inhibitors of protein-protein interactions. The focus of her research, in academia at first then in industry, has been the development of small molecules to interfere and repair altered biological processes linked to diseases.
Biophysical and Structural Principles of PROTAC Mechanism of Action (IL06)
Prof. Alessio CIULLI
UNIVERSITY OF DUNDEE, Dundee, United Kingdom
Alessio Ciulli holds the Personal Chair of Chemical and Structural Biology at the School of Life Sciences, University of Dundee. His research interests are in chemical biology, structural biology and drug discovery of protein-protein interactions (PPIs) within the chromatin and ubiquitin-proteasome systems. Of particular interest are the development and application of small molecules approaches for inducing protein degradation, and chemical genetics and fragment based drug design approaches to target protein surfaces and PPIs.
Alessio graduated in Chemistry (2002) from his hometown Florence under the late Ivano Bertini and obtained his PhD from the University of Cambridge (Chemistry, 2006), studying as a Gates Cambridge Scholar under the supervision of Chris Abell and in collaboration with Astex Pharmaceuticals. Following post-doctoral research on fragment-based drug design with Chris Abell and Tom Blundell, and an HFSP visiting Fellowship at Yale University to begin collaboration with Craig Crews (2009), he was awarded a BBSRC David Phillips Fellowship and returned to Cambridge to start his independent career in 2010. In 2013 Alessio was awarded an ERC Starting Grant and moved his laboratory to the School of Life Sciences at Dundee to take up a Readership and Principal Investigator role within the Division of Biological Chemistry and Drug Discovery. He was promoted to Professor in October 2016. He is a Fellow of the Royal Society of Chemistry. Alessio is the recipient of several prizes and awards, including:
- 2014 Talented Young Italian award
- 2015 EFMC Prize for Young Medicinal Chemist in Academia
- 2015 ICBS Young Chemical Biologist Award
- 2016 RSC Capps Green Zomaya Award in medicinal computational chemistry
- 2016 MedChemComm Emerging Investigator Lectureship.
Coffee Break & Exhibition
The PROTAC Design Toolbox: Biophysically Enabling the Optimisation of a Potent SMARCA Degrader (OC08)
Dr David ZOLLMAN
UNIVERSITY OF DUNDEE, Dundee, United Kingdom
Dr David Zollman is a research scientist at the University of Dundee, whose work focusses on the employment of a range of structural (X-ray crystallography, SAXS, non-denaturing mass spectrometry) and biophysical (SPR, FP, AlphaScreen, ITC) techniques to probe complex biological systems.< br />
David completed his Master’s degree in Medicinal Chemistry at the University of St Andrews before moving to the University of Oxford to conduct his doctorate with Professor Christopher Schofield. Following a post-doctoral placement with Dr Akane Kawamura (also at Oxford) David moved to the University of Dundee to join the group of Professor Alessio Ciulli as a member of an academic-industrial collaboration with Boehringer Ingelheim. David leads the structural biology and biophysics for the Dundee team, aiding the development of novel PROTACs for a range of medically relevant targets.
Exhibitor Short Presentation: Creoptix
Pushing Boundaries in Kinetics Analysis
Rational Design of Kinase Inhibitors Using Structure and Biophysical Data (IL07)
Prof. Stefan KNAPP
GOETHE UNIVERSITY FRANKFURT, Frankfurt am Main, Germany
Prof Stefan Knapp studied Chemistry at the University of Marburg and the University of Illinois. He did his PhD in protein crystallography at the Karolinska Institute in Stockholm and continued his career at the Karolinska Institute as a postdoctoral scientist (1996-1999). From 1999 to 2004 he worked at Pharmacia Corporation and from 2004-2015 at the Structural Genomics Consortium (SGC) at Oxford University. From 2008 to 2015 he was a Professor of Structural Biology at Oxford University (UK) and between 2012 and 2015 he was the Director for Chemical Biology at the Target Discovery Institute. He joined Frankfurt University in 2015 as a Professor of Pharmaceutical Chemistry. Since 2017 he is the CSO of the SGC at the University of Frankfurt.
Lunch, Exhibition & Networking
Session 4: MS-Based Methods
Dr Stefan GESCHWINDNER
ASTRAZENECA, Mölndal, Sweden
Stefan Geschwindner, Associate Director, Head of Biophysics
AstraZeneca R&D Gothenburg; Discovery Sciences; Structure, Biophysics and FBLG
Dr. Stefan Geschwindner has during his Ph.D. at the University of Frankfurt worked with label-free technologies, predominantly with NMR to elucidate protein structures. After his Ph.D. he immediately joined the Astra Structural Chemistry Laboratory as a Senior Research Scientist in 1998 with focus on protein production and characterization, thereby applying a variety of different biophysical methods. Before moving into his current role as Head of Biophysics in 2018, he had different roles as Team leader in Protein Engineering, Delivery leader for Neuroscience as well as Principal Scientist in Biophysics. During the last decade, Stefan has frequently applied affinity-based methods to facilitate the mechanistic understanding of protein-ligand interactions and to enable fragment-based lead generation approaches. He has an excellent track record for developing, implementing and utilizing new affinity-based techniques to aid early lead finding activities and to understand the molecular mode of action of drugs. In the last 5 years he authored over 30 peer-reviewed papers resulting in an h-index of 17 and > 700 citations.
Advances in Structural Mass Spectrometry for Drug Discovery and Therapeutic Protein Characterization (IL08)
Dr Sarah CIANFERANI
UNIVERSITY OF STRASBOURG, Strasbourg, France
Dr. Sarah Cianférani is a research Director at the National Center for Scientific Research (CNRS) in France. She is currently heading the BioOrganic Mass Spectrometry Laboratory at the Institut Pluridisciplinaire Hubert Curien (IPHC) in Strasbourg, a team of 40 people that has strong expertise in proteomic analyses and structural mass spectrometry.
Her expertise focuses on developments in structural mass spectrometry and applications of advanced native mass spectrometry and native ion-mobility mass spectrometry methodologies for biological noncovalent complex characterization, and especially biopharmaceuticals.
Dr. Sarah Cianférani holds a PhD degree in analytical chemistry from the University of Strasbourg, France. She then performed and post-doctoral fellowship at the Institute for Genetics and Molecular Biology (IGBMC) in Strasbourg to gain competences in structural biology. She then joined the AliX company (ancestor of Novalix) to develop native Mass Spectrometry for protein/ligand screening. She was recruited by the CNRS as researcher in 2004 in the team of Alain Van Dorsselaer (BioOrganic Mass Spectrometry Lab, LSMBO) in Strasbourg.
She is now research director at the CNRS and heads the BioOrganic Mass Spectrometry Laboratory (LSMBO). Her group is part of the French National Proteomic Infrastructure. She is co-author of more than 110 scientific papers related to mass spectrometry analysis of proteins.
Identifying an Escape Route from Adverse Effects of the Liver X Receptor Ligands Using HDX-MS (OC09)
Dr Anna BELORUSOVA
ASTRAZENECA, Molndal, Sweden
Dr Anna Belorusova has developed an extensive expertise in structure and biophysics of nuclear hormone receptors and their complexes during her PhD studies at the Institute for Genetics and Molecular Biology (IGBMC) in Strasbourg, France. In 2015 she obtained her PhD degree in Structural Biology and Biophysics from the University of Strasbourg, as well as two prizes for the best doctoral thesis. In 2016 she joined AstraZeneca (Gothenburg, Sweden) as a postdoc, and there she continues investigating nuclear receptors using biophysical tools, in particular HDX-MS. She integrates HDX-MS, structural and functional data using multivariate statistical approaches to understand how ligand-induced conformational changes correlate with beneficial and adverse effects of nuclear hormone receptor modulators observed in animal models, and how knowledge of protein conformation and dynamics could contribute to developing better drugs.
Sugars in the Gas Phase? Novel Techniques to Unravel the Glycocode (IL09)
Prof. Kevin PAGEL
FREIE UNIVERSITÄT BERLIN, Berlin, Germany
Prof. Dr. Kevin Pagel is currently Associate Professor for Bioorganic Chemistry at the Institute of Chemistry and Biochemistry of the Freie Universität Berlin and guest researcher at the Fritz Haber Institute of the Max Planck Society. He earned a diploma in organic chemistry from the University of Leipzig in 2003 and a PhD from the Freie Universität Berlin in 2007. From 2008-2010 he pursued postdoctoral research with Prof. Dame Carol V. Robinson at the University of Cambridge and later at the University of Oxford. In early 2011 Kevin returned to Germany and started building his independent career, first as a research associate at the Fritz-Haber-Institute (2011-2013) and then as an Assistant (2014-2016) and Associate Professor (2017) at the Freie Universität Berlin. Research in the Pagel group is focused on the structural analysis of biological macromolecules in the gas phase using ion mobility-mass spectrometry and gas-phase IR spectroscopy techniques.
Exhibitor Short Presentation: Bruker Daltonics
High-Throughput SPR Screening in Drug Discovery
Use of Mass Spectrometry in Small Molecule Lead Discovery (IL10)
Dr Jörg HOERNSCHEMEYER
F. HOFFMANN-LA ROCHE, Basel, Switzerland
Joerg holds a diploma in chemistry from the University of Bonn (Germany) and obtained his PhD in biochemistry in 2001. From 2001 to 2003 he worked as Post-Doc at the University of Bonn and at the Center of Advanced European Studies and Research (caesar).
In 2003 he joined F. Hoffmann-La Roche in Basel, heading the mass spectrometry group of Pharma Technical Dev Biotech Analytics. From 2010-2012 he worked as principal scientist in Formulation Research and since 2013 he is leading the mass spec group for peptides, proteins and oligonucleotides in preclinical CMC.
Since 2007 Joerg is delegate of the Swiss regulatory agency Swissmedic at the European Directorate for the Quality of Medicines & HealthCare (EDQM, Group of Experts 6, Biologics) in Strasbourg. He is assistant lecturer at the University of Applied Sciences, Northwestern Switzerland and co-chairing the Mass spectrometry group of the Swiss pharma association AEA.
Coffee Break & Exhibition
Session 5: Characterisation of Small Molecules Binding to RNA
Dr Ursula EGNER
BAYER, Berlin, Germany
Hit Discovery for Riboswitch Ligands (IL11)
Prof. Ruth BRENK
UNIVERSITY OF BERGEN, Bergen, Norway
Professor Ruth Brenk, Department of Biomedicine, University of Bergen, Norway. The overall research goal of the Brenk lab is to improve methods used for structure-based drug design and to apply these methods to design ligands for proteins and RNas with biological relevance. A key point in our research is the interplay of theoretical and experimental methods.
Education and former professional experience
1999-2003: PhD in structure-based drug design, Philipps University Marburg, Germany, 2003, supervisor Prof. G. Klebe
1994-1998: Pharmacy degree, Johannes-Gutenberg University Mainz, Germany
Detection of Ligand-Induced Conformational Changes in Oligonucleotides by Second-Harmonic Generation (OC10)
Dr Margaret BUTKO
BIODESY, South San Francisco, United States
Margaret is a senior scientist at Biodesy in South San Francisco, CA where she has focused on detecting and characterizing ligand-induced conformational changes on a wide range of therapeutic targets using Biodesy's Delta. Margaret joined Biodesy four years ago before the launch of the Delta instrument to measure protein conformational changes, and she later initiated work to expand the technology for studying RNA conformational changes. Prior to that, Margaret completed her postdoctoral training at Genentech in the Protein Analytical Chemistry department characterizing critical quality attributes for antibody-based drug products. Margaret received a PhD in Biomedical Sciences from the University of California, San Diego where she studied under Dr. Roger Tsien, and she received a Bachelor's degree in Chemistry from the College of Wooster.
Structural Basis for Gene-Specific RNA Splicing Correction Induced by a Small Molecule (IL12)
Prof. Frédéric ALLAIN
ETH ZURICH, Zurich, Switzerland
Prof. Frédéric Allain obtained his doctorate with Dr.G.Varani at the MRC-LMB of Cambridge (1993-1997). Between 1997 and 2000, he was a Postdoctoral Fellow at UCLA with Prof. J.Feigon, followed by one year as Research associate with Prof.D.Black (HHMI).
In 2001, Frédéric Allain joined the department of Biology of the ETH in Zürich initially as an assistant Professor and since 2010, he is a full Professor. Prof. Allain’s research interest is primarily to determine structures of protein-RNA complexes in order to understand mechanisms of post-transcriptional gene regulation like alternative-splicing, RNA editing and translation regulation.
Prof. Allain was elected EMBO member in 2009.
Prof. Allain is the co-director of the SNF-NCCR RNA and Disease since 2014.
Exhibitor Short Presentation: 2bind
Work with the Experts in Biophysics – A Quick Dive into 2bind’s Tailor-made Services for Drug Discovery
Ribosomal Translation and Human Diseases (IL13)
Prof. Eric WESTHOF
INSTITUT DE BIOLOGIE MOLÉCULAIRE ET CELLULAIRE, Strasbourg, France
Eric Westhof is Emeritus Professor of Structural Biochemistry at the University of Strasbourg, France. He was Director of the Institute of Molecular and Cellular Biology of the CNRS in Strasbourg (2005-2016) and Vice-President for Research and Doctoral Studies of the University of Strasbourg (2007-2012). He is now Delegate for teaching and formation at the French Academy of Sciences. His research activities are centered on the relationships between sequences, three-dimensional structures, evolution and functions of RNA molecules. The tools used are X-ray crystallography, bioinformatics, sequence comparisons, three-dimensional modelling and molecular dynamics simulations. The aims are the understanding of RNA evolution and the continued interplay between sequence changes and RNA structure/activity. He is a member of EMBO (1998), Deutsche Akademie der Naturforscher LEOPOLDINA (2000), Academia Europaea (2001) and of the French Académie des Sciences (2011).