SC11: MECHANISTIC UNDERSTANDING OF PHARMACOLOGICAL PROBES FOR THE UBIQUITIN-PROTEASOME SYSTEM
TUESDAY, SEPTEMBER 25, 6:00 - 8:30 PM
Room: Fairfax


This course is intended for the audience interested in drug discovery programs aimed to develop proteolysis-targeting chimeric molecules (PROTACs) or molecular degraders, and/or small molecule inhibitors targeting components of the ubiquitin-proteasome system (UPS). The first part of the course will cover basic mechanistic biochemistry/cell biology of the ubiquitin proteasome system, which includes E1, E2, E3, and deubiquitinating enzymes, and their macromolecular architecture. Subsequently, we will discuss assays and technologies currently available for the UPS system and known enzyme inhibitors. The second part of the course will cover PROTACs and molecular glue molecules, compounds that induce proteasomal degradation of their drug targets.

Instructor:

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


Topics to be discussed:

  • Mechanisms of E1, E2, E3, and deubiquitinating enzymes (DUBs)
  • Assays and technologies, enzyme inhibitors
  • PROTACs and molecular glues

Instructor Biography:

Statsyuk_AlexanderAlexander 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 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 30 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 and molecular glues.

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