Nicolas Bocquet
leadXpro AG, Switzerland
Title: Structure based drug discovery on membrane protein targets
Biography
Biography: Nicolas Bocquet
Abstract
Today, soluble proteins are managed routinely within the project timelines and scope with the rapid portfolio changes in pharmaceutical industry. Establishment of biophysical and structure-based methods for transmembrane proteins still represents a significant challenge to have an impact on drug discovery. leadXpro combines membrane protein expression, purification and structure determination coupled to premium access to the synchrotron Swiss Light Source (SLS), the Free Electron Laser (SwissFEL) and single particle cryo-electron microscopy (cryo-EM) at the University of Basel. LeadXpro also confronts structural data to different biophysical measurements like thermal shift assays, radiobinding assay and wave guide interferometry in order to generate better lead molecules with appropriate features.
The talk/poster will show advancements in projects and technologies with examples for serial crystallography performed at synchrotron and free electron laser enabling structure determination of challenging drug targets. Moreover, recent efforts and implementation of wave-guide interferometry method for analysis of small (fragment-like molecules)/large ligand binding kinetics on membrane proteins will be discussed in the context of i) lead discovery and optimization ii) biologics targeting membrane proteins. Finally, recent progress in cryo-EM will also be discussed.