Web Desc
Tissue-Selective Nuclear Receptors
Organizer(s): William T. Schrader, John A. Cidlowski, Kenneth S. Korach and Donald P. McDonnell
Date: September 18 - 22, 2005
Location: Beaver Run Resort, Breckenridge, CO, USA
Sponsored by the Director's Fund
Summary of Meeting:
The nuclear hormone receptors engender great research interest, and have spawned numerous scientific meetings. The past Keystone Symposia dealt with this topic from the perspective of molecular biology. This meeting will bring together three aspects of research impacting human health via the nuclear receptors. These three groups are (a) basic scientists, (b) pharmaceutical drug discoverers and (c) clinicians. The meeting will unfold a series of questions regarding unmet medical needs for drugs involving nuclear receptor ligands, recent advances towards a molecular understanding of tissue-selectivity as a hallmark for improved safety and efficacy, and a resources workshop to address and fulfill needs for emerging novel research tools. This meeting will differ from other Keystone meetings dealing with the nuclear hormone receptor family by concentrating upon the link of molecular tools to unmet medical needs for improved therapeutics.
Scholarship Deadline: June 17 2005
Discounted Abstract Deadline: June 17 2005
Abstract Deadline: July 1 2005
Discounted Registration Deadline: July 18 2005
We gratefully acknowledge additional support for this conference from:
Novartis Institutes for BioMedical Research
We gratefully acknowledge additional in-kind support for this conference from those foregoing speaker expense reimbursements:

Boehringer Ingelheim Pharmaceuticals, Inc.

Bristol-Myers Squibb Company

Educational grant from Lilly USA, LLC

Exelixis, Inc.

GlaxoSmithKline

Ligand Pharmaceuticals

Merck Research Laboratories

Wyeth Research Labs
We gratefully acknowledge the generous grant for this conference provided by:

National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Grant No. 1R13-DK070484-01
We appreciate the organizations that provide Keystone Symposia with additional support, such as marketing and advertising:

Click here to view more of these organizations
Special thanks to the following for their support of Keystone Symposia initiatives to increase participation at this meeting by scientists from underrepresented backgrounds:

Click here to view more of these organizations

Program

Sunday, September 18 | 3:00PM - 7:30PM
Registration
Room: Foyer


Sunday, September 18 | 6:30PM - 7:30PM
Refreshments
Room: Foyer


Sunday, September 18 | 7:30PM - 9:30PM
Keynote Session: What's Wrong with Current NHR Therapies?
Room: Peaks 4-5

Speaker 1 of 2
William T. Schrader, NIEHS, National Institutes of Health, USA
Tissue-Selective Receptor Modulators: What Do We Know and What We Only Think We Know?

Sunday, September 18 | 7:30PM - 9:30PM
Keynote Session: What's Wrong with Current NHR Therapies?
Room: Peaks 4-5

Speaker 2 of 2
J. Larry Jameson, Northwestern University School of Medicine, USA
Unmet Medical Needs of NHR Therapies

Monday, September 19 | 7:00AM - 8:00AM
Breakfast
Room: Peaks 6-12


Monday, September 19 | 8:00AM - 11:00AM
Human Disease Targets for Tissue-Selective Modulators
Room: Peaks 4-5

Speaker 1 of 5
* William T. Schrader, NIEHS, National Institutes of Health, USA

Monday, September 19 | 8:00AM - 11:00AM
Human Disease Targets for Tissue-Selective Modulators
Room: Peaks 4-5

Speaker 2 of 5
William W. Chin, Harvard Medical School, USA
Selective NRH as Novel Therapeutics

Monday, September 19 | 8:00AM - 11:00AM
Human Disease Targets for Tissue-Selective Modulators
Room: Peaks 4-5

Speaker 3 of 5
John D. Baxter, University of California, San Francisco, USA
Selective Modulation of the Thyroid Hormone Receptor

Monday, September 19 | 8:00AM - 11:00AM
Human Disease Targets for Tissue-Selective Modulators
Room: Peaks 4-5

Speaker 4 of 5
Gerald H. Nabozny, Boehringer Ingelheim Inc., USA
Glucocorticoids and Inflammatory Disease

Monday, September 19 | 8:00AM - 11:00AM
Human Disease Targets for Tissue-Selective Modulators
Room: Peaks 4-5

Speaker 5 of 5
Heather A. Harris, Wyeth Pharmaceuticals, USA
Characterization and Potential Clinical Applications for Estrogen Receptor-beta Selective Agonists

Monday, September 19 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Monday, September 19 | 11:00AM - 1:00PM
Poster Setup
Room: Peaks 1-3


Monday, September 19 | 1:00PM - 10:00PM
Poster Viewing
Room: Peaks 1-3


Monday, September 19 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Monday, September 19 | 5:00PM - 7:00PM
Experimental Pharmacophores for Investigational Use
Room: Peaks 4-5

Speaker 1 of 4
* Richard Hochberg, Yale University School of Medicine, USA

Monday, September 19 | 5:00PM - 7:00PM
Experimental Pharmacophores for Investigational Use
Room: Peaks 4-5

Speaker 2 of 4
John A. Katzenellenbogen, University of Illinois at Urbana-Champaign, USA
Critical Structural Features Underlying the Activities of Nuclear Hormone Receptor Ligands

Monday, September 19 | 5:00PM - 7:00PM
Experimental Pharmacophores for Investigational Use
Room: Peaks 4-5

Speaker 3 of 4
Lawrence G. Hamann, Novartis Institutes for BioMedical Research, USA
Tissue Selective Androgen Receptor Modulators

Monday, September 19 | 5:00PM - 7:00PM
Experimental Pharmacophores for Investigational Use
Room: Peaks 4-5

Speaker 4 of 4
Richard A. Heyman, ORIC Pharmaceuticals, USA
The Intersection of Nuclear Receptors and Metabolic Syndrome

Monday, September 19 | 7:00PM - 8:00PM
Social Hour
Room: Peaks 1-3


Monday, September 19 | 7:30PM - 10:00PM
Poster Session 1
Room: Peaks 1-3


Tuesday, September 20 | 7:00AM - 8:00AM
Breakfast
Room: Peaks 6-12


Tuesday, September 20 | 8:00AM - 11:00AM
Mouse Genetic Models
Room: Peaks 4-5

Speaker 1 of 4
Günther Schütz, German Cancer Research Center, Germany
Analysis of Glucocorticoid-, Mineralocorticoid- and Estrogen-Receptor Function by Gene Targeting

Tuesday, September 20 | 8:00AM - 11:00AM
Mouse Genetic Models
Room: Peaks 4-5

Speaker 2 of 4
Adriana Maggi, University of Milan, Italy
A Mouse Reporting on ER Transcriptional Activity to Understand the Complexities of Female Physiology in Mammals

Tuesday, September 20 | 8:00AM - 11:00AM
Mouse Genetic Models
Room: Peaks 4-5

Speaker 3 of 4
* Kenneth S. Korach, NIEHS, National Institutes of Health, USA
Estrogen Receptor Pharmacology in Mouse Lines

Tuesday, September 20 | 8:00AM - 11:00AM
Mouse Genetic Models
Room: Peaks 4-5

Speaker 4 of 4
David J. Mangelsdorf, University of Texas Southwestern Medical Center, USA
The Role of LXRs and FXR in Enterohepatic Lipid Metabolism

Tuesday, September 20 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Tuesday, September 20 | 11:00AM - 1:00PM
Poster Setup
Room: Peaks 1-3


Tuesday, September 20 | 1:00PM - 10:00PM
Poster Viewing
Room: Peaks 1-3


Tuesday, September 20 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Tuesday, September 20 | 5:00PM - 7:00PM
Tissue-Selective Receptor Expression and Function
Room: Peaks 4-5

Speaker 1 of 4
* Benita S. Katzenellenbogen, University of Illinois, USA

Tuesday, September 20 | 5:00PM - 7:00PM
Tissue-Selective Receptor Expression and Function
Room: Peaks 4-5

Speaker 2 of 4
Keith R. Yamamoto, University of California, San Francisco, USA
Physiological Expression Patterns Reflect Integration of “Sectors” of Multiple Regulatory Networks

Tuesday, September 20 | 5:00PM - 7:00PM
Tissue-Selective Receptor Expression and Function
Room: Peaks 4-5

Speaker 3 of 4
John A. Cidlowski, NIEHS, National Institutes of Health, USA
The Glucocorticoid Receptor: One Gene, Many Proteins, Extensive Post Translational Modifications

Tuesday, September 20 | 5:00PM - 7:00PM
Tissue-Selective Receptor Expression and Function
Room: Peaks 4-5

Speaker 4 of 4
Richard C. Winneker, Wyeth Pharmaceuticals, USA
Tissue Selective Properties of a Novel, Nonsteroidal Progesterone Receptor Agonist, Tanaproget

Tuesday, September 20 | 7:00PM - 8:00PM
Social Hour
Room: Peaks 1-3


Tuesday, September 20 | 7:30PM - 10:00PM
Poster Session 2
Room: Peaks 1-3


Wednesday, September 21 | 7:00AM - 8:00AM
Breakfast
Room: Peaks 6-12


Wednesday, September 21 | 8:00AM - 11:00AM
Coactivator and Corepressor Proteins and the Tissue Selectiv
ity Problem

Room: Peaks 4-5

Speaker 1 of 4
* William T. Schrader, NIEHS, National Institutes of Health, USA

Wednesday, September 21 | 8:00AM - 11:00AM
Coactivator and Corepressor Proteins and the Tissue Selectiv
ity Problem

Room: Peaks 4-5

Speaker 2 of 4
Jeffrey N. Miner, Ligand Pharmaceuticals, USA
Steroid Receptor Modulators: Approaches to Selectivity for Androgen Receptor

Wednesday, September 21 | 8:00AM - 11:00AM
Coactivator and Corepressor Proteins and the Tissue Selectiv
ity Problem

Room: Peaks 4-5

Speaker 3 of 4
Bert W. O'Malley, Baylor College of Medicine, USA
Coactivators and Tissue Specific Responses to Nuclear Receptors

Wednesday, September 21 | 8:00AM - 11:00AM
Coactivator and Corepressor Proteins and the Tissue Selectiv
ity Problem

Room: Peaks 4-5

Speaker 4 of 4
Donald P. McDonnell, Duke University School of Medicine, USA
The Biological Consequences of Differential Nuclear Receptor-Cofactor Interactions

Wednesday, September 21 | 9:20AM - 9:40AM
Coffee Break
Room: Foyer


Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 1 of 9
* Donald P. McDonnell, Duke University School of Medicine, USA

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 2 of 9
Anne Minnich, Sanofi Phamaceuticals, USA
Effects of Potent and Bioavailable PPARalpha and gamma Agonists in Inflammatory Disease Models

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 3 of 9
Thomas A. Gustafson, Johnson and Johnson, USA
Metaglidasen (MBX-102), a Non-TZD Selective PPARgamma Modulator (SPPARgammaM) with Potent Anti-Diabetic and Hypo-Lipidemic Activity in the Absence of Significant Body or Heart Weight Increases

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 4 of 9
Christine Y. Ivashchenko, Sigilon Therapeutics, USA
Knockout of PPARgamma in Endothelial Cells Increases the Inflammatory Response to TNF-alpha

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 5 of 9
Jun Xia, University of Illinois at Urbana-Champaign, USA
Structural Determinants of Constitutive Androstane Receptor (CAR) Required for its Glucocorticoid Receptor Interacting Protein-1 (GRIP1)- Mediated Nuclear Accumulation

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 6 of 9
Wen Xie, University of Pittsburgh, USA
Pathway- and Gender-Specific Cross-Talk between Xenobiotic Receptors PXR and CAR

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 7 of 9
Edwin R. Sanchez, University of Toledo College of Medicine, USA
Selective Targeting of Steroid-Regulated Physiologies via TPR Co-Chaperones

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 8 of 9
Emily J. Faivre, AbbVie, Inc., USA
Liganded Human Progesterone Receptor Induces Src-Dependent Oscillations of Erk 1/2 MAPK Activity via Transactivation of the EGFR in a Breast Cancer Cell Model

Wednesday, September 21 | 2:30PM - 4:30PM
Workshop
Room: Peak 5

Speaker 9 of 9
Jacek Ostrowski, Bristol-Myers Squibb Company, USA
Chromatin Acetylation is a Potential Mechanism for the Differential Effects of Novel Non-Steroidal Ligands on Transactivation Activity of Androgen Receptor in Mouse Myoblast C2C12 Cells

Wednesday, September 21 | 4:30PM - 5:00PM
Coffee Available
Room: Foyer


Wednesday, September 21 | 5:00PM - 7:00PM
Receptor Structure and Imaging
Room: Peaks 4-5

Speaker 1 of 4
* Geoffrey L. Greene, University of Chicago, USA

Wednesday, September 21 | 5:00PM - 7:00PM
Receptor Structure and Imaging
Room: Peaks 4-5

Speaker 2 of 4
Timothy M. Willson, GlaxoSmithKline, USA
Characterization of PPAR Modulators Derived from Structure-Guided Synthesis

Wednesday, September 21 | 5:00PM - 7:00PM
Receptor Structure and Imaging
Room: Peaks 4-5

Speaker 3 of 4
Dino Moras, Institute of Genetics, Molecular and Cellular Biology, France
Structural basis for ligand (in) dependent activity of RXR

Wednesday, September 21 | 5:00PM - 7:00PM
Receptor Structure and Imaging
Room: Peaks 4-5

Speaker 4 of 4
Donald B. Defranco, University of Pittsburgh School of Medicine, USA
Role of Molecular Chaperones in Nuclear Mobility and Hormone Exchange of Glucocorticoid Receptors

Wednesday, September 21 | 7:00PM - 8:00PM
Social Hour
Room: Peaks 1-3


Wednesday, September 21 | 8:00PM - 11:00PM
Entertainment
Room: Peak 1-3


Wednesday, September 21 | 8:00PM - 11:00PM
Cash Bar
Room: Peaks 1-3


Thursday, September 22 | 10:26AM - 10:26AM
Departure


*Session Chair.