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Keynote SpeakersDissecting Protein-Protein Interaction Networks (KL01)
Microcrystal Electron Diffraction (MicroED): Methodology and Applications (KL02)
Session 1: Hot Topics - COVID-19SARS-CoV-2 3CL protease:
Structure-Based Virtual Screening, Crystallographic Fragment Screening and Assay Implementation to Identify Novel Starting Points for Inhibition (OC02)
Structural and Functional Analysis of the D614G SARS-CoV-2 Spike Protein Variant (OC01)
Session 2: Induced-Proximity Drug Discovery : Selective Protein Degraders, PPI Stabilizers, etc.The Structural Basis of Indisulam-Mediated Recruitment of RBM39 to the DCAF15-DDB1-DDA1 E3 Ligase Complex (IL01)
Targeting a Cryptic Binding Pocket by Disulfide-Induced Rupture of a Homodimeric Protein-Protein Interface (OC03)
Session 3: Integrative Structural Biology & BiophysicsInhibition of the Cysteine Desulfurase in the SUF Pathway of Iron-Sulfur Cluster Biogenesis Towards Development of Novel Antibacterials (OC06)
Hijacking Molecular Plasticity to Fine Tune Nuclear Receptor Signaling: Stuctural Proteomics and Precision Therapeutics (IL02)
Fragment Screening Reveals a Novel Pocket in Cysteine Protease ATG4B (OC05)
Synergistic Use of Ligand Based NMR and Crystallography to Elucidate Small Molecules Interactions with Challenging Targets (OC04)
Identification, Characterization and Conformational Assessment of STING Modulators (IL03)
Session 4: Cryo-EM in Drug Discovery - Accelerating Drug Design for Intractable Targets
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![]() | Dr Kenneth BORRELLI (SCHRÖDINGER, INC., New York, United States) Read more Kenneth Borrelli, PhD is a Senior Principal Scientist at Schrodinger, Inc in New York, USA. Schrödinger’s industry-leading computational platform to accelerate drug discovery is deployed by leading biopharmaceutical and industrial companies, academic institutions, and government laboratories worldwide. Schrödinger is using its platform to advance a pipeline of drug discovery programs including collaborations with pharmaceutical companies, co-founded biotech companies and internal programs. Dr Borrelli manages a research and development group at Schrodinger tasked with pushing the boundaries of structure-based drug discovery. His research interests include cryo-EM model refinement, homology modeling and ADMET modeling.
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Structural Characterization of Different TRPA1 Inhibitors (IL05)
![]() | Dr Lionel ROUGÉ (GENENTECH, San Francisco, United States) Read more As a trained biochemist, my main function within the Structural Biology group has been to deliver high quality proteins for drug discovery applications (assay, immunization campaign or structural studies). After working for many years on soluble targets using crystallography, I have been more recently focused on the structural biology of membrane proteins: in order to enable these high value targets for structure-based drug design, I have been using cryo-EM. In parallel, I have also been interested in understanding the function and activation mechanism of these channels using modulators such as agonists.
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Using Cryo-EM for GPCR Drug Discovery and Development (IL07)
![]() | Prof. Patrick M. SEXTON (MONASH UNIVERSITY, Parkville, Australia) Read more Professor Sexton is a NHMRC Senior Principal Research Fellow at the Monash Institute of Pharmaceutical Sciences, and Director of the ARC Centre for Cryo-electron Microscopy of Membrane Proteins (www.ccemmp.org). He is a leader in the study of GPCRs, biased agonism, on allosteric interactions between GPCRs and other proteins, and small molecule ligands. More recently, his team has been at the forefront of the application of cryo-EM to elucidation of the structure and dynamics of GPCRs. Prof. Sexton’s awards include the ASCEPT Lecturer award, Endocrine Society of Australia Senior Plenary award, Rand Medal (ASCEPT), Vane Medal (British Pharmacological Society (BPS)), and the GSK Research Excellence award. Prof. Sexton is a Clarivate Analytics Highly Cited Researcher, a corresponding member of the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification, a member of the Faculty of 1000 (Molecular Pharmacology division) and an elected Fellow of the BPS.
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From Concept to Reality: CryoEM as an Integral Part of Drug Discovery and Development (IL04)
![]() | Dr Corey STRICKLAND (MERCK, Kenilworth, United States) Read more Dr. Corey Strickland received his Ph.D. from Cornell University and Joined Merck Structural Chemistry, Kenilworth in 1995. He is currently a Sr. Principal Scientist, Structural Chemistry and is head of cryoEM and Structural Chemistry Sourcing. Corey’s work at Merck has spanned multiple disease areas and ranged from lead identification to process development. His research interests include X-ray crystallography, cryo-EM, bioNMR, structure and fragment-based drug discovery. His current focus is on expanding the role and impact of cryoEM on the Merck pipeline. Corey is an alumnus of The Pennsylvania State University.
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Session 5: Advances in Biophysical Techniques : Single-Molecule Techniques, Label-Free Technologies, Surface-Immobilized Techniques beyond SPR, etc.
Too Weak for Biophysics: Concentration-Dependent Crystallographic Soaking as Tool for Fragment Hit Prioritisation (OC10)
![]() | Ms Yuliya DUBIANOK (UNIVERSITY OF OXFORD, Oxford, United Kingdom) Read more Yuliya studied chemistry at the Technical University (TUM) in beautiful Munich, Bavaria - with study and research stays in Ireland and Sweden. Following an internship in the automation team in the Biopharmaceutical Department at Boehringer Ingelheim, Germany, Yuliya joined Frank von Delft’s group at the University of Oxford in October 2017 as a DPhil student. The focus of her work was quantification of crystallographic fragment hits and their progression into potent binders. Recently, Yuliya completed her DPhil and has now joined the Bio Structure and Biophysics unit at Sanofi in France.
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Development of a Microscale Thermophoresis-Based Method for Screening Inhibitors of the Methyl-Lysine Reader Protein MRG15 (OC08)
![]() | Dr Alessandra FEOLI (UNIVERSITÀ DEGLI STUDI DI SALERNO, Fisciano (Salerno), Italy) Read more Alessandra Feoli received her Master of Science degree in “Pharmaceutical Chemistry and Technology” in 2011 at the University of Salerno. Her research thesis, performed at the Oncology Research Center (CROM) of “National Cancer Institute of Naples (INT)- Fondazione G. Pascale” was focused on the mutational analysis of EGFR gene in non-small cell lung cancer, under the supervision of M.D. Nicola Normanno. In 2012 she spent 3 months at Ludwig Maximilian University of Munich (Germany) in the laboratory of Prof. Axel Imhof for the COST action "Epigenetics: From Bench to Bedside." In 2015 she spent six months as visiting scientist at Nanotemper technologies in Munich, where she deepens her knowledge in MST and nanoDSF. In 2016 she obtained her Ph.D in Pharmaceutical Sciences at University of Salerno under the supervision of Prof. Gianluca Sbardella discussing a thesis entitled: “Biomolecular and biophysical approaches to interrogate epigenetic targets: a platform for drug discovery.” From 2016, she is Postdoc at University of Salerno working on different biochemical and biophysical techniques for the identification of new modulators of epigenetic targets.
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Focal Molography - A New Bioanalytical Tool to Eliminate Guess Work in Pharma Research (OC09)
![]() | Dr Volker GATTERDAM (LINO BIOTECH AG, Zurich, Switzerland) Read more Dr. Volker Gatterdam studied chemistry in the beautiful city of Marburg in Germany. He holds a doctoral degree with summa cum laude in biochemistry from the University of Frankfurt where he laid a solid foundation for his scientific interests. His work is focused on the chemical modifications of surfaces for the design and fabrication of biosensors. His interest in the fascinating technology of focal molography started during his PostDoc in Prof. Janos Vörös´group at ETH Zurich. His continuous passion for the technology led him to be one of the co-founders of lino Biotech.
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Ligand-Dependent Structural Plasticity of TrkA Kinase Studied by NMR Spectroscopy (IL08)
![]() | Dr Reto HORST (PFIZER, INC., Grotton, United States) Read more Dr. Reto Horst is a Principal Scientist in the Structural and Molecular Sciences group at Pfizer in Groton, CT. He is developing and applying cutting edge NMR methods to identify and validate hits from various screening funnels and to characterize protein–ligand interactions. Dr. Horst has guided fragment-based drug discovery efforts in various disease areas and made key contributions to several discovery projects. Dr. Horst obtained a diploma (MSc) in Physics and a PhD in Biophysics under the supervision of Nobel Laureate Dr. Kurt Wuthrich at the ETH in Zurich, Switzerland. Before joining Pfizer in 2012, he was a Staff Scientist at Scripps Research in La Jolla, CA, where his research was focused on studying GPCR signalling pathways and chaperonin-assisted protein folding by solution state NMR spectroscopy, resulting in more than 30 peer-reviewed publications that appeared in Tier 1 journals including Cell, Science and PNAS.
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SAR by 19F NMR: Using Protein-Observed Fluorine NMR for Targeting Protein Complexes (IL09)
![]() | Prof. William POMERANTZ (UNIVERSITY OF MINNESOTA, Minneapolis, United States) Read more William C. K. Pomerantz, Associate Professor of Chemistry, University of Minnesota. Prof. Pomerantz received his B.S. in chemistry from Ithaca College in 2002, followed by a Fulbright Fellowship at ETH, Zurich with Professors François Diederich and Jack Dunitz. He obtained a Ph.D. in chemistry under Professors Sam Gellman and Nick Abbott at the University of Wisconsin-Madison and was a postdoctoral fellow under Prof. Anna Mapp at the University of Michigan. He joined the chemistry faculty at the University of Minnesota in 2012. He is currently a McKnight Presidential Fellow. His research develops chemical biology and medicinal chemistry approaches to modulate protein-protein interactions. Protein-Observed Fluorine NMR (PrOF NMR) is one such tool in his lab that is being developed for fragment-based ligand discovery, and has been applied towards inhibiting epigenetic protein complexes. Prof. Pomerantz is currently the global council co-chair for the International Chemical Biology Society and Early Career Board Member for ACS Med. Chem. Lett.
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Real-Time Single-Molecule Detection of Drug-Protein Interactions Using a Novel DNA-Based Nanoscale Actuator (OC07)
![]() | Prof. Terence STRICK (ECOLE NORMALE SUPERIEURE, Paris, France) Read more Prof. Strick has carried out pioneering work in the field of single-molecule biophysics and continues to investigate fundamental molecular processes such as DNA transcription, replication and repair. In parallel he develops novel instruments and molecular substrates to be used in such assays, with the aim of making single-molecule approaches as widely applicable to as many different systems as possible. Recent developments now make it possible to use single-molecule measurements to directly charcterize drug-protein and protein-protein interactions in real-time, providing unique new insights into their modes of association and dissociation.
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Panel Discussion: Cryo-EM in Drug Discovery - Accelerating Drug Design for Intractable Targets
Speakers
![]() | Mr Benjamin APKER (MITEGEN, Ithaca, United States) Read more Ben has spent his 14 year career with MiTeGen, driving business, operations, and product development. His understanding of the company’s and industry’s needs has allowed him to play a critical role in the rapid growth of MiTeGen’s international reputation. With expertise in customer relations, product-line management, industry innovation, and operations, Ben provided a critical leadership role in the development of nearly all aspects of MiTeGen. In addition, his expertise in cryo-EM and X-ray Crystallography methods development and developing technologies for high-throughput sample preparation, vitrification, and cryogenic storage and transport led to tools and methods that are utilized world-wide to further our understanding of the molecular structures of everything from basic materials to viruses. Ben graduated with honors in Physics from SUNY at Geneseo, and was inducted into the National Physics Honors Society.
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![]() | Dr Corey STRICKLAND (MERCK, Kenilworth, United States) Read more Dr. Corey Strickland received his Ph.D. from Cornell University and Joined Merck Structural Chemistry, Kenilworth in 1995. He is currently a Sr. Principal Scientist, Structural Chemistry and is head of cryoEM and Structural Chemistry Sourcing. Corey’s work at Merck has spanned multiple disease areas and ranged from lead identification to process development. His research interests include X-ray crystallography, cryo-EM, bioNMR, structure and fragment-based drug discovery. His current focus is on expanding the role and impact of cryoEM on the Merck pipeline. Corey is an alumnus of The Pennsylvania State University.
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![]() | Dr Denis ZEYER (NOVALIX, Illkirch, France) Read more Denis earned his M.Sc. in biological crystallography and NMR at the Louis Pasteur University (Strasbourg, France). His Ph.D. in protein X-ray crystallography (with Dr. Jean-Paul Renaud and Dr. Dino Moras at the Institute of Genetics and Molecular and Cellular Biology, Strasbourg, France, in collaboration with Bristol Myers Squibb) led to the publication of pioneering structures in the PPAR family of nuclear receptors. In 2003 Denis built structural biology and biophysics groups and launched the research services business of AliX. In that capacity he has been instrumental in building a sound client base including major pharmaceutical companies; establishing a reputation for scientific excellence and reliability; and in technical improvements though internal and external innovations. Denis was appointed CEO of AliX in 2008 and has been CEO of NovAliX since its inception. He has been instrumental in the implementation of Novalix’ cryo-electron microscopy platform in 2015 and its subsequent development with a strong focus for the use of cryoEM in structure-based drug design.
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