Virtual Short Courses*

Our short courses are designed to be instructional, interactive and provide in-depth information on a specific topic. They allow for one-on-one interaction and provide a great way to explain more technical aspects that would otherwise not be covered during our main presentations.

Monday, September 27, 2021   11:30 - 1:30 PM |

SC1: Chemical Biology Tools for Phenotypic Screening and Target Deconvolution

Detailed Agenda
This course is designed to provide an introduction, as well as, best practices on the use of chemical biology probes and assays that have been developed for applications in early drug discovery. Chemists and biologists working in lead generation, assay development, phenotypic screening, target discovery and deconvolution, target engagement and finding mechanism-of-action studies will all benefit from attending this course. The instructors will share their knowledge and expertise and there will be time for open discussion and exchange of ideas.

Brent Martin, PhD, Vice President, Chemical Biology, Scorpion Therapeutics

Paul Brennan, PhD, Professor, Nuffield Department of Medicine, University of Oxford

Andrew Zhang, PhD, Team Leader, Chemical Biology, AstraZeneca

INSTRUCTOR BIOGRAPHIES:

Brent Martin received his Ph.D. in Pharmacology at the University of California in San Diego, working with Nobel Laureate Professor Roger Tsien, where he developed new chemical strategies for correlated fluorescence and electron microscopy. He then carried out postdoctoral studies with Professor Benjamin Cravatt at the Scripps Research Institute developing new strategies for activity-based profiling, high-throughput screening, and chemical proteomics. As faculty member at the University of Michigan in Ann Arbor, he continued expanding the scope of activity-based profiling methods, while also establishing new bioconjugation reactions to detect and profile protein lipidation, redox modifications, and cysteine occupancy. Brent is the recipient of the NCI Howard Temin K99/R00 award in Cancer Research, the NIH Director’s New Innovator Award, and the NIGMS MIRA Established Investigator Award. He then moved to industry to lead the Chemical Biology at Janssen and is currently Vice President and Head of Chemical Biology at Scorpion Therapeutics.

Paul Brennan received his PhD in organic chemistry from the University of California, Berkeley under the mentorship of Paul Bartlett working on synthetic methodology for combinatorial chemistry and synthesizing inhibitors for new anti-bacterial targets. Following three years of post-doctoral research with Steve Ley in Cambridge University on the total synthesis of rapamycin, Paul returned to California to take a position at Amgen. His research was focused on designing and synthesizing kinase inhibitors for oncology. After two years at Amgen, Paul accepted a position as medicinal chemistry design lead at Pfizer in Sandwich, UK. Over the next six years Paul designed and synthesized compounds for most major drug classes: kinases, GPCR’s, CNS-targets, ion-channels and metabolic enzymes. In 2011 Paul joined the Structural Genomics Consortium as a principal investigator to discover chemical probes for epigenetic proteins. He is currently a Professor of Medicinal Chemistry and head of chemistry of the Alzheimer’s Research UK Oxford Drug Discovery Institute at the University of Oxford.

Andrew Zhang is a Team Leader in the Chemical Biology Department at AstraZeneca. He joined AstraZeneca in 2013 with research interests in target deconvolution, particularly using chemical proteomics and orthogonal methods for identifying target engagement events and profiling selectivity. He is now leading the proteomics efforts around profiling the selectivity and mechanism of small molecule protein degraders. Andrew trained at the interface of chemistry and molecular and cell biology, obtaining a B.S. in Chemistry and a B.A. in Molecular and Cell Biology from the University of California, Berkeley, followed by Ph.D. studies with Professor David Spiegel at Yale University around small molecule immunomodulators. Prior to joining AstraZeneca, Andrew carried out postdoctoral trainings with the Drug Discovery Group at the Ontario Institute for Cancer Research (Toronto, Canada) with Dr. Rima Al-awar.

 

SC2: DNA-Encoded Libraries

Detailed Agenda
This course will provide an introduction to DNA-encoded libraries (DEL) and how to apply them to finding new small molecule drug leads. We will cover the chemistry behind library synthesis and then discuss screening selection methods, data analysis, basic chemistry follow-up of hits. We will also compare different DEL platforms and provide a few case studies.

Svetlana Belyanskaya, PhD, Vice President, Biology, Anagenex

Ghotas Evindar, PhD, Executive Director, Drug Discovery, Exo Therapeutics

INSTRUCTOR BIOGRAPHIES:

Dr. Belyanskaya is accomplished scientific leader in the field of small molecule drug discovery and an expert in DNA encoded library platform. She was involved in the development of DEL platform for 20 years. Svetlana has made significant contributions to the design and development of the DEL technology at Praecis Pharmaceuticals and, later, at GlaxoSmithKline. She was instrumental in discovering first DEL-sourced molecule to progress into clinical trials, a potent and selective inhibitor for enzyme soluble epoxide hydrolase (hsEH). At GSK, Svetlana successfully led team of scientists on multiple scientific programs. Svetlana has deep expertise in biochemistry, molecular biology, cell biology and very passionate about future development of DEL technology with goal to find novel quality leads that bring value for the treatment of diseases with unmet medical needs

Ghotas is a senior director of drug discovery at Exo Therapeutics in Cambridge, MA. He has authored well over 50 publications and patents in the area of drug discovery and is committed to education surrounding DNA-encoded library (DEL) technology, leading a number of DEL roundtable discussions and courses over the last several years. He was born and raised in the Kurdish mountains before migrating to Canada. He completed his undergraduate and MSc degrees at the University of Waterloo, concentrating on synthesis and structure-activity studies of aureobasidins. He then joined Vertex Pharmaceuticals, in Cambridge, as a medicinal chemist. While at Vertex, he was instrumental in the success of P38 MAP Kinase (first and second generation), ICE-1 inhibitors (second generation), and early ZAP-70 programs. After four years at Vertex, and four clinical candidates, he moved to the University of Toronto to pursue a PhD degree in organic chemistry with focus on “Novel Approaches to Synthesis of Nitrogen Containing Heterocycles”. After completing his PhD with Dr. Robert Batey, he moved back to the Boston area to join Praecis Pharmaceuticals as a staff scientist. There he led the medicinal chemistry sphingosine-1-phosphate (S1P) receptor agonist discovery program and contributed to the inception of the novel DEL platform. Praecis was acquired by GlaxoSmithKline in 2007 and Ghotas began a 12-year journey with DNA-encoded library technology (ELT) platforms, including portfolio, library and selection design, data analysis and post-selection chemistry. In early 2019, Ghotas moved to Exo Therapeutics where he continues his adventures in small molecule drug discovery.

Monday, September 27, 2021   2:00 - 4:00 PM |

SC3: PROTACs and Molecular Glues for Targeted Protein Degradation

Detailed Agenda
Targeted protein degradation using molecular glues and bifunctional small molecules, known as proteolysis-targeting chimeric molecules (PROTACs), is emerging as a useful tool for drug discovery, and as a new therapeutic modality for chasing previously “undruggable” targets. This course will cover the basic understanding of what these entities are, how they work, and how they can be applied to target and degrade specific proteins of interest. Case studies drawn from the work that the instructors have done in their labs will also be presented.

Alexander Statsyuk, PhD, Assistant Professor, Department of Pharmacological and Pharmaceutical Sciences, University of Houston

Stewart Fisher, PhD, CSO, C4 Therapeutics, Inc.

INSTRUCTOR BIOGRAPHIES:

Alexander Statsyuk is an assistant professor at the University of Houston College of Pharmacy. He obtained his PhD degree at the University of Chicago in 2006, where he synthesized natural product Bistramide A and established its mode of action in cells. He then completed his postdoctoral work at UCSF, where he was working on the development of chemical cross-linkers to identify upstream kinases of protein phosphorylation sites. Since 2010 he has been running his independent research program aimed at discovering drug leads targeting degradation pathways such as ubiquitin-proteasome system and autophagy. He is an author of 32 manuscripts, he filed 10 patent applications, and he is a recipient of Pew Scholar Award. Some of the technologies that he and his group have developed and patented include covalent fragments, novel probes UbFluor to conduct HTS screens to discover E3 ligase inhibitors, activators, and hijackers, and E3-Substrate cross-linkers useful to study E3-Substrate interactions in vitro and to validate E3-Substrate hijackers in vitro.

Dr. Fisher is the Chief Scientific Officer at C4 Therapeutics, a new biotechnology company focused on the selective recruitment of targets to E3 ligases for ubiquitination and degradation by the ubitiquin/proteasome system where he is responsible for strategic delivery of the project portfolio and collaboration management. Prior to joining C4, Dr. Fisher was the Director of Enzymology and Quantitative Biochemistry in the Center for the Development of Therapeutics at the Broad Institute. His group focused on the mechanistic analysis and quantitative assessment of protein:ligand interactions required for therapeutic discovery. Prior to joining the Broad Institute, Dr. Fisher spent 15 years at AstraZeneca in the Infectious Diseases Innovative Medicines Unit, where he led numerous antibacterial programs that progressed through Phase I clinical trials and was the Executive Director, Biological Sciences. His department supported the entire drug discovery project portfolio, from target validation to pharmacodynamics modeling in support of Phase III candidates. In addition, Dr. Fisher spent 2 years at Hoffmann LaRoche leading drug discovery programs in Metabolic Diseases. Dr. Fisher received his B.A. in Chemistry at the University of Vermont and Ph.D. in Chemistry at Caltech and was a National Institutes of Health Post-Doctoral Fellow at the Harvard Medical School with Professor Christopher T. Walsh.

Monday, September 27, 2021   4:30 - 6:30 PM |

SC4: Artificial Intelligence and Machine Learning in Drug Discovery and Development

Detailed Agenda
This course aims to educate a diverse group of scientists – primarily chemists and biologists – about the growing use and applications of artificial intelligence (AI) and machine learning (ML) for early drug discovery. Starting with an overview of current challenges and opportunities, the various talks highlight how AI/ML can help with applications from target identification to clinical applications. The instructors will offer insights into the caveats and limitations of using AI/ML, which will help separate the hope from the hype. This course offers an excellent opportunity for sharing insights on key issues being discussed in the field.

Arvind Rao, PhD, Associate Professor, Department of Computational Medicine and Bioinformatics, University of Michigan

Deepak Rajpal, PhD, Head of Translational Sciences US, Sanofi

Shruthi Bharadwaj, PhD, Head, Science and Technology, Intelligence Strategic Initiatives and Scientific Relations, Sanofi

INSTRUCTOR BIOGRAPHIES:

Arvind Rao is an Associate Professor in the Department of Computational Medicine and Bioinformatics at the University of Michigan. His group uses image analysis and machine learning methods to link image-derived phenotypes with genetic data, across biological scale (i.e. single cell, tissue and radiology data). Such methods have found application in radiogenomics and drug repurposing based on phenotypic screens. Arvind received his PhD in Electrical Engineering and Bioinformatics from the University of Michigan, specializing in transcriptional genomics, and was a Lane Postdoctoral Fellow at Carnegie Mellon University, specializing in bioimage informatics.

Deepak Rajpal is the Head of Translational Sciences US at Sanofi. His group contributes to Translational Science Research across the drug discovery and development pipeline for all major therapeutic areas of interest to Sanofi. His research contributions span mutliple omics platforms and integrative analytical strategies. He is responsible for leading strategic partnerships in multiple therapy areas, internal, and also external to Sanofi, across the globe. As the US leader of the Translational Sciences research team, he has responsibilities of creating vision, and setting the strategic direction for the team in a scientifically innovative and fiscally responsible manner. He has co-authored over 45 publications, with several in high-impact journals. Additionally, Dr. Rajpal has been a member of many outreach activities to serve the communities that he has been part of.

Shruthi Bharadwaj is Head, Science and Technology, Intelligence Strategic Initiatives and Scientific Relations at Sanofi. Until recently she served as the Technical Advisor to the Chief Data and Digital Officer at Novartis. She received her PhD in Biomedical Engineering from the University of Florida and continued her research as a post-doctoral fellow at the MD Anderson Cancer Center. Shruthi has been interested and involved in utilizing AI and machine learning approaches in Pharma. She has a patent that involves machine-learning approach to predict the onset of colon cancer in patients with Inflammatory Bowel Disease. She has won several NIH grants that supported her research in leveraging AI approaches in healthcare. She has published several research articles, book chapters and abstracts that focus on AI approaches in diagnosis and drug development.