Fragment-Based Lead Discovery: Issues and Applications

17 Feb 2014, at 13:00 - 17:00 in Barcelona, Spain

Who Should Attend?

This course is suitable for researchers who are currently using, or who wish to use, Fragment Based Lead Discovery (FBLD) methods to identify and optimise Hits and Leads in a Drug Discovery program. It is also suitable for those who are developing compound libraries for use in FBLD campaigns, and for anyone with an interest in integrating FBLD approaches with existing hit identification and lead optimisation strategies such as HTS.

Learning Objectives

• To understand the theoretical basis underlying the Fragment Based Lead Discovery (FBLD) approach
• To understand the practical aspects of FBLD, and in particular how to avoid some of the more common pitfalls and mistakes which can bedevil an FBLD campaign
• To understand the types of targets for which an FBLD approach will be applicable, and to examine the various experimental methods which can be used to identify and validate fragment hits 
• To learn how FBLD can be integrated with other methods of Hit Identification such as HTS and Virtual Screening, and how low affinity fragments can be evolved into potent hits and leads
• To examine case histories of FBLD campaigns, and to identify strategies for the evolution of low affinity fragments into potent hits and leads

Topics & Course Organisation

1. Introduction 
2. Perspective of the development of FBLD 
3. An overview of the FBLD approach 
4. Compound library design and characterisation 
5. Assaying fragment binding using biophysical and biochemical techniques 
6. Common problems and pitfalls in FBLD campaigns 
7. Experiences and comparison of various FBLD approaches 
8. Integrating fragments with HTS and VS hits 
9. Evolution of fragments into potent leads and hits 
10. FBLD case histories 
11. Discussion
12. Conclusions and prospective