Fragment Based Drug Discovery
Hilton San Diego Resort

San Diego, California


   Fragment-based approaches to lead discovery are rapidly gaining
   interest in many labs as they have established themselves as a useful
   and efficient way to explore new leads for drug candidates. Several
   technologies have matured into reliable methods to detect binding of
   fragments, to screen for new targets and to optimize leads. Top
   experts in industry and academia will address questions such as how to
   select the most suitable projects; how and when to use screening
   methods such as crystallography, NMR or mass spec, either as a
   standalone technique or complimentary; and how to correctly predict

Schedule of Presentations:

Tuesday, April 27, 2010
07:00:00 Registration and Morning Coffee
08:00:00 Chairperson's Opening Remarks
08:05:00 Fragment – Based Techniques
08:10:00 KEYNOTE - FBDD by NMR and Virtual Docking: Puzzling Approaches to Ligand Discovery Maurizio Pellecchia
08:50:00 Novel Heparanase Inhibitors Based on NMR Fragment-Based Strategies Antonio Pineda-Lucena
09:20:00 Shortening the Time to a Successful Fragment HTL Campaign Sandy Farmer
09:50:00 Networking Coffee Break
10:15:00 Methods for Structure Based Scaffold Replacement Chris Williams
10:45:00 SPR-Based Screening of Fragment Library: Case Studies Girija Krishnamurthy
11:15:00 Computational Approaches to Fragment-Based Design and Predicting Fragment Poses Shikha Varma-O’Brien
11:30:00 Exploring Flexible Protein Targets by Fragment-Based Drug Discovery Peter Brandt
12:00:00 Luncheon Presentation (Sponsorship Opportunity Available) or Lunch on Your Own
13:00:00 Break
13:25:00 Chairperson's Remarks
13:30:00 Recent Experiences in Fragment-Based Discovery Roderick E Hubbard
14:00:00 Fragment Optimization of a Dynamic Target: Finding Non-peptidic Matter for the Ala-Val Subpockets XIAP Cathy Moore
14:30:00 Fragment-Based Design of Oally Bioavailable CDK Inhibitors Andrew Woodhead
15:00:00 Use of a Metabolome-Inspired Fragment Library for Identifying Startpoints for Anti-Infective Drugs Doug Davies
15:15:00 Networking Refreshment Break, Poster and Exhibit Viewing
16:00:00 Speaker to be Announced
16:30:00 Combining Structurally Related Fragment and Screening Libraries: A Case Study Daniel Obrecht
17:00:00 Talk Title to be Announced Ye Che
17:30:00 Networking Cocktail Reception in the Exhibit Hall
18:30:00 End of Day
Wednesday, April 28, 2010
07:45:00 Continental Breakfast Break-Out Discussions
08:55:00 Chairperson's Opening Remarks
09:00:00 Fragment-Based Lead Generation of Inhibitors Engineered Towards Long Residence Time Gerhard Mueller
09:30:00 Challenges and Progress in Computational Fragment-Based Discovery Noeris Salam
10:00:00 Sponsored Presentation (Opportunity Available)
10:15:00 Coffee Break, Poster and Exhibit Viewing
11:00:00 SbN / FBDD Yields Highly Potent and Selective BACE Inhibitors Daniel Wyss
11:30:00 DNA-Encoded Self-Assembling Chemical Libraries used for Lead Generation and Affinity Maturation  Jorg Scheuermann
12:00:00 End of Conference
3D Tissue Models
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