MONDAY, APRIL 2 | 6:00-9:00 PM DINNER SHORT COURSE

SC8: Introduction to the Ubiquitin Proteasome System

This course is intended for the audience interested in drug discovery programs aimed to develop PROTACS (molecular degraders) and/or small molecule inhibitors targeting components of the ubiquitin-proteasome system. This course will cover basic mechanistic biochemistry of the ubiquitin proteasome system, which includes E1, E2, E3, and deubiquitinating enzymes, and their macromolecular architecture. Subsequently the curse will transition into a general discussion of existing biochemical assays and technologies to discover PROTACS and small molecule inhibitors of E1, E2, E3, and deubiquitinating enzymes. Finally, the course will discuss existing PROTACs and pharmacological probes targeting E1, E2, E3, and deubiquitinating enzymes, their pharmacological properties, and basic control experiments that need to be done to inform a better design of pre-clinical and clinical studies.

Topics to be covered:

• Mechanisms of E1, E2, E3, and DUB enzymes
• Technologies available and experimental controls
• Discovered inhibitors and emerging biology

Instructor:

Alexander Statsyuk, Ph.D., 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 Ph.D. 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 22 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, and novel probes UbFluor to conduct HTS screens to discover E3 ligase inhibitors