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Biophysical Methods in Drug Discovery: How MST Fits in UCB’s Toolbox ?
| Dr Nicolas BASSE (UCB CELLTECH, Slough, United Kingdom) Read more
Dr Basse spent 10 years developing his expertise in Biophysics and Protein Chemistry working on several drug discovery projects.
Since 2012, he has been part of the Structural Biology Department at UCB Celltech. His responsibilities include leading a small molecule program and looking after some of the biophysics instrumentation.
He studied biochemistry, biophysics and structural biology at the University of Paris (Denis Diderot France) where he received his PhD working on the proteasome. He then joined Alan Fersht's group in Cambridge (UK) to work on p53 and then joined the LMB (MRC, Cambridge) to work on ribosome biology. Close window
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MicroScale Thermophoresis: Interaction Analysis and Beyond
| Dr Dennis BREITSPRECHER (NANOTEMPER TECHNOLOGIES GMBH, Muenchen, Germany) Read more
Dr. Breitsprecher studied Biochemistry in Hannover, Germany, and has a strong background in fluorescence-based biophysical and microscopic methods. After graduating at the Institute of Biophysical Chemistry at Hannover Medical School in the lab of Jan Faix in 2010, he joined the lab of Prof. Bruce Goode at Brandeis University (Waltham, MA) as a DFG research fellow. His work was focused on elucidating the role of the cytoskeleton in cell-migration, using a combination of single-molecule imaging and a wide spectrum of biophysical techniques. He then joined NanoTemper Technologies in 2013 as principle investigator of the Research and Development unit, where he further improves and optimizes applicability, performance and sensitivity of MicroScale Thermophoresis . Close window
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Using MicroScale Thermophoresis to Evaluate UHTS Hits
| Mr Edward DINUNZIO (MERCK, New Jersey, United States) Read more
Edward DiNunzio received his B.A. in Molecular Biology and Biochemistry from Rutgers University (New Brunswick, New Jersey). Since joining Merck Research Laboratories in 2008, he has utilized a number of biophysical techniques, including Surface Plasmon Resonance (SPR), Differential Scanning Calorimetry (DSC), Affinity Selection Mass Spectrometry (AS/MS) and Temperature Dependent Fluorescence (TdF) to elucidate compound mechanisms of action in support of lead identification and discovery efforts across a range of disease areas. Close window
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Towards Novel Antivirals for Human Hepatitis B Virus Infections
| Dr Neil FERGUSON (UNIVERSITY COLLEGE DUBLIN, Dublin, Ireland) Read more
Career History
2008-present: Tenured Senior Lecturer (Structural Biology), University College Dublin
2003-2008: Tenured team-leader, MRC Centre for Protein Engineering, Cambridge, UK
2002-2003: Senior Investigator, MRC Centre for Protein Engineering, Cambridge, UK
2001-2003: MRC Career Development Fellowship, MRC Centre for Protein Engineering
2000-2001: Post-doctoral research associate, MRC Centre for Protein Engineering,
Cambridge, UK (mentor: Prof. Sir Alan R. Fersht)
1994-1995: Zeneca Pharmaceuticals (Infection Unit), Cheshire, UK
Research Interests
- Biomolecular self-assembly mechanisms:
• protein folding
• protein misfolding
• virus replication and assembly
- Thermodynamics of protein folding, stability and allostery
- Biomolecular interactions and disease
- Protein structure-function relationships
- Therapeutic targeting of challenging or ‘HTS unfriendly’ targets
- Fragment-based lead discovery
- Methods and assay development Close window
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Structural Basis of SUFU-GLI Interaction in Human Hedgehog Signaling Regulation
| Dr Katharina GEGENSCHATZ-SCHMID (KAROLINSKA INSTITUTET, Huddinge, Sweden) |
The Heat of the Moment: Using MST to Access Binding Thermodynamics
| Dr Geoff HOLDGATE (ASTRAZENECA, Macclesfield, United Kingdom) Read more
Geoff undertook a degree in biological and biochemical sciences at the University of Salford starting in 1988. As part of his undergraduate studies Geoff undertook a year in industry and joined the Protein Function team of ICI Pharmaceuticals in 1990. This work involved mechanistic studies on the epidermal growth factor receptor tyrosine kinase, leading to the discovery of a potent inhibitor related to Iressa (trademark of AstraZeneca). Following graduation in 1992, he rejoined ICI as a permanent member of the Protein Function Team. ICI Pharmaceuticals subsequently became Zeneca Pharmaceuticals, which merged with Astra to form AstraZeneca. During the last 20 years Geoff has applied the techniques associated with mechanistic enzymology and biophysics to the study of structure-function relationships on numerous drug targets and associated ligands, including several successful drug discovery projects, such as Iressa, Crestor and Caprelsa (trademarks of AstraZeneca). He currently holds the position of Principal Scientist and Associate Director in Biophysics within the Discovery Sciences Department at AstraZeneca, Alderley Park. He leads a team of 8 scientists whose work involves the identification and characterisation of hit and lead compounds. His work interests include a range of biophysical techniques (including ITC, DSC, SPR), as well as mechanistic enzymology approaches to characterise the mechanism, kinetics and thermodynamics of protein-ligand interactions for exploitation in drug design. Close window
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Biophysical Analysis on Membrane Protein Targeting and Assembly
| Dr Alexej KEDROV (GENE CENTER MUNICH, Munich, Germany) Read more
Dr Kedrov obtained Dr. rer. nat. degree in Biology/Biophysics from the Technical University of Dresden with a focus on single-molecule biomechanics and later worked as a postdoctoral and a senior researcher to establish fluorescence analysis of membrane transport in the University of Groningen (Netherlands). Since recently, he has been continuing his research projects in LMU Munich working in the Structural Biology group of Prof. Roland Beckmann. His research has covered mechanisms of protein stabilization and folding, interactions with substrates/inhibitors, as well as assembly of protein:protein and protein:lipid complexes assayed by biophysical and biochemical methods. He extensively employed quantitative biomolecular analysis based on fluorescence spectroscopy (incl. FRET, FCS, FCCS), light scattering and atomic force microscopy (DLS, AFM), as well as thermodynamics techniques - isothermal and scanning microcalorimetry (ITC, DSC) and surface plasmon resonance (SPR) - combined with conventional analytical approaches. He established a range of MST-based assays to study protein and RNA interactions in solution and at lipid membranes, and currently uses the method for studying ribosome:ligand complexes. Close window
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Chemical Tractability Assessments with Encoded Library Technology; Probing 82 Bacterial Targets with a 2 Trillion Member DNA Encoded Library
| Dr Carl MACHUTTA (GLAXOSMITHKLINE, Collegeville, United States) Read more
Dr. Carl Machutta obtained his PhD in Chemistry with a focus in Protein Biochemistry and Enzymology from Stony Brook University in NY. He studied transient 1D NOE NMR for fragment design as a post-doctoral fellow and he studied protein crystallography as a visiting post-doctoral scientist at the University of Wϋrzburg in Germany. He joined the Molecular Discovery Research (MDR) group at GlaxoSmithKline (GSK) in 2009 where he uses High Throughput Screening (HTS), Encoded Library Technology (ELT) and biophysical approaches to support leads discovery for therapeutic programs in Oncology and Infectious Diseases. Dr. Machutta has used multiple biophysical, mechanistic and computational techniques for enzyme characterization and inhibitor discovery in his career and he will highlight the role MST has played in leads discovery at GSK. Close window
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Eighty Targets in Four Years - Integrating MST in an Industrial Setting
| Dr Ismail MOAREFI (CRELUX GMBH, Martinsried, Germany) Read more
Collaborating with Nanotemper since 2009. Founder and CSO of Crelux, a globally active drug discovery service provider for the pharma and biotech industry (Since 2005). Founder and CSO of SiREEN (2002-2005). Responsible for bringing two structure-based drug discovery projects from idea to animal proof-of-concept. Group leader at Max-Planck institute for biochemistry (1998-2002). Postdoctoral work at Rockefeller University 1995-1998. PhD from institute for biochemistry at Ludwig-Maximilians University Munich. Co-authored more than 30 publications in high profile journals with currently over 3500 citations. Close window
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MicroScaleThermophoresis in Modern Drug Discovery Process
| Dr Alexey RAK (SANOFI AVENTIS, Vitry-sur-Seine, France) Read more
Dr. Rak has a M. Sc in Biology and Genetics from Kharkiv state university (Ukraine) and a M.Sc in Biochemistry from Moscow state university (Russia). He obtained his Ph.D. in Biochemistry and Biophysics at the Institute of Protein Research at the Russian Academy of Sciences (Pushchino, Moscow region, Russia) and at the Karolinska Institute and the Royal Institute of Technology in Stockholm (Sweden). For his postdoctoral research he joined the Department of Physical Biochemistry at the Max Planck Institute of Molecular Physiology (Dortmund, Germany) in 1999. In 2003 he became Group Leader of the Structural biochemistry lab at the same institute. In 2007 he was recruited by Sanofi-aventis in Paris as head of protein crystallization, since 2009 he is head of the protein crystallization and the biophysics group. In 2013 he became head of BioStructure and Biophysics at SDI/LGCR Sanofi R&D in France. Close window
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Fast and Quantitative Analysis of Aptamer-target Interactions Using MicroScale Thermophoresis
| Dr Thomas SCHUBERT (2BIND, Regensburg, Germany) |
Application of MicroScale Thermophoresis in Hit Identification and Validation
| Dr Markus ZEEB (BOEHRINGER-INGELHEIM PHARMA, Biberach an der Riß, Germany) Read more
Dr Zeeb is a biochemist with a strong background in biophysics and NMR. He obtained his diploma and Ph.D. in biochemistry at the University of Bayreuth (Germany) in the research group of Prof. Franz X. Schmid and PD Dr. Jochen Balbach (2000, 2004) working on NMR structure determination of proteins and protein nucleic acid complexes as well as studying protein folding with NMR and biophysical methods. For his postdoctoral research he moved to The Scripps Research Institute in La Jolla, CA (USA) where he was working as a Skaggs Institute and DFG Research fellow in the group of Prof. Peter E. Wright on the structural determinants and mechanism of type 1 muscular dystrophy using NMR spectroscopy (2004-2007). Dr. Zeeb was recruited by Boehringer Ingelheim Pharma GmbH & Co. KG in Biberach a. d. Riss (Germany) in June 2007. As Principal Scientist in the Department of Lead Identification and Optimization Support he is responsible for primary fragment screening applying a variety of biophysical methods and project support using NMR spectroscopy. Close window
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Protein Interaction Analyses: a Basis to Understand Essential Biological Reactions, Infection and Disease Mechanisms
| Prof. Dr Peter F. ZIPFEL (FRIEDRICH SCHILLER UNIVERSITY, Jena, Germany) Read more
1975 – 1980: Studies Biology and Biochemistry at the University of Bremen
1980 – 1984: PhD at the Institute for Physical Biology, University of Bremen
1985 – 1988: Postdoctoral Fellow at the Laboratory of Immunoregulation, the National Institutes of Health (NIH), Bethesda, Maryland, USA (supported by the DAAD)
1989: Research Scientist at the Laboratory of Immunoregulation, the National Institutes of Health (NIH), Bethesda, Maryland, USA
1989 – 2000: Group leader the Bernhard Nocht Institute for Tropical Medicine, Hamburg
1993: Docentship at the University of Hamburg, Topics Immunology and Molecular Biology
1999: Professor, University of Hamburg
Since 2000: University Professor for Infection Biology, Friedrich Schiller University, Jena
Head department of Infection Biology, Leibniz Institute for Natural Product Research and Infection Biology – Hans Knöll Institute (HKI)
Since 2002 : Deputy Leibniz Institute for Natural Product Research and Infection Biology – Hans Knöll Institute (HKI)
2004: Research Price of the state of Thüringen
2007: Heinz Spitzbart Price of the European Society for Infectious Diseases in Gynecology and Obstetrics
2008: EFIS Lecture Award of the European Society of Immunological Societies
2009: Main Research Price of the German Society for Hygiene and Microbiology.
Research Interest
Role of Complement in homeostasis, health and disease; Infection biology
of human pathogenic fungi (Candida albicans), Immune response and regulation on infectious pathogens, genetic basis for autoimmunity, infectious diseases and kidney disorders.
Memberships and scientific management
President and Board member of the European Complement Network (2005-2011), Board member of the experimental and Clinical Immunology, Speaker of the „International Leibniz Research School for Microbial Interactions, ILRS“, Jena, German Society of Hygiene and Microbiology, (Deutsche Gesellschaft für Hygiene und Mikrobiologie (DGHM)), German Society of Nephrology, (Deutsche Gesellschaft für Nephrologie (DGfN)), German Society of Immunology (Deutsche Gesellschaft für Immunologie (DGfI)), European Working Party for the Genetics of Complement Associated Kidney Disorder, Congress President of the 14th European Meeting on Complement in Human Disease, 14EMCHD, 2013, in Jena
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