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The Industry's Preeminent Event on Novel Drug Targets ...

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R<br />

Inaugural n September 24 - 25, 2013<br />

Targeting<br />

CVT<br />

Epigenetic Readers<br />

Inhibiting Chromatin Readers - from Bromodomains to Bey<strong>on</strong>d<br />

M<br />

»»<br />

Suggested <str<strong>on</strong>g>Event</str<strong>on</strong>g> Package<br />

September 23: Biochemical and Structure-Based Approaches to<br />

Epigenetic <strong>Drug</strong> Discovery Short Course 3<br />

September 23: Characterizati<strong>on</strong> and Quantificati<strong>on</strong> of Hist<strong>on</strong>e<br />

Modificati<strong>on</strong>s Short Course 8<br />

September 24-25: Targeting Epigenetic Readers C<strong>on</strong>ference<br />

September 25-26: Next-Generati<strong>on</strong> Hist<strong>on</strong>e Deacetylase Inhibitors<br />

C<strong>on</strong>ference<br />

Tuesday, September 24<br />

7:00 am Registrati<strong>on</strong> and Morning Coffee<br />

FEATURED SESSION: LEADERS IN EPIGENETIC DRUG<br />

DISCOVERY<br />

8:10 Chairpers<strong>on</strong>’s Opening Remarks<br />

8:15 <strong>Drug</strong>ging the Epigenome<br />

Cheryl H. Arrowsmith, Ph.D., Chief Scientist, Structural Genomics C<strong>on</strong>sortium;<br />

Professor, Medical Biophysics; Canada Research Chair, StructuralProteomics,<br />

University of Tor<strong>on</strong>to<br />

9:00 <strong>Drug</strong>ging the Epigenome in Cancer<br />

Peter J. Tummino, Ph.D., Head, Biology, Cancer Epigenetics Discovery<br />

Performance Unit, Oncology R&D, GlaxoSmithKline Pharmaceuticals<br />

9:45 Grand Opening Coffee Break in the Exhibit Hall with Poster Viewing<br />

MECHANISTIC INSIGHTS INTO READER-INDUCED<br />

TUMORIGENESIS<br />

10:45 Targeting Bromodomains in NUT Midline Carcinoma<br />

Christopher A. French, M.D., Assistant Professor, Department of Pathology, Harvard<br />

Medical School; Assistant Professor, Pathology, Brigham and Women’s Hospital<br />

11:15 Sp<strong>on</strong>sored Presentati<strong>on</strong> (Opportunity Available)<br />

11:45 CHD5 and H3: A Must-Read for Tumor Suppressi<strong>on</strong><br />

Alea A. Mills, Ph.D., Professor & Team Leader, Cold Spring Harbor Laboratory<br />

12:15 pm Talk Title to be Announced (Work Currently Undisclosed)<br />

John Trzupek, Ph.D., MBA, Principal Scientist, Biotherapeutics, External<br />

Chemistry Innovati<strong>on</strong>, Pfizer<br />

12:45 Lunche<strong>on</strong> Presentati<strong>on</strong> (Sp<strong>on</strong>sorship Opportunity Available) or<br />

Lunch <strong>on</strong> Your Own<br />

PROGRESS TOWARDS NOVEL CHEMICAL READER<br />

ANTAGONISTS<br />

2:15 Chairpers<strong>on</strong>’s Opening Remarks<br />

2:20 From Epigenetic Mechanism to Targeted <str<strong>on</strong>g>The</str<strong>on</strong>g>rapy<br />

Ming-Ming Zhou, Ph.D., Harold and Golden Lamport Professor and<br />

Chairman, Department of Structural & Chemical Biology; Co-Director,<br />

Experimental<str<strong>on</strong>g>The</str<strong>on</strong>g>rapeutics Institute, Icahn School of Medicine at Mount Sinai<br />

2:50 Promoting Illiteracy: Inhibiti<strong>on</strong> of Methyl-Lysine Readers by<br />

Small Molecule Chemical Probes<br />

Lindsey Ingerman James, Ph.D., Research Assistant Professor, Center for<br />

Integrative Chemical Biology & <strong>Drug</strong> Discovery Divisi<strong>on</strong> of Chemical Biologyand<br />

Medicinal Chemistry Eshelman School of Pharmacy; Visiting Scientist,<br />

Chemical Biology, GlaxoSmithKline, Research Triangle Park<br />

3:20 Targeting Selective Inhibiti<strong>on</strong> of BET Sp<strong>on</strong>sored by<br />

Proteins by C<strong>on</strong>text Specific Engagement of Tandem<br />

Bromodomains with Cofer<strong>on</strong>s<br />

Lee Arnold, Ph.D., Vice President & CSO, Cofer<strong>on</strong> Inc.<br />

3:50 Refreshment Break in the Exhibit Hall with Poster Viewing<br />

4:30 Disrupting the Reader<br />

John M. Denu, Ph.D., Director, Epigenetics <str<strong>on</strong>g>The</str<strong>on</strong>g>me, Wisc<strong>on</strong>sin Institute<br />

for Discovery; Professor, Biomolecular Chemistry, School of Medicine and<br />

PublicHealth, University of Wisc<strong>on</strong>sin<br />

5:00 Hist<strong>on</strong>e Binding Mechanisms and Specificities of PHD Fingers<br />

Tatiana Kutateladze, Ph.D., Associate Professor, Department of Pharmacology,<br />

Anschutz Medical Campus, University of Colorado<br />

5:30 Interactive Breakout Discussi<strong>on</strong> Groups<br />

6:30 Welcome Recepti<strong>on</strong> in the Exhibit Hall with Poster Viewing<br />

7:30 Close of Day<br />

Wednesday, September 25<br />

7:30 am Registrati<strong>on</strong> and Morning Coffee<br />

THERAPEUTIC APPLICATIONS OF INHIBITING BET<br />

BROMODOMAINS<br />

8:00 Chairpers<strong>on</strong>’s Opening Remarks<br />

8:05 Targeting MYCN with BET Bromodomain Inhibitors in<br />

Neuroblastoma<br />

Kimberly Stegmaier, M.D., Associate Professor, Department of Pediatrics, Harvard<br />

Medical School; Independent Investigator, Pediatric Oncology, Dana-Farber Cancer<br />

Institute; Co-Director, Pediatric Hematologic Malignancy, Bost<strong>on</strong> Children’s Hospital<br />

& DFCI; Associate Member, Broad Institute of Harvard and MIT<br />

8:35 Bromodomain Inhibiti<strong>on</strong> as a <strong>Novel</strong> <str<strong>on</strong>g>The</str<strong>on</strong>g>rapeutic Treatment<br />

for Pulm<strong>on</strong>ary Fibrosis<br />

David C. Budd, Ph.D., H<strong>on</strong>orary Lecturer, Department of Inflammati<strong>on</strong>,<br />

Center for Rheumatology & C<strong>on</strong>nective Tissue Diseases, University College<br />

L<strong>on</strong>d<strong>on</strong>Medical School<br />

9:05 BET Proteins as Critical Links between Chr<strong>on</strong>ic Inflammati<strong>on</strong>,<br />

Insulin-Resistant Obesity and Certain Cancers<br />

Gerald V. Denis, Ph.D., Associate Professor, Cancer Research Center, Department<br />

of Pharmacology & Medicine, Bost<strong>on</strong> University School of Medicine<br />

9:35 M<strong>on</strong>itoring Inhibiti<strong>on</strong> of Bromodomain Protein Sp<strong>on</strong>sored by<br />

Interacti<strong>on</strong>s with Chromatin in Living Cells Using BRET<br />

Danette L. Daniels, Ph.D., Group Leader, Functi<strong>on</strong>al<br />

Proteomics, Promega Corporati<strong>on</strong><br />

10:05 Coffee Break in the Exhibit Hall with Poster Viewing<br />

10:50 Mechanisms of BET Bromodomain Inhibiti<strong>on</strong> in the C<strong>on</strong>trol<br />

of Gene Expressi<strong>on</strong><br />

Robert J. Sims III, Ph.D., Senior Director of Biology, C<strong>on</strong>stellati<strong>on</strong> Pharmaceuticals, Inc.<br />

11:20 Identificati<strong>on</strong> of Potent, BET Bromodomain Inhibitors for<br />

Treatment of Cancers<br />

Hosahalli Subramanya, Ph.D., Senior Vice President, Structural Biology & Lead<br />

Generati<strong>on</strong>, Aurigene Discovery Technologies, Ltd.<br />

11:50 Lunch <strong>on</strong> Your Own<br />

1:40 PLENARY KEYNOTE PRESENTATIONS<br />

See Page 3 for Details<br />

3:10-3:50 pm Refreshment Break in the Exhibit Hall with Poster Viewing<br />

3:50 Close of C<strong>on</strong>ference<br />

8 DiscoveryOnTarget.com

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