Target Identification, Validation, and Screening in Drug Discovery and Development

Advances in biology, chemistry, biophysics and engineering have resulted in a vast number of potential disease-relevant drug targets and an increased efficiency in screening compounds for drug-like activity. Students will learn both the conceptual and current methodology being utilized in the identification and validation of new targets for drug intervention. This course will explore screening methods for hit identification and lead optimization as well as new approaches to biological models for drug discovery.

The particular topics to be discussed include: the concepts of target identification and validation; in vitro and in vivo techniques; how this approach is driving present drug discovery efforts; pharmaceutical companies’ new potential pharmacological targets; historical prospective of the evolution of TI/TV efforts and the paradigm shift to gene-derived targets.

Learning Outcomes

• Understand the principles of target identification and validation and strategies used in target and drug discovery.
• Explain the various drug target classes and explain specific techniques used for target identification and validation
• Understand the principles of target screening strategies, assays and approaches used in lead identification and optimization during preclinical development of drugs
• Appreciate the evolution of target identification from past to present and future strategies