Pre-Conference Workshop Day

Pre-Conference Workshop Day - October 26, 2021

Our workshops are streamed so you are able to attend 3 out of 9 workshops. You can choose A, B or C followed by D, E or F, followed by G, H or I. Do you want to attend all of our workshops? Check out our group booking discounts so you can bring your colleagues!

*All times shown in EDT*

Workshop A - 8:30 am 

TPD 101 | Invigorate Your Knowledge
of Targeted Protein Degradation

With more degraders heading into the clinic than ever before and with an influx of members to the TPD community, this workshop will be your one-stop- shop to understanding targeted protein degradation to support the progression of your own research.

Receive a crash course on TPD including:

• Understanding the fundamental biology
• Discuss target selection and the existing toolbox for discovery
• Optimizing degrader design for efficient degradation
• Key discovery and development considerations

Workshop Leader:

Gwen Hansen, CSO, Nurix

Workshop B - 8:30 am

Determining the Kinetics of Small Molecule Induced Ubiquitination to Improve Drug Design

Understanding the catalytic underpinnings of protein degradation is essential for the characterization and utility of targeted protein degradation as an emerging therapeutic strategy.

Join us to discuss:

• Tools to understand and optimize catalytic properties
• Opportunities to increase selectivity and reduce off-targets
• How to optimize proximity to improve kinetics
• Current technologies to measure thermodynamics

Workshop Leaders:

Charu Chaudhry, Principal Scientist, Janssen R&D

Kristin Riching, Scientist, Promega

Rick Deibler, Senior Scientist, C4 Therapeutics 

Workshop C - 8:30 am

De-risking Clinical Development of a Novel Protein Degrader

As the field progresses towards to the first clinically approved protein degrader, there are key translational challenges that need to be overcome to successfully achieve safety and efficacy in the clinic.

Join us to discuss:

• A non-interventional study in Hidradenitis Suppurativa & Atopic Dermatitis patients to de-risk clinical development of the IRAK4 degrader KT-474
• Establishing and validating key translational biomarkers for inclusion in future clinical trials

Workshop Leader:

Alice McDonald, Director, Translational Medicine, Kymera

10:30 am | Networking & Morning Refreshments 

Workshop D - 11:00 am 

Discovery of Small Molecule Protein Degraders for the Treatment of Neurodegeneration Caused by Protein Misfolding: Huntington’s Disease as a Case Study

One of the causative agents of neurodegenerative diseases is misfolded protein aggregates, which are currently considered as undruggable. Emerging technologies for chemical protein degradation are opening up the possibility of selective elimination of target proteins through physiological protein
degradation machineries.

Join us to discuss:

• Phenotypic screening to identify protein conformation modulators: discovery of protein degraders and conformation correctors
• Characterization of small molecules using patient derived disease models and machine learning to prioritize small molecules based on efficacy and safety
• Why we chose to tackle Huntington’s disease and how we can leverage our learnings to approach other neurodegenerative diseases

Workshop Leader:

Beth Hoffman, CEO, Origami Therapeutics

Workshop E - 11:00 am

Destruction of DNA-Binding Proteins by Programmable O’PROTAC

DNA-binding proteins including transcription factors (TFs) play essential roles in gene transcription and DNA replication and repair. However, this group of proteins are generally considered undruggable as they lack an enzymatic catalytic site or a ligand
binding pocket.

Join us to discuss:

• The significance of development of PROTACs to target DNA binding proteins such as transcription factors for treatment of human diseases
• The current challenges in targeting transcription factors for degradation and function inhibition
• The conceptual and technical advances of O’PROTACs and future directions for drug development
• Future directions and potential for O’PROTACs chemical tool & drug discovery and development

Workshop Leaders:

Haojie Huang, Gordon H. & Violet Bartels Professor & Director of Basic Urologic Research, Mayo Clinic

Hong-yu Li, Arkansas Research Alliance Professor and Director of Developmental Cancer Therapeutics, University of Arkansas for Medical Sciences

Workshop F - 11:00 am

Understanding & Overcoming PROTAC Resistance in Cancer

PROTACs offer to bring new tools to the resistance arms race. However, whilst offering solutions to known inhibitor-associated mechanisms, degraders are expected to come with resistance mechanisms of their own. In this workshop we will discuss both sides of this developing picture.

Join us to discuss:

• What advantages do PROTACs offer to address inhibitor associated resistance mechanisms?
• What are likely to be the main resistance mechanisms to VHL and Cereblon based PROTACs?
• What strategies could be employed in the future to address PROTAC associated resistance mechanisms?

Workshop Leaders:

Claire Whitworth, Project Lead Scientist, University of Dundee

William Farnaby, Team Leader, University of Dundee

1:00 pm | Networking Lunch

Workshop G - 2:00 pm 

A Method for Pursuing TPD Approaches & Other Benefits Utilizing the Autophagy Pathway Compared to Ubiquitin-Proteasome Pathway

Since protein degradation become an attractive therapeutic strategy, most research and progression has focused on the UPS however this does have limitations.

Join us to discuss:

• The landscape and recent updates of autophagy receptor and AUTAC approach
• mTOR-independent autophagy activator harnessing the non-canonical autophagy pathway
• AUTAC approach using covalent binders

Workshop Leader:

Jo Hyunsun, Founder & CEO, Pin Therapeutics

Workshop H - 2:00 pm

Developing Effective & Clinically Relevant Potency Assays to Optimize Degrader Design

Current loss of signal (“down”) assays for identifying degraders often exhibit poor signal-to-noise ratios, narrow dynamic ranges, and false positives from compounds that nonspecifically suppress transcription or translation.

Join us to discuss:

• How is degradation actually measured?
• How to profile PROTACs
• How to develop reproducible, accurate, robust, stability- indicating and practical potency assays for assessing protein degrader potency
• What are the best assays available to detect clinical potency of protein degraders?

Workshop Leaders:

Matthew Oser, Assistant Professor of Medicine, Harvard Medical School

Vidyasagar Koudri, Oncologist, Dana-Farber Cancer Institute

Workshop I - 2:00 pm

Novel Applications & Drug Delivery Aspects of Proteolysis Targeting Chimera

Being relatively large molecules, PROTACs are challenging to deliver to the tumor target site and formulation must be taken into consideration

Join us to discuss:

• BRD4 and EGFR targeting PROTAC for the treatment of various solid tumor
• Drug delivery limitations of PROTAC class of molecules
• Translational formulation approach and studies in human tumor xenograft study

Workshop Leader:

Ketankumar Patel, Associate Professor of Pharmaceutics, St John’s University, NY