8th NovAliX Conference

Dr. Stacey SOUTHALL

Dr Stacey Southall, Director of Biophysics at Sosei Heptares Current research interests are GPCR drug discovery, primarily the contribution of biophysical and structural data to SBDD. Her team provides biophysical data such as SPR and MS to support a variety of internal and collaborative GPCR drug discovery programs. They also form the cryo-EM arm of the Sosei Heptares structural biology platform, complementing our X-ray crystallography capabilities and enabling SBDD. She completed her PhD in Biochemistry at University of Cambridge and followed this with post-doctoral positions at UEA, Institute of Cancer Research and EMBL-Hamburg prior to joining Sosei Heptares in 2014.

Dr. Dirk KESSLER

• 17 years of pharma industry experience at Boehringer Ingelheim
• Heading Structural Research Oncology Research in Vienna. Responsible for the following labs: Protein Science, Protein Crystallography, NMR & Analytics, Computational Chemistry, CryoEM
• Focus on “undruggable” cancer targets
• Responsibility for early project portfolio with respect to Enablement and Hit finding initiatives incl. FBS

Dr. Bret NANNENGA

Brent Nannenga is an Assistant Professor of Chemical Engineering in the School for Engineering Matter, Transport and Energy at Arizona State University and a member of The Biodesign Institute’s Center for Applied Structural Discovery. He received his Ph.D. in Chemical Engineering from the University of Washington in 2011 under the supervision of François Baneyx. Following his graduate studies, he conducted postdoctoral research at Janelia Research Campus (Howard Hughes Medical Institute) in the lab of Tamir Gonen, where he focused on the development and application of microcrystal electron diffraction (MicroED). Since joining Arizona State University in 2015, his research has focused on the continued development of MicroED, as well as using structure determination to engineer biomolecules and materials with novel and unique properties.

Prof. Michelle ARKIN

Michelle is a Professor of Pharmaceutical Chemistry at the University of California, San Francisco and an Adjunct Professor at the Buck Institute of Research on Aging. Her lab focuses on developing first-in-class chemical probes and drug leads for novel therapeutic targets in age-related diseases such as Alzheimer’s Disease and cancer. Michelle co-directs the UCSF Small Molecule Discovery Center (SMDC) and frequently collaborates with biotech and pharmaceutical companies. Several startup companies have grown out of work done at the SMDC. Michelle is the President of Board of Directors the Academic Drug Discovery Consortium, a member of the Board of Directors for the Society for Laboratory Automation and Screening (SLAS), and a member of the Editorial board of the Assay Guidance Manual and Current Protocols in Chemical Biology. She represents UCSF in the National Cancer Institute’s Chemical Biology Consortium and the Accelerating Therapeutics for Opportunities in Medicine (ATOM) consortium. Before UCSF, Michelle was the Associate Director of Cell Biology at Sunesis Pharmaceuticals, where she helped discover and develop inhibitors of protein-protein interactions, including IL-2/IL-2R, and LFA1/ICAM (lifitigrast).

Prof Holger STARK

Holger Stark is a Professor at the University of Göttingen and a Director at the Max-Planck-Institute for biophysical Chemistry in Goettingen. He studied Biochemistry in Berlin and obtained training in electron microscopy and image processing at the Fritz-Haber-Institute in Berlin. After a postdoc at the Imperial College in London, he moved to Marburg to become a group leader and two years later he moved to Goettingen where he is since. In 2007 he was appointed as a full Professor and 2015 as a Director of the Max-Planck-Institute. The research of Holger Stark is focused on structure determination of large macromolecular complexes such as the ribosome, spliceosome, proteasome and several enzymatic complexes by cryo-EM and X-ray crystallography. The lab develops methods for improved biochemical sample preparation, image-processing software and is involved in the development of new electron microscopical hardware.

Dr, Maria M. FLOCCO

Dr. Flocco is Vice President, Global Head of Structural Biology, Biophysics and Fragment-Based Lead Generation at AstraZeneca. Maria has 20 years of pharmaceutical industry and drug discovery experience. Previous to joining AstraZeneca, she held various positions of increasing responsibility in Pfizer and Pharmacia. Prior to her career in the pharmaceutical industry, she was a lecturer at the Centre for Structural Biochemistry of the Karolinska Institute, Stockholm. Maria received a PhD in Physical Chemistry from the City University of New York, and postdoctoral training in X-ray crystallography at the Fox Chase Cancer Centre, Philadelphia, and the Uppsala Biomedical Centre, Sweden.

Dr. MariJean EGGEN

MariJean Eggen is a Director and Scientific Lead in RNA Therapeutics at Eli Lilly, Indianapolis. MariJean joined Eli Lilly in Discovery Chemistry as a Medicinal Chemist-Oncology in 2003 after spending 3 years at Pharmacia working in Infectious Disease research. Throughout her career at Lilly she has had numerous scientific and leadership roles in small molecule Discovery Chemistry Research & Technology and now RNA Therapeutics. With the patient in mind, her teams have worked across therapeutic areas and target classes building effective cross disciplinary teams, influencing drug discovery strategies and pushing the envelope with technologies to solve complex problems. Fragment Based Drug Discovery strategies and the increasingly complex targets versus disease has pushed her interest in biophysics, ligand identification and optimization strategies and her growing perspective across modalities.

Prof. Alessio CIULLI

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.

Dr. Harren JHOTI

Harren Jhoti co-founded Astex in 1999 and was Chief Scientific Officer until November 2007 when he was appointed Chief Executive Officer. He was elected a Fellow of the Royal Society in 2018, the Royal Society of Chemistry in 2016, and of the Academy of Medical Sciences in 2015. In January 2018 he was honoured with a Lifetime Achievement Award from the UK BioIndustry Association (BIA). He received the Prous Institute-Overton and Meyer Award for New Technologies in Drug Discovery from the European Federation for Medicinal Chemistry in 2012 and was also named by the Royal Society of Chemistry as “Chemistry World Entrepreneur of the Year” for 2007.

Dr. Jhoti has published widely including in leading journals such as Nature and Science, and has also been featured in TIME magazine after being named by the World Economic Forum a Technology Pioneer in 2005. He has served on the board of the BIA, the UK BioIndustry Association and currently consults for life science venture capital firms. Before founding Astex in 1999, he was head of Structural Biology and Bioinformatics at GlaxoWellcome in the United Kingdom (1991-1999). Prior to Glaxo, Dr. Jhoti was a post-doctoral scientist at Oxford University. He received a B.Sc. (Hons) in Biochemistry in 1985 and a Ph.D. in Protein Crystallography from the University of London in 1989.

Prof. Kurt WÜTHRICH

Kurt Wüthrich is the Cecil H. and Ida M. Green Professor of Structural Biology at The Scripps Research Institute, La Jolla, CA, USA, and a Professor of Biophysics at the ETH Zürich, Zürich, Switzerland. His research interests are in structural biology and structural genomics. His specialty is nuclear magnetic resonance (NMR) spectroscopy with biological macromolecules, where he contributed the NMR method of three-dimensional structure determination of proteins and nucleic acids in solution. Kurt Wüthrich’s achievements have been recognized by the Prix Louis Jeantet de Médecine, the Kyoto Prize in Advanced Technology, the Nobel Prize in Chemistry, and by a number of other awards and honorary degrees.

Prof. Martin KARPLUS

Present Positions:
Theodore William Richards Research Professor, Harvard University, l999-2004 T. W. Richards Professor Emeritus of Chemistry, Harvard University, 2004-present Professeur Conventionné, Université Louis Pasteur (now Université de Strasbourg), Strasbourg, 1995-present

Education:
Harvard College, B.A., 1950
California Institute of Technology, Ph.D., 1953 (with Linus Pauling)
Oxford University, Postdoctoral Fellow, 1953-55 (with C.A. Coulson)

Professional Career:
National Science Foundation Postdoctoral Fellow, Oxford University, 1953-55
Instructor 1955-57, Assistant Professor 1957-60, Associate Professor 1960, University of Illinois
Associate Professor 1960-63, Professor 1963-66, Columbia University
Professor, Harvard University, 1966-1979
Professeur Associé, Université de Paris-Sud, 1972-73
Professeur, Université de Paris VII, 1974-75
Theodore William Richards Professor of Chemistry, Harvard University, l979-1999
Professeur Associé, Université de Paris-Sud, 1980-81
Professeur, Collège de France, Paris, 1980-81, 1987-88
Professeur Associé, Université Louis Pasteur, Strasbourg, 1992, 1994-95
Eastman Professor, Oxford University, 1999-2000
Linnett Visiting Professor, Cambridge University, Fall 2003

Honors & Awards:
Antonio Feltrinelli International Prize for Chemistry from Accademia Nazionale dei Lincei, 2011
Nobel Prize in Chemistry, 2013
Foreign Fellow of the Royal Society of Chemistry, 2013
Commandeur de la Legion d’Honneur, 2014
Doctor Honoris Causa, Bar-Ilan University, 2014

Memberships:
American Academy of Arts & Sciences, 1966
National Academy of Sciences, 1967
International Academy of Quantum Molecular Science, 1967
Netherlands Academy of Arts & Sciences (foreign member), 1991
The Royal Society, U.K. (foreign member), 2000
Foreign Fellow of the Royal Society of Chemistry, 2013

Research Field:
The research of Dr. Karplus is in theoretical chemistry, including the electronic interpretation of NMR and ESR spectra of molecules, the development of techniques for the evaluation of molecular properties, and the formulation of detailed models for chemical reactions. His recent work is concerned with molecules that play an important role in living systems.

Prof. Jean-Pierre CHANGEUX

Jean-Pierre Changeux PhD is International Faculty at the Kavli Institute for Brain & Mind University of California San Diego and professor at the Collège de France & Institut Pasteur, Paris. His PhD studies with Jacques Monod, led to the discovery that chemical signals regulate the biological activity of proteins by acting at “allosteric” sites distinct from the biologically active sites via a conformational change (1961-1965). He then proposed (1964) that this type of regulation applies to receptor mechanisms engaged in the transmission of chemical signals in the nervous system and through his life-time work, validated this insight. His studies were initiated by the first identification of a neurotransmitter receptor: the nicotinic acetylcholine receptor together with Lee & Kasai (1970) and culminated by a contribution, together with Corringer & Delarue, to establishing the 3-D structure and conformational transition of prokaryotic orthologs of nicotinic receptors by X-ray crystallography and molecular dynamics (2005-15). He and his colleagues also deciphered the topology of allosteric modulatory sites for pharmacological ligands (1996-2011), thereby substantiating a novel strategy of drug design based on allosteric modulation. Moving to neuronal networks, Changeux, together with Courrège & Danchin (1973, 1976) formulated and experimentally tested the theory that long-term epigenesis of neuronal networks occurs by the activity-dependant selective stabilization, and elimination, of developing synapses. Last, in particular with Dehaene, he proposed and tested models for defined cognitive tasks and their pharmacological modulation in particular, a neuronal hypothesis for conscious processing, implicating a “global neuronal workspace” composed of a brain-scale horizontal network of long axon neurons (1991- (1998-2015).
Changeux has published several books including Neuronal Man (1985), What Makes Us Think? (with Paul Ricoeur) (2002), Physiology of truth (2002).
His academic accolades include the Gairdner award (1978), the Wolf prize (1983), the Goodman and Gilman Award in drug receptor pharmacology (1994), the Balzan Prize (2001), the US National Academy of Sciences Award in Neurosciences (2007), the Japanese Society for the Promotion of Science Award for Eminent Scientists,Tokyo (2012) and the Olav Thon Foundation’s International Research Award for. Mathematics/ Natural Sciences and Medicine, Oslo (2016).

Dr Dan ERLANSON

Dr. Daniel A. Erlanson is the co-founder of Carmot Therapeutics and an inventor of its iterative fragment-linking technology, Chemotype Evolution. Prior to Carmot, Dr. Erlanson spent a decade developing technologies and leading medicinal chemistry efforts in oncology and other diseases at Sunesis Pharmaceuticals, which he joined at the company’s inception. Before Sunesis, he was an NIH postdoctoral fellow with James A. Wells at Genentech. Dr. Erlanson earned his PhD in chemistry from Harvard University in the laboratory of Gregory L. Verdine and his BA in chemistry from Carleton College. As well as co-editing two books on fragment-based drug discovery, Dr. Erlanson is an inventor or author on more than forty patents and scientific publications. He edits a blog devoted to fragment-based drug discovery, Practical Fragments (http://practicalfragments.blogspot.com/).

Dr Alain BECK

Alain Beck is Senior Director of Analytical Chemistry, New Biological Entities, at the Center of Immunology Pierre Fabre (FR) and associated editor of mAbs (USA). He has contributed to the R&D of clinical stages anticancer mAbs and ADCs (dalotuzumab licensed to Merck, telisotuzumab vedotin licensed to AbbVie and h515H7) and vaccines (RSV, ELA/P40). He has published 176 papers and reports on mAbs, biosimilars, biobetters, ADCs, bsAbs, Fc-fusion structures/functions relationships and developability. He was involved in more than 230 scientific meetings (AIS, ASMS, BAS, EAC, HPLC, IBC, IMSC PEGS, SEP, WADC, WBC) as chairperson, invited speaker, panelist, moderator, advisor, and organizer as well as meetings with regulatory agencies (ANSM, EMA, EDQM, FDA, PEI, WHO).

Dr Gerard BRICOGNE

Gerard Bricogne is the founder and director of Global Phasing Ltd., a small non-profit research group specialised in methods and software for macromolecular X-ray crystallography, supported mostly by a Consortium of pharmaceutical companies who make extensive use of its software. He started his PhD work in 1972 at the MRC Laboratory of Molecular Biology, under the supervision of David Blow, at a time when there were only 12 structures in the PDB, and has dedicated his whole research career to the field of mathematical and computational methods. He applied his PhD work on non-crystallographic symmetry to the solution of the first two virus crystal structures, then became interested in the role of probability theory in the direct solution of the phase problem. This led him to introduce Bayesian statistical methods into the areas of experimental phasing and structure refinement, implemented respectively in the SHARP and BUSTER programs from his group. His other interests have been in the improvement of processing methods for diffraction data, through an EEC Workshop held in 1986-89 whose influence is still felt today, and more recently in improving the design and conduct of diffraction experiments themselves. His contributions to the advancement of crystallographic methods were recognised by the award of the Aminoff Prize of the Royal Swedish Academy of Sciences in 2009.

Dr Sandra JACOB

Sandra Jacob is executive director and head of Structural Biophysics in the Novartis Institutes for BioMedical Research in Basel, Switzerland. Her group works mainly in lead discovery and optimization using X-ray, NMR and other biophysical methods to find and characterize interactions of ligands with proteins and RNA. Sandra is recognized for her expertise in kinase inhibition and her work has resulted in the discovery of Tasigna, a drug for the treatment of Chronic Myelogenous Leukemia. She is a driver of novel approaches for target modulation, the most recent examples being non-ATP site inhibitors of kinases. She studied Chemistry at the University of Melbourne in Australia and followed this up with a Ph.D. using protein crystallography at the St. Vincent’s Institute of Medical research in Melbourne. She joined Ciba Geigy, now Novartis, after studies including lipocalins at Uppsala University in Sweden and focusing on membrane proteins at the University of Basel.

Prof. Gerhard KLEBE

Gerhard Klebe is full professor for pharmaceutical chemistry at the University of Marburg, Germany. His research is directed towards the understanding of protein-ligand interactions using chemical synthesis, microcalorimetry, molecular biology, crystallography, bioinformatics and software development. Software tools such as CoMSIA, AFMoC, DrugScore, Relibase/Cavbase or MOBILE have been developed in the group. He studied chemistry in Frankfurt/M, obtained his PhD in physical chemistry and spent postdoctoral stays in France and Switzerland. In BASF he was responsible for molecular modeling and crystallography. In 2005 he refused an offer from ETH Zürich, for a chair in Pharmaceutical Chemistry, published more than 280 scientific papers, serves on the editorial board of several journals, was member of the Board of Governors of the CCDC and is on the advisory board of the Leibniz-Institute FMP in Berlin. In 2011 he received an ERC Advanced Grant to support the research of his group. He organizes in two years frequency an International Workshop on New Approaches in Drug Discovery and Design. Further details: www.agklebe.de.

Prof. Sir Tom BLUNDELL

Sir Tom Blundell FRS, FMedSci University of Cambridge 1. Research interests in the molecular architecture of living organisms have been focused on molecular and structural biology of growth factors, receptor activation, signal transduction and DNA repair, important in cancer and other diseases. Tom Blundell has characterised the roles of multiprotein assemblies in achieving high signal-to-noise in cell regulatory and signalling systems. He also has developed extensive software, pioneering knowledge-based approaches for structural bioinformatics that are used worldwide in academia and in the biotech and pharmaceutical industries. He has developed new approaches to exploring biological and chemical space for target selection and lead discovery in the development of candidate drugs. He has published over 500 research papers, including 30 in Nature and Science. 2. Academic 1964 BA in Natural Sciences; 1967 D.Phil. Oxford University; 1973 Lecturer, Biological Sciences, Sussex University; 1976-1996 Professor of Crystallography, Birkbeck College, London; 1991-96 Chief Executive Officer, AFRC; Founding CEO, BBSRC; 1996 – 2009 William Dunn Professor and Head of Biochemistry, University of Cambridge; 2003- 2009 Head, School of Biological Sciences, Cambridge; 2009-2016, Director of Research; Emeritus Professor Biochemistry, Cambridge; 2. Honours 1984 FRS; 1985 Member of EMBO; 1986 Alcon Award; 1987 Gold Medal, Institute Biotechnology; 1987 Krebs Medal, FEBS; 1988 Ciba Medal, Biochemical Society; 1988 Feldberg Prize in Biology and Medicine; 1993 Member Academia Europaea; 1995 Fellow, Indian National Science Academy; 1996 Gold Medal, Society for Chemical Industry; 1997 Knighthood; 1998 First Recipient, Pfizer European Prize for Innovation; 1998 Bernal Medal, Royal Society; 1999 Founding Member, Academy of Medical Sciences; 2005-2008 President UK Biosciences Federation; 2006 Hon Memb, British Biophysical Society; 2006 Honorary Fellow Royal Society Chemistry; 2008 Foreign Member, Third World Academy of Sciences; 2008 Ramachandran Professor, IISc Bangalore; 2009-2011 President, Biochemical Society; Honorary Fellow. 2011 Foreign Member Chilean Academy of Sciences. 2011 President, UK Science Council; 2012 Honorary Fellow, Society of Biology 3. Industry: companies founded, boards etc Astex Therapeutics: Co-founder, 1999, Board Member, Chair SAB 1999-2011; Biofabrika: Co-founder, 1989 – 1991; Celltech: Non-executive Director, 1996-2004; Chair SAB, 1998- 2004; UCB Celltech, Science Advisory Board, 2005; SmithKline Beecham: International R&D Board, 1997-1999; Pfizer: Consultant in UK and USA, 1983-1990; Parke Davis: US Consultant, 1987-1990; Abingworth Management Ltd, Science Advisory Board, 1986-1990, 1996-; Syntaxin: member of SAB; FEI: SAB 2007-2010; Isogenica, Scientific Consultant, 2008 – 4. Public Bodies: Research Councils: AFRC Council (1985-1990); DG, (1991-1994); BBSRC Founding CEO, BBSRC, 1994-1996. Non-executive Chairman of BBSRC: 2009 – Royal Commission on Environmental Pollution, Chairman (1998-2005); Advisory Council on Science and Technology (ACOST) Cabinet Office (1988-1990).

Dr David SWINNEY

David Swinney has over 20 years of industrial experience (Roche, Syntex) working to identify promising leads, clinical candidates and effective mechanisms of drug action to address unmet medical needs. Dave has a PhD in medicinal chemistry from the University of Washington, Seattle, a recognized expertise in binding kinetics and biochemical pharmacology, and is currently at the non-profit Institute for Rare and Neglected Diseases Drug Discovery, aka iRND3, working to identify new drug discovery starting points to address unmet medical needs.