Speakers

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Samuel Sparks
Senior Investigator
Silicon Therapeutics

Dr. Samuel Sparks is a scientist with expertise in biomolecular NMR, small angle scattering and protein-ligand interactions. His work at Silicon Therapeutics focuses on utilizing NMR methods to support and facilitate drug discovery. He also develops methodology to integrate biophysical data with molecular dynamics simulations, working closely with Silicon’s computational team. During his doctoral research Sam characterized the interactions between intrinsically disordered nuclear pore proteins and transport factors that underlie the fast and selective transport of macromolecules through the nuclear pore complex (NPC). This research helped to elucidate NPC’s translocation mechanism and expanded the understanding of the mechanisms of interactions involving disordered proteins. He received his bachelor’s and master’s degree in Chemistry from Clark University and his PhD in Biochemistry from Albert Einstein College of Medicine under the supervision of Dr. David Cowburn.

Day Two

WEDNESDAY 18 NOVEMBER 2020

11:30 am | Drugging the Undruggable: Integration of Biophysics, Genetics, Molecular Dynamics and Docking

Evris Gavathiotis
Professor of Biochemistry & Medicine
Albert Einstein College of Medicine

Dr. Evris Gavathiotis is a Professor of Biochemistry and Medicine at Albert Einstein College of Medicine. He received his B.Sc. in Chemistry at the University of Crete, Greece and his Ph.D. in biological chemistry from the University of Nottingham, UK. He completed postdoctoral research at Rockefeller University and at Dana-Farber Cancer Institute and he was junior faculty at Harvard Medical School. In 2011, he started his lab at Einstein and became tenured full professor in 2019. His research focuses on mechanisms and protein interactions in cell death and cell survival signaling and the discovery and optimization of small molecule modulators towards novel chemical tools and therapeutics. His research has pioneered mechanistic insights of BCL-2 family proteins and other key signaling proteins. He has discovered first-in-class small molecules for several “undruggable” targets and demonstrated novel pharmacological strategies. His research has contributed to the founding of three biotechnology companies (Stelexis Therapeutics, Selphagy Therapeutics, Aspida Therapeutics) that are advancing novel therapeutics for cancer and aging-associated diseases. Dr. Gavathiotis has received numerous awards for his research including the Sidney Kimmel Scholar Award, the 2014 Young Chemical Biologist Award, the Pershing Square Sohn Prize and the Irma T. Hirschl Career Scientist Award.

Day Two

WEDNESDAY 18 NOVEMBER 2020

9:00 am | Harnessing Structure-Based Technologies for Novel Target and Drug Discovery

Nathan Fuller
Director of Chemistry
Alkermes

Nathan received his Ph.D. from the University of North Carolina at Chapel Hill under the guidance of James Morken.  He then went on to conduct post-doctoral research in the lab of Stephen F. Martin at the University of Texas at Austin.  He began his career as a medicinal chemist at Wyeth Research in Cambridge, MA working in the inflammation group, and then joined Satori Pharmaceuticals in Cambridge, MA where he worked on a program targeting gamma-secretase modulators for the treatment of Alzheimer’s disease.  In 2013, Nathan began a role at AstraZeneca in Waltham, MA in the Chemistry Innovation Centre, working in the Fragment-Based Lead Generation group.  In late 2015, he joined the team at Rodin Therapeutics, leading the chemistry efforts that resulted in the discovery of complex selective HDAC inhibitors for the treatment of synaptic pathology in neurologic disorders.  In late 2019 Rodin Therapeutics was acquired by Alkermes, and Nathan has continued working with Alkermes to harness the potential of complex selective HDAC inhibitors as therapeutic approaches for neurologic disorders with synaptic pathology.

Day Two

WEDNESDAY 18 NOVEMBER 2020

1:30 pm | CoREST Complex-Selective HDAC Inhibitors Promote Pro-Synaptic Effects and Represent Promising Therapies to Treat Synaptopathies

Christopher Browne
Senior Research Scientist
AstraZeneca

Chris Browne is a Senior Research Scientist in Chemical Biology & Proteomics at AstraZeneca. His team focuses on supporting all therapeutic area’s drug discovery programs using cutting-edge mass spectrometry-based proteomics with specific emphasis on small molecule target identification and validation, target engagement, and selectivity profiling. Before AstraZeneca, Chris completed a post doc at Dana-Farber Cancer Institute and Harvard Medical School, focusing on proteome wide discovery of covalent inhibitor modification sites and development of covalent small molecule probes for understudied kinases.

Day One

TUESDAY 17 NOVEMBER 2020

12:00 pm | The New Age of Discovery: Harnessing Chemoproteomics for Small Molecule Drug Design

Douglas Johnson
Senior Director of Chemical Biology & Proteomics
Biogen

Douglas Johnson is a Senior Director of Chemical Biology & Proteomics at Biogen in Cambridge, MA. Prior to moving to Biogen, Doug was at Pfizer for 18 years where his most recent position was Senior Scientific Director and Head of Chemical Biology in Cambridge, MA.  Prior to Pfizer, Doug was an NIH postdoctoral fellow at Harvard University in the laboratory of Professor David A. Evans. He obtained his Ph.D. in organic chemistry at The Scripps Research Institute under the guidance of Professor Dale L. Boger and graduated summa cum laude from the University of Minnesota with a BS in chemistry. He is an author or inventor on more than 90 publications and patents.

Day One

TUESDAY 17 NOVEMBER 2020

9:00 am | Application of Chemical Biology Probes and Bioorthogonal Chemistry in Drug Discovery

Nick Shah
Head of In Vitro Pharmacology
DiCE Molecules

Nick is a scientist and leader with extensive experience in leading cross-functional technical teams that build tools to interrogate difficult drug targets. He currently leads the In Vitro Pharmacology efforts at DiCE Molecules where the team is working to leverage chemical evolution in small molecule drug discovery. Prior to DiCE, Nick was an early scientist at Flexus Biosciences / FLX Bio and helped discover two molecules that are currently in clinical testing for cancer immunotherapy: BMS-986205 in multiple Phase II trials & FLX475 in Phase I. Throughout his career, he has been deeply involved in assay development for drug discovery while leading project teams and managing multiple large-scale screening campaigns.  In his spare time, Nick advises early-stage startup founders through two accelerators: Springboard and Creative Destruction Lab.  Nick completed his PhD at the University of Toronto and a postdoctoral fellowship at Stanford University.

Day One

TUESDAY 17 NOVEMBER 2020

8:50 am | Chair’s Opening Remarks

Christopher Dimitri
Investigator
GSK

Christopher joined GSK in 2016 and with others developed the Encoded Library Technology platform to serve as a robust technology with which to assess small molecule tractability of novel targets.  Prior to joining GSK, he worked with aptamers as both research tools while at Novartis and as a therapeutic modality while at Archemix. He obtained my Ph.D. in Cell Biology from Harvard Medical School where worked on the Ras-MAPK signaling pathway in the lab of Dr. John Blenis.

Day One

TUESDAY 17 NOVEMBER 2020

1:30 pm | Predicting Small Molecule Tractability of Novel Targets to Prioritize and Accelerate Hit Identification Activities

Benjamin Ruprecht
Associate Principal Scientist of Chemical Biology
Merck

Benjamin Ruprecht is an Associate Principle Scientist in the Chemical Biology and Chemoproteomics group at Merck Research Laboratories in Boston, MA. His focus is on the development and application of mass spectrometry-based proteomics, chemoproteomics and bioinformatics tools to support diverse and multi-disciplinary drug discovery projects. He earned his PhD at the Technical University of Munich in the laboratory of Prof. Dr. Bernhard Kuster where he worked on chemoproteomic affinity matrices, studied mechanisms of drug resistance and developed phosphoproteomics methods to deconvolute cellular signalling pathways.

Day One

TUESDAY 17 NOVEMBER 2020

3:30 pm | A High-Throughput, Mass Spectrometry-Based Proteomics Platform for Rapid Drug Perturbation Profiling

Thomas Smith
Senior Investigator
Novartis

Thomas Smith earned a MA and PhD in biological sciences at the University at Buffalo, NY and completed post-doctoral studies at the University of Cincinnati College of Medicine, OH in cell pharmacology and biophysics.  In 2001, Dr. Smith joined the scientific staff in the Department of Cardiovascular and Metabolic Diseases at Genetics Institute / Wyeth Research in Cambridge, MA focusing on platelet biology and therapies for cardiovascular diseases, before joining the Novartis Institutes for Biomedical Research in Cambridge, MA in 2007.  In his current role in the department of Chemical Biology and Therapeutics at Novartis, Dr. Smith works with project teams from multiple disease areas to enable early stage drug discovery efforts on new programs of therapeutic interest.  He is co-author or inventor on over 30 publications and patents.

Day One

TUESDAY 17 NOVEMBER 2020

11:30 am | Finding the Needle in the Haystack: Learnings in Integrated Lead Discovery

Day Two

WEDNESDAY 18 NOVEMBER 2020

8:50 am | Chair’s Opening Remarks

Reto Horst
Principal Scientist
Pfizer

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.

Day Two

WEDNESDAY 18 NOVEMBER 2020

9:30 am | Ligand-Dependent Structural Plasticity of TrkA Kinase Studied by NMR Spectroscopy

Grahame McKenzie
Chief Scientific Officer
Phoremost

Grahame is a biologist with 15 years of experience in academic and industrial drug discovery. After completing his PhD at the MRC LMB, Grahame worked in big pharma for Novartis and then GlaxoWellcome, and then for Lorantis, a start-up biotech. After 7 years working with Ashok Venkitaraman at the MRC Cancer Unit in Cambridge, Grahame co-founded PhoreMost with Torrance and Venkitaraman, and joined the company full-time at Babraham in 2015.

Day One

TUESDAY 17 NOVEMBER 2020

2:00 pm | PROTEINi: A Unique Approach to Expand Druggable Space

Kristin Riching
Senior Research Scientist
Promega

Kristin received her PhD in Biomedical Engineering from the University of Wisconsin – Madison, where she studied the structural and mechanical properties of collagen fibers and their effects on breast cancer cell migration in invasive ductal carcinoma.  She joined Promega in 2014 as a postdoctoral researcher and is currently a Senior Scientist developing technologies to characterize degradation and protein interactions within the ubiquitin proteasomal pathway in living cells.

Day One

TUESDAY 17 NOVEMBER 2020

10:00 am | Monitoring Dynamics of Protein Degradation in Living Cells

Dave Wustrow
SVP of Discovery & Pre-Clinical Development
RAPT Therapeutics

David joined RAPT Therapeutics in 2016 bringing more than 20 years of drug discovery experience. He previously led chemistry efforts at Cleave Biosciences directed towards the discovery and development of first in class agents for the treatments of solid and hematologic malignancies. Previously he directed chemistry efforts at Xenoport, Neurogen and Pfizer.

Day Two

WEDNESDAY 18 NOVEMBER 2020

10:00 am | Leveraging Structure Based Design with Computational Chemistry to Discover Novel USP7 Inhibitors with Enhanced Potency

Arek Kulczyk
Assistant Professor of Biochemistry, President and Founder of CryoEMcorp
Rutgers University

Dr. Arek Kulczyk is an Assistant Professor of Biochemistry at Rutgers University and President and Founder of CryoEMcorp, a consulting company providing expert advice in the field of cryo- EM.  Kulczyk laboratory (http://kulczyk-lab.cryoemcorp.com) integrates structural approaches, in particular single-particle cryo-EM, cryo-ET, CLEM and single-molecule methods to study large macromolecular assemblies with medical relevance.  Currently, the main focus of the laboratory is on structure determination of human mitochondrial replisome, complexes involved in apoptotic signalling and other multi-protein assemblies. By using the above methods, Dr. Kulczyk expects to reveal mechanistic information that may subsequently facilitate development of novel therapeutics against cancer and neurodegenerative disorders.  Arek earned his Ph.D. in biophysics from the MRC LMB at the University of Cambridge, the birthplace of cryo-EM.  His graduate work focused on structure determination of DNA-binding domains from DNA ligase III and PAPR, the two medically important proteins involved in DNA repair.  During his postdoctoral studies at Harvard University, Arek developed single-molecule methods to study DNA replication.  Prior to joining Rutgers, Arek held a junior faculty appointment at Harvard Medical School, where he determined a cryo-EM structure of bacteriophage T7 replisome, the first structure of a functioning replication complex assembled on DNA resembling a replication fork.

Mark Bures
Director of Modeling & Simulations
Silicon Therapeutics

Mark is Director of Modeling and Simulations at Silicon Therapeutics, with over 30 years of experience in structure and property-based drug design. Prior to his current role, Mark was a Director of Discovery at Assembly Biosciences where he is a co-inventor of three clinical compounds targeting HBV core protein as a potential curative therapy for hepatitis B viral infection. Mark began his career in computational chemistry at Abbott Labs, where he helped develop one of the first 3D database searching tools that was used extensively in hit identification across multiple therapeutic areas. Following Abbott, Mark joined Eli Lilly and Company where he championed the use of structure-based design techniques and approaches for GPCR drug discovery, including contributing to two clinical candidates. In addition, for over 20 years, Mark has been active in fragment-based drug discovery, including leveraging biophysical techniques in hit generation and lead optimization. 

Steve Swann
Senior Director of Medicinal Chemistry & Computational Design
Silicon Therapeutics

Steve is a highly experienced medicinal chemist and molecular designer with over 10 years of project leadership experience across several therapeutic areas and a proven record of advancing molecules through early hit-to lead phases into late stage preclinical / IND enabling studies.  Throughout his career Steve has become an industry recognized expert in SBDD with extensive experience in applying computational tools to supporting new compound design and project decision making. Steve joined Silicon Therapeutics from Takeda Pharmaceuticals (San Diego, CA), where he was Associate Director of Chemistry and lead a team of 8 chemists and 2 computational scientists who supported projects across the portfolio. Prior to Takeda, he spent 6 years in the medicinal chemistry groups at Eli Lilly and Abbvie where he gained unique experience in the early stages of drug discovery including: FBDD, novel approaches to hit ID and lead optimization, efficiency metrics, as well computational modeling and SBDD across different target classes. His research experience covers gastroenterology, immuno-oncology, inflammation, and autoimmune diseases.  Steve obtained and dual B.S in Biology and Chemistry and received his PhD from the University of Delaware working for John Koh.   

Jenny Viklund
Director of Protein Science & Drug Design
Sprint Bioscience

Jenny Viklund is a Chemistry project leader for the Vps34 project at Sprint Bioscience, from fragment hit to in vivo PoC. Responsible for development of the Sprint Bioscience fragment screening platform, as well as workflows for enabling and driving drug design and data analysis.Prior to joining Sprint Bioscience, ten years as a computational chemist at AstraZeneca, Sweden. Contributor to two CNS programs that are currently in clinical trials. Education: Master of Science in Molecular Biotechnology, Uppsala, Sweden

Day Two

WEDNESDAY 18 NOVEMBER 2020

2:00 pm | Strategies for Pursuing Novel Targets using Fragment-Based Drug Discovery

Nir London
Senior Scientist
The Weizmann Institute of Science

Dr. Nir London completed his BSc magna cum laude in 2006 and his MSc in 2007, both in computer science and computational biology at the Hebrew University of Jerusalem. He completed his PhD in computational structural biology in 2011. He joined the Department of Pharmaceutical Chemistry at the University of California, San Francisco, as an EMBO post-doc fellow starting in 2012, and joined the Weizmann Institute as a senior scientist in 2015. Dr. London's lab is focused on covalent chemical biology and drug discovery and has developed several technologies for the design of covalent inhibitors. These include DOCKovalent, one of the first methods for covalent virtual screening. Electrophile fragment screening, generation of covalent analogs for known reversible ligands and the design of electrophilic peptides. His honors include the Chorev Award by the Israeli Chemical Society, the Dimitris N. Chorafas Foundation Award, a postdoctoral award from the Program for Breakthrough Biomedical Research. Most recently he also received the Alon fellowship, an award of excellence from the Israel Cancer Association and the Breast Cancer Research Foundation - AACR Career Development Award for Translational Breast Cancer Research. Recently Dr. London was selected for the IUPAC periodic table of young chemists.

Day One

TUESDAY 17 NOVEMBER 2020

9:30 am | Covalent Inhibitor Discovery by Electrophile Fragment Screening

William Pomerantz
Associate Professor of Chemistry
University of Minnesota

William C. K. 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, and was granted tenure in 2018. He is currently a McKnight Presidential Fellow.  His research focuses on the development of chemical biology and medicinal chemistry approaches for modulating protein-protein interactions. Protein-Observed Fluorine NMR (PrOF NMR) is one such tool in his lab that is being developed as a new method for fragment-based ligand discovery (FBLD), and has been applied towards inhibiting a diverse area of 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.

Day One

TUESDAY 17 NOVEMBER 2020

4:00 pm | SAR by 19F NMR: Using Protein-Observed Fluorine NMR for Targeting Epigenetic Protein Complexes