DMMC Course DRUG DESIGN: PRINCIPLES & TECHNIQUES

1015-1100 Friday 20 April 2007. Albert Lecture Theatre, RCSI

The concept of pharmacophore: biological perspective
Dr Niamh Moran, RCSI

This lecture builds on the previous one, illustrating with examples of peptides and peptidomimetics that have been developed as drugs, and highlighting areas for concern in such development. Using the cardiovascular system as an example, the development of a simple peptide-based drug (namely RGD; an integrin receptor ligand) will be reviewed focusing on experimental analysis of the pharmacophore. The targeting of intracellular ligands using cell-permeabilizing delivery agents will be discussed. Finally, a summary of the time involved in biological screening and verification will be presented.