8:55 am Chair Opening Remarks
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
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
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
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
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