Previous Webinar
Targeting Deubiquitinases for Therapeutic Benefit
September 20, 2022, 10:00 am EDT / 4:00 pm CEST
Watch WebinarProgram
Host and moderator: Ingrid Wertz, Bristol Myers Squibb
10 min
|
Ingrid Wertz, Bristol Myers Squibb
|
Introducing Deubiquitinases
|
40 min
|
Sara Buhrlage & Anthony Varca, Dana-Farber Cancer Institute
|
Targeting Deubiquitinases for Therapeutic Benefit
|
10 min
|
Moderated by Ingrid Wertz
|
Audience Q&A
|
Abstract
Co-opting the Ubiquitin/Proteasome System is an emerging therapeutic strategy, as demonstrated by Cereblon E3 Ligase Modifying Drugs (CELMoDs), Selective Estrogen Receptor Degraders (SERDs), and heterobifunctional degraders in the clinic. Deubiquitinases (DUBs) are a class of proteases that disassemble ubiquitin chains and remove ubiquitin moieties from target proteins. We will discuss strategies for targeting deubiqutinases, with an emphasis on achieving potency and specificity to achieve maximal therapeutic benefit.
BIO SKETCHES
Ingrid Wertz (Bristol Myers Squibb)
Ingrid Wertz is the executive director of Protein Homeostasis Center of Excellence at BMS. She and her team are responsible for developing protein degrader medicines for patients in need by harnessing degradation systems naturally present within the human body. Their aim is to specifically target and eliminate disease-relevant proteins that have been largely undruggable. Prior to joining Bristol Myers Squibb, Ingrid was a principal scientist in the departments of Discovery Oncology and Early Discovery Biochemistry at Genentech, where she led the company’s degrader platform aimed at co-opting ubiquitin system enzymes for therapeutic benefit.
Sara Buhrlage (Dana-Farber Cancer Institute)
Sara Buhrlage is heading a cancer chemical biology lab at the DFCI. Her lab has established an integrated DUB-focused platform comprised of DUB-targeted libraries with novel scaffolds and chemotypes and a suite of established and novel biochemical and chemoproteomic assays that has accelerated development of selective probes and annotation of function and translational potential for multiple DUBs. The group is now building on these successes to generate a deep bench of inhibitor focused projects as well as expanding the platform through innovation in DUB ligand mechanisms of action and DUB-focused technologies.
Anthony Varca (Dana-Farber Cancer Institute)
Anthony Varca just graduated from the Harvard Chemical Biology PhD program, where he worked in the Buhrlage lab. His research has focused on the design and implementation of a high-throughput screen and orthogonal validation assays towards the identification of selective small molecule DUB inhibitors. Subsequent work has focused on the optimization of screening hits into small molecule probe compounds for studying DUBs' function and role in disease.