Wednesday, August 26, 2020   11:45 - 1:45 PM |

SC8: Targeted Protein Degradation Using PROTACs, Molecular Glues, and More

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

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.

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

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.

Friday, August 28, 2020   10:00 - 12:00 PM |

SC14: Ligand-Receptor Molecular Interactions and Drug Design (LIVE ONLY)

Detailed Agenda
This course provides an overview of protein-ligand interactions and drug design principles. The presentation is targeted to medicinal chemists. Part 1 covers hydrophobic, H-bonding and electrostatic interactions; Part 2 covers specialized topics such as conformation analysis, pi-stack, cation-pi, halogen bonding, protein-protein interface, and covalent inhibition. Medicinal chemistry case studies are incorporated.

Maricel Torrent, PhD, Principal Research Scientist, Molecular Modeling, AbbVie Inc.

INSTRUCTOR BIOGRAPHY:

Maricel Torrent, PhD, Principal Research Scientist, Molecular Modeling, AbbVie Inc.

Accomplished Molecular Modeler with extensive experience in Drug Discovery. Primary strengths in Computer-Aided Drug Design – both structure-based and ligand-based – as well as data mining and analysis. Inspiring leader, sought mentor & coach, fun team player, and extremely creative co-inventor with proven results across various top 10 pharmaceutical companies – Merck, Abbott, AbbVie. Dynamic international speaker and presenter in numerous scientific conferences across the globe. Co-author of more than 80 peer-reviewed scientific articles; two book chapters.