Chemistry Weekly Seminar - Dr. Len Luyt
Dr. Len Luyt, of The University of Western Ontario, will present a seminar at 4:00 p.m. in Thorvaldson 271.
Title:
The ghrelin receptor and its appetite for fluorinated peptides and small molecules.
Abstract:
The peptide ghrelin is the endogenous ligand for the growth-hormone secretagogue receptor (GHSR), also referred to as the ghrelin receptor. While the primary role of ghrelin relates to appetite regulation, there is increasing evidence for the cancer associated implications of the presence of the GHSR. We are developing a variety of fluorine-containing ghrelin analogues for the purpose of molecular imaging of the GHSR and as potential diagnostic-therapeutic pairs. In this seminar I will describe our efforts to create high affinity fluorine-containing ligands that target the GHSR. These truncated peptides and small molecules have been successfully radiolabelled with 18F for PET imaging, while also having the potential to be used as peptide therapeutics with natural 19F. Dimerization of the GHSR is believed to play an important role in signalling and we have discovered a bivalent ligand capable of inducing and stabilizing the receptor homodimer, with unique signalling characteristics.