SC8: TARGETED PROTEIN DEGRADATION USING PROTACs, MOLECULAR GLUES, AND MORE

MONDAY, AUGUST 24 | 6:00 - 9:00 PM (DINNER PROVIDED)

Targeted protein degradation using molecular glues and bifunctional small molecules known as proteolysis-targeting chimeric molecules (PROTACs) are 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. Instructors will give short presentations and there will be more time for discussion-based learning to tackle some of the topics listed below.

Topics to be Covered:

• Pros and cons of using PROTACs versus molecular glues
• PROTACs and molecular glues: Do we use them to induce protein degradation only?
• Molecular events required for PROTAC-mediated degradation
• New screening technologies available to discover PROTAC and molecular glues for E3 ligases
• Applying enzymology concepts to the optimization of targeted protein degraders
• Protein degradation beyond bi-functional degraders
• Pursuing previously undruggable protein targets
• Issues surrounding PK/PD, biotransformation and in vivo delivery

Instructors:

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.

Chandrasekhar Abbineni, PhD, Senior Group Leader, Aurigene Discovery Technologies Limited

Dr. Chandrasekhar is a medicinal chemist with experience spanning 20 years at Aurigene Discovery Technologies and Dr. Reddy’s laboratories Ltd. He has obtained his PhD in synthetic organic chemistry from JNTU, India. He has successfully led several Hit2Lead, Lead optimization, precandidate and candidate nomination campaigns in metabolic disorders and oncology therapeutic areas. He is co-inventor of a clinical candidate in phase I/II for CRPC and co-authored several publications and patents.

Tauseef Butt, PhD, President and CEO, Progenra, Inc.

Dr. Tauseef R. Butt is the President and CEO of Progenra. Dr Butt obtained his PhD degree in Molecular Biology from The University of Glasgow, Scotland. He was a Staff Fellow at the National Institutes of Health, Bethesda, MD, before joining SmithKline Beckman (now GSK) Pharmaceuticals. He was Assistant Director in Research and Development at SmithKline. He also served as Adjunct Professor Biochemistry and Biophysics, University of Pennsylvania Medical School, Philadelphia (1989-2000). He has published over 100 papers in life sciences research. Dr. Butt serves as an Adjunct Professor in Biomedical Engineering at Drexel University, Philadelphia and is active in a number of national and regional professional organizations, including several dedicated to biotechnology.

Additional Instructors to be Announced

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