Epigenetic dysregulation is now a hallmark of several complex pathologies, including cancer, metabolic disorders, cardiovascular and neurological diseases. Disease-specific epigenetic signatures such as DNA methylation, hydroxymethylation, and non-coding RNAs are now being utilized clinically for prognostics and diagnostics, while an expanding collection of genetically aberrant, abnormally expressed or chromatin-interacting epigenetic enzymes are positioned as promising targets for therapeutic intervention. The Clinical Epigenetics conference is designed to explore the complete landscape of clinical epigenetics - from diagnostic to therapeutic advances - highlighting the unprecedented impact of epigenetics on precision treatment and medicine.
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Monday, February 10
10:30 am Conference Program Registration
KEYNOTE SESSION: CANCER (EPI)GENOMICS
11:50 Chairperson’s Opening Remarks
12:00 pm The Cancer Epigenome
Peter A. Jones, Ph.D., D.Sc., Director, USC Norris Comprehensive Cancer Center; Distinguished Professor, Urology, Biochemistry & Molecular Biology, Keck School of Medicine, University of Southern California
Recent genome sequencing projects have revealed a surprising number of unanticipated mutations in genes which modify the epigenome. These studies have revealed a much closer interaction between the genetic and epigenetic basis of human cancer. We have begun to explore the potential effects of these mutations on the epigenome, paying particular attention to the existence and roles of chromatin accessibility in carcinogenesis. There is also excitement at the potential to use drugs to target these changes and I will discuss the effects of DNA methylation inhibitors.
12:30 Crosstalk between 5-Methylcytosine, 5-Hydroxymethylcytosine and Histone Modifications in Cancer
Gerd Pfeifer, Ph.D., Lester M. and Irene C. Finkelstein Endowed Chair, Biology & Professor, Epigenetics and Genetics of Cancer, Cancer Biology, City of Hope
Although changes of the epigenome, such as perturbation of DNA methylation patterns, are common events in human cancer, their contribution to the initiation and progression of malignant tumors has remained unclear. We have analyzed histone and DNA cytosine modifications in human cancer and normal tissue. The relationship between chromatin marks and cytosine modifications will be discussed. We propose a model in which specific epigenetic changes are shown to be important for the selection of tumor-driving events and thus may play a major role in cancer progression.
1:00 Session Break
1:15 Luncheon Presentations (Sponsorship Opportunities Available) or Lunch on Your Own
2:15 Session Break
KEYNOTE SESSION: BIOTECHS FUELING EPIGENETIC DRUG DEVELOPMENT
2:30 Chairperson’s Remarks
2:35 Talk Title to be Announced
Eric Hedrick, M.D., CMO, Epizyme
3:05 Small Molecule Inhibition of BET Protein Bromodomains: Mechanisms of Action and Potential Therapeutic Applications
Michael R. Cooper, M.D., CMO, Constellation Pharmaceuticals
Constellation and others are now developing small molecule inhibitors of BET protein bromodomains that have pharmaceutical properties suitable for clinical application. Given that the anti-tumor activity of BET inhibitors may arise from the suppression of a number of different cancer-relevant genes, the challenge will be to identify the most important determinants of anti-tumor activity in different malignancies. The presentation will review mechanistic studies of BET inhibitors and discuss potential molecularly defined disease subsets for clinical evaluation.
3:35 Early Clinical Development of OTX015, a Potent BET Bromodomain Inhibitor
Esteban Cvitkovic, M.D., Co-Founder and CSO, OncoEthix
I will present key information on the molecule and clinical formulations of OTX015, providing results from randomized, placebo-controlled trials in healthy volunteers. Also, preliminary results from ongoing dose-range finding studies in patients with relapsed/refractory hematologic malignancies will be discussed.
4:05 Sponsored Presentations (Opportunities Available)
4:35 Refreshment Break and Transition to Plenary Keynote
6:15 Grand Opening Reception in the Exhibit Hall with Poster Viewing
7:45 Close of Day
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