NexMR AG reposted this
Many people have asked us: can you do 19F photohyperpolarization and design fragment libraries? Gabriela Stadler (PhD student in the Riek group, Institute for Molecular Physical Science (IMPS), ETH Zurich) has been working over the last 12 months to satisfy your (and our) curiosity. She now understands how 19F should be inserted into fragments to obtain high photohyperpolarization. She also addressed the key aspects of 19F fragment screening, such as fragment mixtures and the mechanisms behind binding contrast. Her platform for small molecule primary screening measures fragment mixtures within seconds at low micromolar concentration and enables the discovery of new chemical matter against critical oncology targets. This Wednesday, at EUROMAR in Bilbao, Gabriela will be unveiling her pioneering work for the first time. This is a presentation you cannot afford to miss. If you are at Euromar, seize the opportunity to witness her talk and engage in a discussion with her.
19F is already very sensitive, using less protein makes little sense because you are already doing fragments. Also 19F libraries are small, not sure it is a solid case for dnp here
I am not sure F labelled frags (or small molecules) have been such a magic bullet. Felix, has the methodology improved ? In the past this more than often failed to deliver with too many false positives.
lifelong learner
1moHi Felix, I have really enjoyed the talk of Gabriela and we do actually aim for a similar goal = faster measurements using 19f ligands for drug discovery. Do you think we can adopt your photocidnp protocol to our 19F-MRI as well? What are the requirements on a fluorinated reporter ligand? Are we limited in time? Our proof of concept study would definitely profit in increasing detection sensitivity of 19f signal at micromolar concentration.