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This meeting took place in 2002



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Proteolytic Enzymes as Therapeutic Targets (B3)


Organizer(s) Robert L. Heinrikson and Jan Potempa
February 3—8, 2002
Keystone Resort • Keystone, Colorado USA
Abstract Deadline: Nov 2, 2001
Late Abstract Deadline:
Scholarship Deadline:
Early Registration Deadline: Dec 3, 2001

Sponsored in part by The Director's Sponsor Fund

Summary of Meeting:
Proteolytic enzymes play roles in almost every biological system, and they have proven to be important therapeutic targets for drug development. Inhibitors of angiotensin converting enzyme (ACE) represent a major success in benefiting sufferers of hypertension. HIV-protease inhibitors have literally changed the duration and quality of life of AIDS patients. Discoveries of new proteases continue unabated, and it remains a problem of how to develop inhibitors of these enzymes as drugs. Currently, the proteases involved in liberating the toxic Abeta peptide that accumulates in Alzheimer's Disease represent a topic of intense interest. Cysteinyl proteases such as caspases and virally encoded enzymes are also current targets with inhibitors entering clinical trials. This meeting will update, and facilitate scientific exchanges among investigators working on a spectrum of proteases that have been shown to participate in biological pathways relevant to human disease.

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No registration fees are used to fund entertainment or alcohol at this conference

Conference Program    Print  |   View meeting in 12 hr (am/pm) time


SUNDAY, FEBRUARY 3

16:00—19:00
Registration

Quandary Foyer
18:15—19:15
Welcome

Quandary Foyer
19:15—19:30
Orientation

Quandary
19:30—20:30
Keynote Address
Meeting has ended...abstracts no longer viewable online.

Quandary
Charles T. Esmon, Oklahoma Medical Research Foundation, USA
Regulation of Blood Clotting and Inflammation by the Protein C Anticoagulant Pathway


MONDAY, FEBRUARY 4

07:00—08:00
Breakfast

Castle Peak 3-4
08:00—11:00
Protease Targets in Alzheimer's Disease: New Therapeutic Perspectives
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Dennis J. Selkoe, Harvard Medical School, USA
Intramembranous Proteolysis of Notch and APP in the Genesis and Treatment of Alzheimer's Disease

Sukanto Sinha, Elan Pharmaceuticals, Inc., USA
Bace/beta-Secretase Target: Biology and Inhibition

Yong Shen, Sun Health Research Institute, USA
Short Talk: Alteration of beta-Secretase (BACE) Expression in Sporadic AD Brain

09:20—09:40
Coffee Break

Castle Peak Foyer
11:00—13:00
Poster Setup

Castle Peak 3-4
13:00—21:30
Poster Viewing

Castle Peak 3-4
14:00—16:00
Workshop 1: Aspartyl Proteinase and Approaches to AD Therapy

Castle Peak 1-2
* Dennis J. Selkoe, Harvard Medical School, USA

Yong-Tae Kim, Oklahoma Medical Research Foundation, USA
Enzymic Properties of Recombinant BACE2

Alex Loukas, George Washington University Medical Center, USA
Compatibility Between Hookworm Aspartyl Proteases and Host Hemoglobins is a Determinant of Host Range.

Hyman Engelberg, Cedars Sinai Medical Center, USA
Heparin Inhibits Proteolytic Enzymes Involved in Alzheimer's Disease Pathogenesis

16:00—16:30
Coffee & Snacks Available

Castle Peak Foyer
16:30—18:30
The Ups and Downs of Proteinase Inhibitor-Based Therapy of Viral Infections
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Ben M. Dunn, University of Florida College of Medicine, USA
Overview of Viral Peptidases as Therapeutic Targets

Peter S. Dragovich, Pfizer Global Research & Development, USA
Orally Bioavailable Human Rhinovirus 3C Protease Inhibitors

Cynthia F. Shuman, Uppsala University, Sweden
Short Talk: Studies of Drug Resistant Variants of HIV-1 Protease and Inhibitors Using Interaction Kinetic Analysis

Bret B. Beyer, University of Florida, USA
Short Talk: The Use of Chromogenic Libraries of Octapeptides to Elucidate Subsite Preference of Plasmodium Aspartic Proteinases

18:30—19:30
Welcome Mixer

Castle Peak 3-4
19:30—21:30
Poster Session 1: Aspartyl , Cysteinyl and Serine Proteases

Castle Peak 3-4

TUESDAY, FEBRUARY 5

07:00—08:00
Breakfast

Castle Peak 3-4
08:00—11:00
Caspases as Therapeutic Targets
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Nancy A. Thornberry, Kallyope, Inc., USA
Proteoses and Their Roles in Apoptosis

Guy S. Salvesen, Sanford-Burnham Medical Research Institute, USA
To Live or to Die: Regulation of Apoptosis Revealed at the Molecular Level

Mark A. Murcko, Relay Therapeutics, USA
Clinical Evaluation of an Inhibitor of Caspase 1

Sandra Moore Waugh, University of California, San Francisco, USA
Short Talk: Structural Determinants of Specificity among Proteases with High Sequence Identity and Dramatically Different Substrate Specificities

09:20—09:40
Coffee Break

Castle Peak Foyer
11:00—13:00
Poster Setup

Castle Peak 3-4
13:00—21:30
Poster Viewing

Castle Peak 3-4
14:00—16:00
Workshop 2: Cysteinyl, Serine and Metalloproteases

Castle Peak 1-2
* Robert L. Heinrikson, Pfizer Inc., USA

Fabien Lecaille, Mount Sinai School of Medicine, USA
Identification of Cathepsin K Residues Necessary for Complex Formation with Glycosaminoglycans

Nadine Hornig, Cancer Research UK, UK
Regulation of the Novel Cell Cycle Protease ‘Separase’ in Yeast

Peter J. Tummino, Janssen Pharmaceutical Companies of Johnson and Johnson, USA
Hydrolysis of Biologically Active Peptides by Human Angiotensin-Converting Enzyme-Related Carboxypeptidase (ACE2)

Wenyan Wang, Schering-Plough Research Institute, USA
The Conserved C-Terminal Threonine of Hepatitis C Virus NS3 Regulates Autoproteolysis and Ensures Proper Assembly of the NS3/NS4A Complex

Martha A. O'Brien, Promega Corporation, USA
Development of Luminescent Protease Assays

16:00—16:30
Coffee & Snacks Available

Castle Peak Foyer
16:30—18:30
Secreted Proteases in Cancer
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Lynn M. Matrisian, Vanderbilt University School of Medicine, USA
Secreted Proteinases in Cancer: The Matrix Metalloproteinase Experience

Ralph Weissleder, Massachusetts General Hospital, USA
In vivo Imaging of Protease Activity

Bonnie F. Sloane, Wayne State University School of Medicine, USA
Cell Surface Proteolysis: Contribution of Cysteine Proteases

Rainer Friedrich, Friedrich Miescher Institute for Biomedical Research, Switzerland
Short Talk: Crystal Structure of the Catalytic Domain of MTSP-1, A Type-II Transmembrane Serine Proteinase Implicated in Cancer

18:30—19:30
Welcome Mixer

Castle Peak 3-4
19:30—21:30
Poster Session 2: Metalloproteinases, Regulation and General Topics

Castle Peak 3-4

WEDNESDAY, FEBRUARY 6

07:00—08:00
Breakfast

Castle Peak 3-4
08:00—11:00
Exopeptidases
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Brian W. Matthews, University of Oregon, USA
Structure and Function of E. coli Methionine Aminopeptidases

Hans-Ulrich Demuth, Probiodrug AG, Germany
DPIV Inhibitors in Diabetes Treatment

Francesc X. Aviles, Universidad Autonoma de Barcelona, Spain
Inhibitors of Metallocarboxypeptidases. Potential Antitumor and Fibrinolytic Agents

C. Robin Ganellin, University College London, UK
Design of Butabindide, The First Inhibitor of Tripeptidyl Peptidase II

Jan Konvalinka, Institute of Organic Chemistry and Biochemistry, Czech Republic
Short Talk: Structure and Activity of Recombinant Human Glutamate Carboxypeptidase II

09:20—09:40
Coffee Break

Castle Peak Foyer
16:00—16:30
Coffee & Snacks Available

Castle Peak Foyer
16:30—19:00
Targeting Bacterial and Parasitic Proteinases
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Jan Potempa, University of Georgia, USA
Proteolytic Enzymes of Pathogenic Bacteria as Virulence Factors and Potential Targets for Drug Development

Michael A. Curtis, University of London, UK
Proteinases of Porphyromonas gingivalis as Targets for Proteinase Inhibitor-Based Treatment of Periodontal Disease

Michael N.G. James, University of Alberta, Canada
The Use of the Ascaris Pepsin Inhibitor, PI3, in the Design of Novel Peptide Inhibitors for Aspartic Proteinases

James H. McKerrow, University of California, San Diego, USA
Parasite Proteases: New Insights into the Evolution, Diversity and Function of Cysteine Proteases

Doron C. Greenbaum, University of Pennsylvania, USA
Short Talk: A Functional Proteomics Approach to Understand the Role of Cysteine Proteases in P.falciparum

17:40—18:00
Coffee Break

Castle Peak Foyer
19:00—20:00
Welcome Mixer

Castle Peak 3-4

THURSDAY, FEBRUARY 7

07:00—08:00
Breakfast

Castle Peak 3-4
08:00—11:00
Selected Aspects of Intracellular Proteolysis
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
* Donald F. Steiner, University Of Chicago, USA
Proteolytic Processing in the Secretory Pathway

Christine M. Debouck, Ardennes Biosciences LLC, USA
Application of Genomics to the Identification and Validation of Drug Targets

Frank Uhlmann, Cancer Research UK London Research Institute, UK
The Proteolytic Mechanism of Chromosome Segregation

Wolfgang P. Baumeister, Max Planck Institute of Biochemistry, Germany
The 26S Proteasome: A Supramolecular Complex Designed for Controlled Proteolysis

John W.M. Creemers, University of Leuven, Belgium
Short Talk: Identification of Physiological Substrates of Proprotein Convertases

09:20—09:40
Coffee Break

Castle Peak Foyer
16:00—16:30
Coffee & Snacks Available

Castle Peak Foyer
16:30—18:30
Challenges and Opportunities in Development of Proteinase Inhibitors as Therapeutics
Meeting has ended...abstracts no longer viewable online.

Castle Peak 1-2
Wolfram Bode, Max Planck Institut, Germany
Crystal Structures of Proteinases: Tools for the Understanding of Substrate Specificity

Edwin L. Madison, , USA
Transmembrane Serine Proteases in Cancer

Stefan Strobl, 4SC AG, Germany
Short Talk: Protein Structures - The Basis for in Silico Drug Design

18:30—19:30
Welcome Mixer

Castle Peak 3-4
19:30—22:30
Entertainment

Castle Peak 3-4

FRIDAY, FEBRUARY 8

 
Departure


*Session Chair †Invited, not yet responded.



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


National Institutes of Health

Grant No. 1 R13 AG20281-01




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