Conference Day 1

Day One

Wednesday, April 27

Day Two

Thursday, April 28

All times in EDT

8:30 am Registration Opens & Welcome Coffee

8:50 am Chair’s Opening Remarks

Identifying & Validating Valuable Undiscovered or Unexploited Ligases

9:00 am Enabling New E3 Ubiquitin Ligases for Targeted Protein Degradation

  • Ryan Potts Head of Induced Proximity Platform, Amgen

Synopsis

  • New approach to evaluate E3 ubiquitin ligases for targeted protein degradation
  • Tackling discovery of small molecule ligands for E3 ubiquitin ligases
  • An update on our progress to expanding the toolbox of E3 ubiquitin ligases for targeted protein degradation

9:25 am Arvinas’ PROTAC® Discovery Engine: Selecting & Employing E3 ligases for PROTACs

Synopsis

  • Overview of Arvinas’ PROTAC portfolio and PROTAC Discovery Engine platform
  • Employing E3 ligases at Arvinas
  • Mechanistic understanding of a new E3 ligase employed for PROTAC

9:50 am Strategies to Identify Novel E3 Ubiquitin Ligases for Targeted Protein Degradation

Synopsis

  • Screening approaches to Identify new E3 Ligase Binders
  • Hit confirmation and follow up studies
  • Proof of concept studies using identified E3 Ligase Binders

10:15 am NanoBRET Target Engagement: A Best-In-Class Method to Quantify PROTAC Permeability

Synopsis

• A novel application of NanoBRET target Engagement to determine cellular:
• Potency via cell based competition assays
• ntracellular availability by comparing compound activity in in-tact and gently lysed cells
• Permeability by using target engagement to measure the rate of equilibration across the cell membrane

10:40 am Live Panel Q&A – Ask the Speakers Your Burning Questions

11:00 am Morning Break & Structured Networking

Optimizing Tissue & Disease Specific Ligase Targeting Therapeutics

12:00 pm Drugging Tissue Restricted E3 Ligases for TPD-based Precision Medicine

  • Hakryul Jo Associate Director, Platform Biology, Kymera Therapeutics

Synopsis

  • Roles of different types of E3 ligases
  • Promises and challenges of exploiting tissue restricted E3 ligases
  • Strategies to prioritize novel E3 ligases for TPD application

12:25 pm Roles of Cullin Ring Ubiquitin Ligases (CRL’s) In the Pathogenesis of Brain Cancers

Synopsis

  • Overview of the CRLs complexes investigated in my laboratory
  • Novel aspects of CRLs regulation
  • Potential for drug development in this class of E3s

12:50 pm Role of Cullin-RING Ligases in Malignant Hematopoiesis

  • Luca Busino Assistant Professor in Cancer Biology, University of Pennsylvania

Synopsis

  • Tumor suppressive Cullin Ring Ligases
  • B-cell lymphoma
  • Notch signaling

1:15 pm Live Panel Q&A – Ask the Speakers Your Burning Questions

1:30 pm Lunch & Networking Break

2:30 pm Roundtable Session: Tissue & Cell Selectivity – Highlighting the Potential for Selective E3 Targeting

  • Jennifer Johnston Chief Executive Officer, NysnoBio
  • Vincenzo D’Angiolella Associate Professor, University of Oxford
  • Dan Robbins Associate Director, Medicinal Chemistry, Nurix Therapeutics
  • Wei Zhang Assistant Professor, University of Guelph
  • Satpal Virdee MRC Investigator & Professor of Chemical Biology, MRC Protein Phosphorylation & Ubiquitylation Unit, University of Dundee

Synopsis

  • As expression and profiling data begin to shed light on the distribution of E3’s across cell and tissue types, it is becoming evident that such data may provide promising insights to aid the development of tissue E3 specific targeting, within a therapeutic context.
  • What is the difficulty of selectively targeting E3’s in tumor cells and tissue types of interest?
  • How specific degradation can be induced within a specific tissue type, avoiding cross effects around the body?
  • What is the importance and use of expression data for our understanding and insight to develop tissue and cell specific E3 therapeutic?

3:15 pm Afternoon Break & Refreshments

Harnessing Structural Identification of Ligand &Linker Binder to Guide E3 Targeting Drug Development

3:45 pm Approaches to Find Molecular Glue Degrader Using Novel E3 Ligase Binder

  • Hyunsun Jo Founder & Chief Executive Officer, Pin Therapeutics

Synopsis

  • Novel E3 ligase hit finding strategy
  • Biological validation of E3 ligase binder
  • Approach to find a molecular glue degrader

4:10 pm Discovery of FHD-609: A Potent & Selective IV Administered Heterobifunctional Degrader of BRD9 in Phase 1 Clinical Trials

  • Qianhe Zhou Principal Scientist, Foghorn Therapeutics

Synopsis

  • Introduction to Foghorn Therapeutics and discovery platforms
  • Synovial Sarcoma and rational of degrading BRD9 in Synovial Sarcoma
  • Preclinical in vitro and in vivo data of FHD-609 in Synovial Sarcoma models

4:35 pm The Discovery of Oral PROTAC’s for Prostate Cancer: HP518 & Beyond

  • Wu Du Senior Vice President, Hinova Pharmaceuticals

Synopsis

  • Prostate cancer remains an unmet medical need and PROTAC’s targeting AR provides a new approach to meet this need
  • Hinova discovered an oral AR PROTAC HP518 for clinical development
  • Progress on dual targeting oral PROAC’s

5:00 pm Live Panel Q&A – Ask the Speakers Your Burning Questions

  • Corey Strickland Vice President Molecular Technology, Proteovant
  • Hyunsun Jo Founder & Chief Executive Officer, Pin Therapeutics
  • Qianhe Zhou Principal Scientist, Foghorn Therapeutics
  • Wu Du Senior Vice President, Hinova Pharmaceuticals

5:15 pm Chair’s Closing Remarks & End of Conference Day One

Day Two
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