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Previous Webinar

Targeting Deubiquitinases for Therapeutic Benefit

September 20, 2022, 10:00 am EDT / 4:00 pm CEST

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Program

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

Headshot of Ingrid Wertz

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.

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Headshot of Sara Buhrlage

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. 

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Headshot of Anthony Varca

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.

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