Symeres webinar on structure based drug discovery for membrane proteins by Michael Hennig March 11, 2021, 10 am or 6 pm CET
Integral membrane proteins such as GPCR’s, ion-channels and transporters are drug targets for the majority of all approved medicines. While structure-based drug discovery on soluble proteins is managed well within the project timelines and portfolio changes in pharmaceutical industry, transmembrane proteins are still underexplored because of their challenges to be expressed, purified and made them work for drug ligand interaction analysis by biophysical methods and high-resolution structure determination.
Based on a unique platform for membrane protein expression, purification and engineering, the preferred access to synchrotron/free electron laser (SLS/SwissFEL) for X-ray analysis and cryo-EM facilities (Uni Basel), leadXpro is able to screen, optimize and structurally characterize small molecules and biotherapeutics in complex with drug targets timely to impact the drug discovery of novel therapeutics.
Showcase examples will include the structure determination of the chemokine receptor CCR2 by X-ray analysis and cryo-EM structures of human TRPV4 with bound small molecule agonist as well as an antibiotics transporter target.
Future developments include application of femtosecond X-ray pulses to enable monitoring and capturing of dynamic processes of ligand binding and associated conformational changes with great impact to the design of candidate drug compounds.