Gordon Research Conferences
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Conference Program
 
High Throughput Chemistry & Chemical Biology
June 20-25, 2010
Les Diablerets Conference Center
Les Diablerets, Switzerland
Chair:
Michael A. Foley

Vice Chair:
Roland E. Dolle

Dear Colleagues,

The 2010 High Throughput Chemistry and Chemical Biology Gordon Research Conference will be held June 20 – 25 at the Les Diablerets Conference Center in Les Diablerets, Switzerland. This year’s vice chair is Dr. Roland Dolle, of Adolor Corporation. High throughput chemistry and chemical biology is a dynamic, rapidly evolving field that has an important role in molecular probe development and drug discovery.

The high throughput chemistry and chemical biology community has contributed significantly to the evolution of the drug discovery process with the major emphasis in the field evolving towards methods to accelerate lead generation/ lead optimization, focused parallel synthesis, high throughput technology, and chemical biology. This year’s program will feature cutting edge talks bridging the disciplines of organic synthesis, catalysis, medicinal chemistry, and chemical biology as applied towards high speed synthesis, parallel chemistry approaches, rapid generation of structure activity relationships to accelerate drug discovery, and the discovery of small molecule probes to study the role of newly discovered protein targets and molecular pathways in disease initiation and progression.

Feedback from monitors and attendee self-evaluation has given this meeting an excellent rating. A review of the 2009 program will give you an idea of the range of topics typically covered. Participants are encouraged to present posters. The 2009 poster winners; Sueng Bum Park, Seoul National University; Berengere Sauvagant, Schering-Plough; and Rolf Breinbaer; Institute of Organic Chemistry, Tu Graz, Austria, will be presenting talks this year.

High Throughput Chemistry and Chemical Biology will continue the tradition of excellent science in a relaxed atmosphere. I would like to encourage the application and attendance of scientists from diverse backgrounds and experiences, including women, minorities, graduate students, post docs, academic, and industrial researchers to the Conference. Continued corporate support in terms of leading edge talks, conference attendance, and financial backing is essential to insure that High Throughput Chemistry and Chemical Biology continues to meet the needs of the drug discovery and probe development community in the future. I look forward to an outstanding conference in 2010 and thank you for your support and interest.

Michael A. Foley, Ph.D.
Chair 2010
GRC High throughput Chemistry and Chemical Biology
Broad Institute of MIT and Harvard University


Contributors

SUNDAY
4:00 pm - 8:00 pmArrival and Check-in (Check-in Desk Closed 6:00 pm - 7:45 pm)
6:00 pmDinner
7:30 pm - 7:40 pmWelcome / Introductory Comments by GRC Site Staff
7:40 pm - 9:30 pmFrontiers in Drug Discovery
Discussion Leader: Lisa Marcaurelle (Broad Institute)
7:40 pm - 8:20 pm James Wells (UCSF)
"Turning Enzymes ON with Small Molecules"
8:20 pm - 8:35 pm Discussion
8:35 pm - 9:15 pmRobert Gould (Epizyme)
"Epigenetics: The Present and Future of Cancer Therapeutics"
9:15 pm - 9:30 pm Discussion
MONDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHit to Lead / Medicinal Chemistry
Discussion Leader: Craig Lindsley (Vanderbilt University)
9:00 am - 9:20 amSamuel Gerritz (Bristol-Myers Squibb)
"The Discovery and In Vitro Optimization of a Novel Class of PTPgamma Inhibitors"
9:20 am - 9:30 am Discussion
9:30 am - 9:50 amScott Sutton (Pfizer)
"Parallel Synthesis and Metabolite Indentification of Phenol Containing HSP90 Inhibitors"
9:50 am - 10:00 am Discussion
10:00 am - 10:30 am Coffee Break
10:30 am - 11:00 amJurgen Dinges (Abbott)
"Hit-to-Lead Efforts Towards Novel EP1 Inhibitors for Pain Modulation"
11:00 am - 11:10 am Discussion
11:10 am - 11:40 amGebhard Thoma (Novartis)
"Hit-to-Lead Chemistry on Chemokine Receptor Antagonists: Inhibitors of CXCR3 and CXCR4 in Transplantation"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pmPeter Hamley (Sanofi-Aventis)
"Accelerated Drug Discovery through High Throughput Chemistry"
12:20 pm - 12:30 pm Discussion
12:30 pmGroup Photo / Lunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 5:30 pmPoster Session I
5:30 pm - 7:30 pmChemical Biology
Discussion Leader: Angela Koehler (Broad Institute)
5:30 pm - 6:20 pmClifton Barry (NIH)
"High-Throughput Approaches to Understanding Vulnerabilities in the Metabolism of Mycobacterium Tuberculosis"
6:20 pm - 6:30 pm Discussion
6:30 pm - 7:15 pmLisa Marcaurelle (Broad Institute)
"Building a Unique Compound Collection through Diversity-Oriented Synthesis: It's All About Stereochemistry!"
7:15 pm - 7:30 pm Discussion
8:00 pmDinner
TUESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmHigh Throughput Technologies
Discussion Leader: Samuel Gerritz (Bristol-Myers Squibb)
9:00 am - 9:20 amWolfgang Klute (Pfizer)
"Learning More from Libraries: Monomer and Reaction Success"
9:20 am - 9:30 am Discussion
9:30 am - 9:50 amKenneth Bair (Forma Therapeutics)
"Adventures with CS Mapping"
9:50 am - 10:00 am Discussion
10:00 am - 10:30 am Coffee Break
10:30 am - 11:00 amMichael Naesby (Evolva Inc.)
"Genetic Chemistry - A Synthetic Biology Platform for the Discovery of "Unnatural" Natural Compounds and their Directed Evolution"
11:00 am - 11:10 am Discussion
11:10 am - 11:40 amAngela Koehler (Broad Institute)
"Tackling Challenging Targets with Small-Molecule Microarrays"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pmDaniel Varon Silva (Max Plank)
"Automated Oligosaccharide Synthesis: A High Throughput Method for the Synthesis of GPI-Anchored Proteins and Glycoproteins"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 5:30 pmFree Time
5:30 pm - 7:30 pmChemical Biology
Discussion Leader: Paul Hanson (Kansas University)
5:30 pm - 6:20 pm Craig Lindsley (Vanderbilt University)
"Molecular Switches' on Allosteric Ligands that Modulate Modes of Pharmacology"
6:20 pm - 6:30 pm Discussion
6:30 pm - 7:20 pm Allen Annis (Aileron)
"High-Throughput Discovery and Characterization of Protein-Ligand Interactions by Affinity Selection-Mass Spectrometry"
7:20 pm - 7:30 pm Discussion
8:00 pmDinner
WEDNESDAY
7:30 am - 8:30 amBreakfast
9:00 am - 12:30 pmChemical Methodology and Library Development
Discussion Leader: Ann Rowley (Broad Institute)
9:00 am - 9:20 amAlexander Doemling (University of Pittsburg)
"A Novel Approach to Small Molecule Protein-Protein Interaction Discovery: MDM2/4 p53"
9:20 am - 9:30 am Discussion
9:30 am - 9:50 amRolf Breinbauer (Graz University of Technology)
"The Tale of Two Enantiomers - Synthesis of Tool Compounds in Chemical Biology"
9:50 am - 10:00 am Discussion
10:00 am - 10:30 am Coffee Break
10:30 am - 11:00 amPaul Hanson (Kansas University)
"Facilitated DOS Approaches to Sultam Libraries"
11:00 am - 11:10 am Discussion
11:10 am - 11:40 amDerek Tan (MSKCC)
"Strategies and Tactics in the Synthesis of Natural Product-based Libraries"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pmSeung-Bum Park (Seoul National University)
"Importance of Molecular Diversity using Privileged Substructures for Translational Science and Chemical Biology"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 4:00 pmFree Time
4:00 pm - 5:30 pmPoster Session II
5:30 pm - 7:30 pmSynthetic Chemistry / Catalysis
Discussion Leader: Martin Burke (University of Illinois)
5:30 pm - 6:15 pmOliver Reiser (University of Regensburg)
"Immobilized Catalysts towards Applications in High Throughput Chemistry and Flow Processes"
6:15 pm - 6:30 pm Discussion
6:30 pm - 7:15 pmVy Dong (University of Toronto)
"Mechanism-Inspired Strategies for Organic Synthesis"
7:15 pm - 7:30 pm Discussion
7:30 pm - 8:00 pmBusiness Meeting (Part I)
(Nominations for the next Vice Chair; Fill out Conference Evaluation Forms)
8:00 pmDinner
THURSDAY
7:30 am - 8:30 amBreakfast
8:40 am - 9:00 amBusiness Meeting (Part II)
(Next Vice Chair Candidates Statements; Election of the next Vice Chair)
9:00 am - 12:30 pmMedicinal and Synthetic Chemistry
Discussion Leader: Oliver Reiser (University of Regensburg)
9:00 am - 9:20 amYoung-Tae Chang (National University of Singapore)
"LuminoGenomics by Diversity-Oriented Fluorescence Library Approach (DOFLA)"
9:20 am - 9:30 am Discussion
9:30 am - 9:50 amAndrew Phillips (University of Colorado)
"Chemistry and Biology with Natural Products and Other Small Molecules"
9:50 am - 10:00 am Discussion
10:00 am - 10:30 am Coffee Break
10:30 am - 11:00 amJames Barrow (Merck)
"Neuroscience Drug Discovery"
11:00 am - 11:10 am Discussion
11:10 am - 11:40 amAlex Godfrey (Lilly)
"The Virtual MedChem Lab - Making it Rea!"
11:40 am - 11:50 am Discussion
11:50 am - 12:20 pmMartin Burke (University of Illinois)
"The Prospect of Molecular Prosthetics: Small Molecules with Protein-Like Functions"
12:20 pm - 12:30 pm Discussion
12:30 pmLunch
1:30 pm - 5:30 pmFree Time
5:30 pm - 7:30 pmFrontiers in Drug Discovery
Discussion Leader: Robert Gould (Broad Institute)
5:30 pm - 6:05 pmChris Abell (University of Cambridge)
"Fragment-Based Approaches in Drug Discovery and Chemical Biology"
6:05 pm - 6:15 pm Discussion
6:15 pm - 6:35 pm Fred Berst (Novartis)
"Hinge-less Inhibitors of Kinases"
6:35 pm - 6:45 pm Discussion
6:45 pm - 7:20 pmAlan Palkowitz (Lilly)
"Phenotypic Drug Discovery: A Globally Integrated Platform Approach for Innovation"
7:20 pm - 7:30 pm Discussion
7:30 pm - 8:00 pmBusiness Meeting (Part III)
(Announce next Vice Chair; Discuss future Site & Scheduling preferences)
8:00 pmDinner
FRIDAY
7:30 am - 8:30 amBreakfast
9:00 amDepart

Last Updated: July 22, 2010
 
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