Cambridge Healthtech Institute’s 3rd Annual

GPCRs & Membrane Proteins
( GPCR和膜蛋白质 )

Designing Drugs Targeted at Proteins with Multiple Membrane-Spanning Domains

2019年4月10日~11日

 

Cell surface complex membrane proteins such as G protein-coupled receptors (GPCRs), ion channels and transporters are attractive targets to design or discover drug agents against. They play important physiological roles and are accessible to compounds circulating in the body, including potential new drug agents. However, due to their membrane-embedded nature, this drug target class is less tractable to structure-based drug design approaches that rely on solubilization of the proteins to obtain X-ray crystal structures. However, genetic ‘tricks’ that facilitate solubilization, better biophysical tools that enable study of proteins while still in the membrane and advances in electron microscopy are speeding progress in rational drug design and screening efforts against complex membrane proteins. At Cambridge Healthtech Institute's 3rd Annual GPCRs & Membrane Proteins conference, join fellow medicinal chemists, structural biologists, biophysical chemists and translational researchers to witness and discuss the impact of new structural knowledge about and tools for studying GPCRs and other complex membrane proteins for target-based drug design.

Coverage will include, but is not limited to:

 

  • New knowledge from cryoEM, NMR and X-ray crystallography studies on membrane proteins
  • Impact of new structures of GPCRs, ion channels and transporter proteins on structure-based drug design
  • Biosensor-based biophysical techniques (SPR and others) aiding membrane protein-based drug discovery
  • Using lipid bilayers, artificial vesicles and nanoparticles for membrane proteins
  • Case studies of new membrane-targeted drug candidates and their optimization challenges
  • GPCR-ligand kinetics and impact on drug design
  • Biased agonists and allosteric modulators of GPCRs, with a focus on opioid alternatives
  • Addressing GPCR pharmacological complexities in drug design

* 活动内容有可能不事先告知作更动及调整。