*All times shown in EST

9:20 am Chair’s Opening Remarks

Epigenetic Targets: From Familiar to Novel

9:30 am Panel Discussion – HDAC3, BET, RNA, So Many Targets – Exploring New Potential in Well Known Targets to Create New Value & Diversify Pipelines

  • Thomas Paul Senior Director, Epigenetics Research, Pfizer
  • Xuedong Liu Professor, Department of Biochemistry, University of Colorado-Boulder and Co-Founder and SAB, OnKure Inc.
  • Robert Soliva Head of Drug Discovery, Oryzon Genomics

Synopsis

  • Discuss disease positioning and the importance of this in creating value out of your existing IP
  • Highlight the criteria you should consider before exploring a new therapeutic area
  • Explore current examples of therapeutics that have been reused in this way
  • How can this potential be capitalized on for both oncological and non-oncological indications? Dr. Nikhil

10:00 am Targeting Histone H2AThr120 Phosphorylation in Colon Cancer

  • Nikhil Ghate Postdoctoral Research Associate , University of Southern California

Synopsis

  • Evaluate how VprBP is highly expressed in colon cancer and how the level of histone H2Athr120 phosphorylation is correlated with expression of VprBP
  • VprBP is a kinase responsible to phosphorylate histone H2AThr120 in colon cancer
  • Identify how VprBP kinase inhibitor (B32B3) inhibits the growth of colon cancer cells in vitro and in vivo

10:30 am Virtual Speed Networking & Morning Networking Break

11:00 am From Mechanism of Action to Biomarker Discovery – how chromatin landscape informs the drug discovery process.

Synopsis

Biology happens in 3D, are you looking in the right dimension?

During this presentation you will learn about…

  • How chromatin topology can inform disease mechanisms of action
  • Insights into drug response by capturing the 3-D gene regulatory landscape
  • The latest tools for capturing genome-wide and targeted chromatin topology
  • Enhancing bio-marker discoveries with genome topology

11:10 am Precision Epigenetic Therapy for Blood Cancers

  • Ari Melnick Professor, Weill Cornell - Cornell University

Synopsis

  • Understand what constitutes an epigenetic mechanism that drives cancer
  • Understand what constitutes a genuine epigenetic therapy vs targeting general
  • Define the kinds of biomarkers that are useful to guide precision deployment of epigenetic therapies

11:40 am Next generation genomic mapping with CUTANA CUT&RUN

Synopsis

  • Successor technology to Chromatin ImmunoPrecipitation (ChIP)
  • Dramatically reduced (>10x) sample and sequencing depth requirements
  • Broad target compatibility (e.g. histone modifications, transcription factors, ATPases)
  • Reliable, cost-effective workflow
  • Automated 96-well plate format dramatically increases throughput

11:50 am “Breaking” a lncRNA-Protein Complex as a Novel Approach to Target Cancer Metabolism

Synopsis

  • LncRNA-protein interaction and epigenetic regulation
  • Topological analysis for the design of inhibitors
  • Therapeutic effects of LncRNA-protein complex disruption

Carrying Out Studies with Robust Trial Design, Planning & Execution

12:20 pm Lunch Networking Break

12:50 pm Leverage the spatial properties of the genome to discover translational markers towards novel diagnostics, therapies and treatments.

  • Ibrahim Jivanjee Director of Product Management and Marketing , Arima Genomics, Inc

Synopsis

  • Characterize disease subtypes by illuminating the mechanisms behind genetic disease
  • Identify new therapeutic targets by looking beyond the flat genome
  • Measure therapeutic response by assessing the impact of a drug on the regulatory landscape
  • A scalable platform that carries you from discovery to validation and screening

1:00 pm OKI-179, an Oral Class 1-selective Depsipeptide HDAC Inhibitor: Phase 1 Results & Phase 2 Plans

  • James Winkler Vice President - Biology & Translational Medicine, OnKure Inc.

Synopsis

  • OKI-179 is an oral depsipeptide HDAC Class 1 inhibitor, the same class as the IV drug romidepsin
  • Demonstrating how OKI-179 has completed Phase 1 with excellent PK, PD and safety
  • Discussing a molecular approach to Phase 2 trials

1:30 pm A Novel CBP/p300 Inhibitor for the Treatment of AR-driven Cancers

  • Sylvie Guichard Senior Director - Translational Science & Biology, Forma Therapeutics

Synopsis

  • Presenting a novel CBP/p300 inhibitor which antagonizes AR signalling
  • Analyzing the efficacy of the drug in several models of AR-driven tumors in vitro and in vivo
  • It is currently in Ph1 clinical trial in prostate cancer

2:00 pm Presentation from Arpeggio

2:10 pm Afternoon Networking Break

2:30 pm Molecular Correlates of Response to TAZVERIK®: the Value of Translational Studies

  • Neil Michaud Senior Director of Translational Medicine , Epizyme, Inc.

Synopsis

• Companion Diagnostic use to stratify subjects according to EZH2
mutation status in NHL
• Molecular analysis reveals pharmacodynamics of epigenetic inhibition
and correlates of response
• Tumor microenvironment changes post EZH2 inhibition

Start Strong with Meaningful Preclinical Research

3:00 pm Discovery of a First-in-Class KAT6A/KAT6B Inhibitor CTX-648 (PF-9363) with Potent Anti-Tumor Activity in ER+ Breast Cancer with KAT6A Dysregulation

  • Thomas Paul Senior Director, Epigenetics Research, Pfizer

Synopsis

  • Molecular dysregulation of KAT6A has been observed in several cancers, including amplifications in breast, lung, ovarian cancer along with oncogenic fusions in AML
  • CTx-648 (PF-9363) is a first-in-class potent KAT6A/KAT6B inhibitor that possess high selectivity versus other MYST family members (KAT7, KAT5, KAT8)
  • CTx-648 (PF-9363) inhibits expression of ESR1 expression leading to potent anti-tumor activity in ER+ breast cancer models

3:30 pm Targeting FET-Rearranged Sarcomas Through Inhibition of LSD1

Synopsis

  • Understanding the scaffolding function of LSD1
  • Highlighting the seclidemstat mediated inhibition of LSD1 proteinprotein interactions
  • Evaluating the in vitro activity of seclidemstat in FET-rearranged sarcomas

4:00 pm Noncoding RNA & Epigenetics in Animal Health

Synopsis

  • Demonstrating how host-virus interaction and epigenetics regulation with ncRNA are orchestrated together in Marek’s Disease process
  • Recently, we also found the chromatin structure, alleles, and epi-alleles as biomarkers actively involved in the process that modify responses to MDV infection
  • Interestingly, epigenetic manipulation controlling the virus loads paves a feasible way to improve animal health and welfare