Epigenetics in Drug Discovery Agenda

Registration

Chemical Probes for Epigenetic Targets
Susanne Muller Knapp, Group Head Structural Genomics Consortium (SGC), University Of Oxford, United Kingdom

Chemical probes, well-characterized, potent, selective and cell-active tool compounds, are essential tools in biology and target validation. More than 30 probes against epigenetic targets have been developed by the SGC and provided to the scientific community, which greatly accelerated research in this area.

Targeting on Epigenetic Proteins for Cancer Therapy
Jun Qi, Lead Scientist, Dana Farber Cancer Institute, United States of America

Lysine acetylation has emerged as a signalling modification of broad relevance to cellular and disease biology. Targeting acetyl-lysine recognition modules with small molecules have been successfully achieved not only in basic mechanistic understanding, but also promising in human clinic investigation.

Coffee and Networking in Exhibition Hall

Application of Super-enhancer Analysis for Drug Discovery
Christian Fritz, Vice President, Syros, United States of America

‘Super-enhancers’ regulate genes important for cell identity and cell fate. We are mapping super-enhancers in patient tumors in order to identify novel oncology targets as well as accelerate existing small molecules into the clinic.

Anti-Tumor Efficacy of BAY 1238097 In Preclinical Hematological And Solid Tumor Models
Bernard Haendler, , Bayer Healthcare, Germany

Lunch & Networking in Exhibition Hall

Poster Viewing Session

Technology Spotlight:
Tools for Epigenetic Target Based Drug Discovery – Assays for Methyltranferase/Demethylase Activity and Histone Binding by NanoBRET Technology
Craig Malcolm, Strategic Collaborations Manager, Promega UK Ltd

This technology snapshot presentation will introduce a range of novel technologies from Promega applicable drug discovery programmes for epigenetic targets.

Assays and Inhibitors for Targeting the Histone Methylome
Manfred Jung, Chemical Epigenetics Group Leader, Universität Freiburg, Germany

Reversible histone methylation is a major factor in epigenetic regulation. In this talk we will present work from our lab on assay development, screening and bioguided inhibitor optimization concerning histone demethylases and methyl lysine binding proteins, so called readers.

Coffee and Networking in Exhibition Hall

Targeting Epigenetic Reader Domains with Medicinal Chemistry and Chemical Biology
Stuart Conway, Professor, University Of Oxford, United Kingdom

Epigenetic Enzymes Regulating Macrophage Function and Inflammatory Responses
Menno de Winther, Professor, University Of Amsterdam, Netherlands

Macrophage regulation in inflammation greatly depends on epigenetic remodeling and associated epigenetic enzymes. We try to identify relevant enzymes to modulate inflammation and disease.

Drinks Reception

End of Day One

Structure-based Development of Inhibitors for Epigenetic Targets
Takashi Umehara, Unit Leader, RIKEN Center for Life Science Technologies (CLST), Japan

Structure-based development of inhibitors for the histone demethylase LSD1, and studies identifying several roles of its demethylase activity by utilizing them as chemical probes, will be presented.

Targeting DNA Methylation in Treatment of Behavioural and Mental Disorders; Lessons from Cancer
Moshe Szyf, Professor, McGill University, Canada

Alterations in DNA methylation and chromatin structure were implicated in a variety of mental disorders, pointing to the prospect of epigenetic drugs in psychiatry. We will discuss preclinical data providing evidence for efficacy of DNA methylation modulation in cocaine addiction.

Coffee and Networking in Exhibition Hall

ORY-2001 - An Epigenetic Approach to Treat Alzheimer's Disease and other Neurodegenerative Disorders
Tamara Maes, Chief Scientific Officer, Oryzon, Spain

This talk will relate the role of LSD1 in the brain and will show how the dual LSD1/MAO-B inhibitor ORY-2001 improves memory in mice models for Alzheimer's and Huntington's disease.

Chemogenomic Approaches to Spatiotemporal Regulation of HDAC Activity
Ralph Mazitschek, Assistant Professor, Broad Institute Of MIT And Harvard, United States of America

We present a novel and generalizable approach that enables high-resolution, optical control of histone deacetylases based on photochromic inhibitors using visible light. The presented compounds have high isoform selectivity and exhibit a differential activity of three orders of magnitude.

Lunch & Networking in Exhibition Hall

Poster Viewing Session

Technology Spotlight:
Chromatrap; A More efficient, Sensitive & Robust Method of Chromatin Immunoprecipitation
Amy Beynon, Product Development Manager, Chromatrap

The talk will cover aspects of Epigenetics including therapeutic potential and ChIP. Chromatrap and its filter capabilities in providing tools for epigenetic research along with the advantages and development of future assays.

Playing the System: Finding Selective Chemical Probes for Bromodomain Epigenetic Readers
Paul Bamborough, Computational Chemistry Section Head, GlaxoSmithKline, United States of America

This presentation describes examples of using structural, computational and medicinal chemistry to find potent and selective inhibitors of untargeted non-BET family bromodomains.

HDAC6 Inhibition: Getting Microtubule Transport Back on Track
Matthew Jarpe, Associate Vice President Of Biology, Acetylon Pharmaceuticals, United States of America

HDAC6 inhibition restores fast axonal transport along microtubules that is critical for neuronal health. Inhibition of HDAC6 is effective in animal models of peripheral neuropathy and neurodegenerative diseases.

Coffee and Networking in Exhibition Hall

Targeting Histone H3K36me3-deficient Cancers
Tim Humphrey, Associate Professor, University Of Oxford, United Kingdom

Loss of the histone H3K36me3 mark is frequently observed in cancer cells, suggesting this epigenetic mark as an important therapeutic target. Evidence will be presented indicating that H3K36me3-deficient cancer cells can be effectively targeted using the WEE1 inhibitor AZD1775. The underlying mechanism of this synthetic lethality and its implications will be discussed.

Follicular Lymphoma an Epigenetic Addicted Cancer
Jude Fitzgibbon, Professor, Queen Mary University Of London, United Kingdom

Mutations in histone acety (CREBBP) and methy ltransferases (KMT2D, EZH2) are present in 80% of Follicular Lymphoma tumours. Epigenetic therapies focussing on H3K4 and K27 offer promising new approaches to treatment of this incurable disease.

Close of Conference