8:55 am Chair Opening Remarks

  • Isaac Klein Chief Scientific Officer, Dewpoint Therapeutics

9:00 am PANEL DISCUSSION: 2022 & Beyond: Where Do We See the Epigenetics Drug Discovery & Development Landscape Over the Next 5 Years?

Synopsis

  • Outlining the successes of the past year in epigenetics drug development
  • Reviewing novel approaches to targeting epigenetic regulators to diversify your pipeline
  • Shedding light on the need to explore novel translational applications for epigenetic drugs to enter new indications

Harnessing Technology to Better Understand Gene Expression

9:45 am Identifying Novel Targets for Epigenetic Drug Discovery & Development to Accelerate Pipeline Decision Making

Synopsis

  • Developing new understanding of SETD2 in multiple myeloma and DLBCL
  • Acquiring awareness of novel targets and the potential for new inhibitor development

10:15 am Improvements to ChIP-seq by Using Automation & Spike-in Normalization Approaches

  • Alon Goren Assistant Professor, University of San Diego California (UCSD)

Synopsis

  • Building and improving assays to better understand the relationship between chromatin structure and regulation of gene expression and other phenotypes
  • Capitalizing on this understanding of mechanisms that is associated with gene expression to enhance target identification and activity

10:45 am
Morning Break & Structured Networking Session

Pinpointing Novel Targets & Concepts for Target & Drug Discovery

11:15 am SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

Synopsis

  • PF-06939999 is a potent and selective S-adenosyl methionine competitive inhibitor of PRMT5 being explored in solid tumor tumors in a phase 1 study
  • PRMT5 inhibition by PF-06939999 treatment reduced the in vitro and in vivo proliferation of NSCLC cancer cells, with dose-dependent decreases in symmetric dimethyl arginine (SDMA) levels and changes in alternative splicing of numerous pre-mRNAs.
  • Analysis of sensitivity to the inhibitor, across a panel of NSCLC cell lines, identified mutations in the splicing factor RBM10 that could be used as a predictive biomarker of response
  • Models of acquired drug resistance to SAM-competitive and peptidecompetitive PRMT5 inhibitors identified mutations in the PRMT5 enzyme unique to the binding mode for each compound and highlighted SAM- competitive inhibitors have less susceptibly to complete drug resistance.

11:45 am Exploring the Discovery & Development of an Oral Trispecific Cancer Drug

  • Claes Wahlestedt Associate Dean & Center Director for Therapeutic Innovation; Chief Scientific Officer, University of Miami Miller School of Medicine; Epigenetix

Synopsis

  • Developing new understanding of existing targets and their functions
  • Acquiring awareness of novel targets and the potential for new inhibitor development
  • Combining multiple cancer fighting properties in one drug and advancing clinical biomarker utility in the epigenetic space

12:15 pm
Lunch & Networking

1:15 pm Leveraging CRISPR: Identification of Essential Proliferation & Trametinib Resistance Mechanisms in Uveal Melanoma

Synopsis

  • Leveraging CRISPR to identify novel genetic dependencies
  • Validation of CRISPR screening hits
  • Using CRISPR screening results to guide pharmacological targeting of essential mechanisms

1:45 pm Detailing the Opportunities for Epigenetic Drug Discovery & Development in CNS Tumors to Inform Pipeline Decision Making

  • Kirk Tanner Chief Scientific Officer, National Brain Tumor Society

Synopsis

  • Glioblastoma is one of the first tumors where a single epigenetic modification, the methylation of the MGMT gene, was found to be of clinical relevance
  • Cataloguing the additional alterations (IDH1/2 mutations and histone 3 variants) that either interfere with epigenetic modifier enzymes or alter alter global H3K27me3 levels
  • Overviewing the landscape of opportunities for therapeutic targeting of epigenetic drivers in CNS tumors

2:15 pm
Afternoon Break & Networking

2:45 pm Developing Small-Molecule Drugs for Epigenetic Treatments of Psychiatric Disorders

Synopsis

  • Rationalizing the use of small-molecule compounds to target metabolicepigenetic pathways in the brain
  • Blocking a metabolic enzyme controls the epigenetic encoding of maladaptive memory
  • Preclinical models to develop epigenetic therapeutics for neuropsychiatric disorders

3:15 pm Spearheading CRISPR/Cas9 Screening to Identity Genes Necessary for LSD1 to Maintain the Neuroendocrine Identify of Small Cell Lung Cancer

  • Matthew Oser Assistant Professor of Medicine Dana Farber Cancer Institute, Harvard Medical School

Synopsis

  • Leveraging genome-wide CRISPR/Cas9 screening to identify key targets of LSD1
  • Identifying key regulators of neuroendocrine cell state
  • Highlighting cell state plasticity to unmask immunogenicity

3:20 pm End of Day One

3:45 pm Roundtable Discussion: Improving Cross-functional Collaboration in Biopharma

Synopsis

  • Exploring current shortcomings within functional workplace collaboration and cross-industry relationships
  • Brainstorming novel routes to elevating cross-functional relationships

4:15 pm Chair’s Closing Remarks