CMSE IMPACT - Alex Dickson

  • Oct 31, 2019
  • Homepage Hero, News

There is a protein called TSPO which is up-regulated in neuroinflammation. Small molecules that bind selectively to TSPO are used in PET scans to reveal concussions, brain inflammation and damage to neurons. We are currently working to simulate the binding and release pathways of a ligand used in PET scans called PK-11195.  Interestingly, we find that the surrounding lipid membrane acts as a “pit-stop” along the binding and unbinding route, which could have implications for ligand binding kinetics, and the design of future drug molecules that target the TSPO protein.

side view image looking within the plane of the membrane

top view looking down on the membrane

 

 

 

 

 

 

To explain the image findings above, TSPO is in grey, the PK-11195 ligand is in sphere representation and the lipid molecules that make up the membrane are shown as sticks.  The first image is a “side view” looking within the plane of the membrane, and the second image is a “top view”, looking through the membrane.

 

To watch a video of this content explained by Dr. Dickson, click the video below: