SC1: COVALENT FRAGMENTS: APPLICATIONS IN TARGET-BASED AND PHENOTYPIC SCREENS
MONDAY, APRIL 8, 10:00 AM – 1:00 PM

The course will cover the design principles of covalent fragment libraries, target-based and phenotypic screens using covalent fragments, strategies to grow fragments into drug leads, and case studies.

Topics to be covered:

• Design principles of covalent fragment libraries
• Current technologies for covalent fragment-based screens
• Examples of target-based and phenotypic screens using covalent fragments
• Strategies and considerations for growing fragments into drug leads
• Case studies of coupling covalent fragment growth with selectivity profiling in cells
• Using covalent fragments as toolkits to discover novel drug targets in phenotypic screens
• Photo-crosslinking methods to identify fragment drug targets in cells

Instructor:

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 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 vdegradation 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.