Terry Kenakin presents: 7 Transmembrane Receptor Allostery: Putting Numbers to Shapeshifting Proteins. Bioinformatics Seminar, January 23 1pm.

As the technology of discovery advances to the point where various behaviors of 7TM receptors can individually be observed, it is clear that receptors are much more 'micro-processors' of information than 'on-off' switches. This has introduced a phenomenon referred to as 'functional; selectivity' into the field and opened new horizons for drug discovery. In addition, the increased emphasis of functional screening has introduced a great many more allosteric ligands into new chemical entity space. The need to quantify drug effect on these complex systems to guide medicinal chemistry requires new models and approaches; these will be discussed as well as the impact of energy landscape molecular dynamics on 7TM drug discovery. Finally, advances in allosteric HIV entry inhibitors will be presented as an example of where allostery can offer unique therapeutic applications.