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

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C<br />

Eighth Annual n September 24 - 25, 2013<br />

GPCR-Based DTB <strong>Drug</strong> Discovery<br />

With a Focus <strong>on</strong> Allosteric Modulators<br />

T<br />

R<br />

M<br />

»»<br />

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

FGN<br />

September 23: Practical Aspects of Structure-Based <strong>Drug</strong> Discovery<br />

with GPCRs Short Course 2<br />

September 23: Allosteric Modulators of GPCRs Short Course 4<br />

September 24-25: GPCR-Based <strong>Drug</strong> Discovery C<strong>on</strong>ference<br />

September 25-26: GPCR-Targeted <str<strong>on</strong>g>The</str<strong>on</strong>g>rapies C<strong>on</strong>ference<br />

Tuesday, September 24<br />

CVT<br />

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

G PROTEIN-COUPLED RECEPTOR STRUCTURE<br />

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

8:15 Structural insights into Functi<strong>on</strong> and Pharmacology of GPCR<br />

Superfamily<br />

Vsevolod (Seva) Katritch, Ph.D., Assistant Professor, <str<strong>on</strong>g>The</str<strong>on</strong>g> Scripps Research<br />

Institute<br />

8:45 FEATURED PRESENTATION: Molecular Signatures of GPCRs<br />

Christopher Tate, Ph.D., Professor, Laboratory of Molecular Biology, MRC,<br />

United Kingdom<br />

9:15 GPCR Ligand Design via SAR-Guided Homology Models<br />

Mark Bures, Ph.D., Research Advisor, Computati<strong>on</strong>al Chemistry, Eli Lilly<br />

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

ANTIBODIES AND GPCRs<br />

10:45 Nanobodies for the Structural and Functi<strong>on</strong>al Characterizati<strong>on</strong> of<br />

GPCR Transmembrane Signaling: From Structure to Functi<strong>on</strong> to <strong>Drug</strong>s<br />

Jan Steyaert, Ph.D., Head of Department, Structural Biology, Vrije University<br />

Brussels, Belgium<br />

Sp<strong>on</strong>sored by<br />

11:15 Antibodies Against Difficult <strong>Targets</strong>: How to<br />

Tackle G-Protein Coupled Receptors<br />

Stefanie Urlinger, Ph.D., Director, Research & Development, MorphoSys AG<br />

11:45 M<strong>on</strong>ocl<strong>on</strong>al Antibodies against Endothelin A and B Human<br />

GPCR Subtypes<br />

Frederic Ducancel, Ph.D., Head, Laboratory, Institute of Biology and Technology,<br />

Saclay, Atomic Energy Commissi<strong>on</strong>, France<br />

12:15 A <strong>Novel</strong> Regulatory Role of a Humanized Anti-CCR4<br />

Antibody in Cancer Immunotherapy<br />

DeKuan Chang, Ph.D., Research Fellow, Cancer Immunology & AIDS, Dana-<br />

Farber Cancer Institute<br />

12:45 LUNCHEON PRESENTATION: New Era of GPCR Sp<strong>on</strong>sored by<br />

<strong>Drug</strong> Discovery: Multi-Pathway Screening Technologies<br />

Elizabeth R. Quinn, Ph.D., Director, LeadHunter Discovery<br />

Services, DiscoveRx Corporati<strong>on</strong><br />

LIGAND-BIASED SIGNALING<br />

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

2:20 FEATURED PRESENTATION: Allosteric Regulati<strong>on</strong> of G<br />

Protein-Coupled Receptors: Implicati<strong>on</strong>s to Functi<strong>on</strong>ally Selective<br />

Ligand Pharmacology<br />

Roger K Sunahara, Ph.D., Associate Professor, Pharmacology, University of<br />

Michigan Medical School<br />

2:50 Discovery of β-Arrestin-Biased Ag<strong>on</strong>ists of Dopamine D2<br />

Receptors<br />

Kyle Butler, Ph.D., Post-Doctoral Fellow, Laboratory of Jian Jin, Divisi<strong>on</strong> of Chemical<br />

Biology and Medicinal Chemistry,<str<strong>on</strong>g>The</str<strong>on</strong>g> University of North Carolina at Chapel Hill<br />

3:20 Sp<strong>on</strong>sored Presentati<strong>on</strong> (Opportunity Available)<br />

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

4:30 Directed Evoluti<strong>on</strong> of C<strong>on</strong>formati<strong>on</strong>ally-selective GPCR<br />

Antibodies and Applicati<strong>on</strong>s to Discovering Biased Ligands<br />

Aar<strong>on</strong> Ring, MD/PhD candidate, Laboratory of K. Christopher Garcia,<br />

Department of Structural Biology, Stanford University School of Medicine<br />

5:00 GPCR-Biased Ligands as Improved <str<strong>on</strong>g>The</str<strong>on</strong>g>rapeutics: Promise and<br />

Progress<br />

J<strong>on</strong>athan Violin, Ph.D., Director, Biology, Trevena, Inc.<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 />

NEW APPROACHES FOR ALLOSTERICS,<br />

INTERNALIZATION AND OTHER PHARMACOLOGIC<br />

CHALLENGES<br />

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

8:05 Functi<strong>on</strong>al Evaluati<strong>on</strong> of 5-HT2C Receptor Ag<strong>on</strong>ists for Obesity<br />

Dave Unett, Ph.D., Vice President, Receptor Pharmacology, Arena Pharmaceuticals<br />

8:35 Label-free Assays to Probe Ligand-Biased Signaling<br />

H<strong>on</strong>g Xin, Ph.D., Principal Scientist, CREATe Core technologies, Janssen R&D<br />

9:05 Structure of FSH and Receptor Ectodomain Complex:<br />

Relevance to the Discovery of Small Molecule Allosteric Modulators<br />

Xuliang Jiang, Ph.D., Associate Director, Structural Biology and Computati<strong>on</strong>al<br />

Chemistry, EMD Ser<strong>on</strong>o<br />

9:35 Sp<strong>on</strong>sored Presentati<strong>on</strong> (Opportunity Available)<br />

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

10:50 <str<strong>on</strong>g>The</str<strong>on</strong>g> “No Ligand Depleti<strong>on</strong>” Assumpti<strong>on</strong> Is Unnecessary and<br />

Can Be Misleading<br />

Gilles Gnacadja, Ph.D., Principal Analyst, System Informatics, Amgen<br />

11:20 Discovery of Positive Allosteric Modulators of the Mu-Opioid<br />

Receptor<br />

Neil Burford, Ph.D., Senior Research Investigator II, Lead Discovery & Profiling,<br />

Molecular Sciences and Candidate Optimizati<strong>on</strong>, Bristol-Myers Squibb Company<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 />

14 DiscoveryOnTarget.com

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