Targeting TEAD with small-molecule inhibitors is an emerging therapeutic strategy for YAP/TAZ-dependent human cancers with Hippo pathway alterations. Bridgene Biosciences Inc. identified three hits with the Isobaric Mass Tagged Affinity Characterization (IMTAC) screening platform that covalently bound to TEAD1 with the binding site being cysteine 359, which led to the BGI-9004 compound.
Researchers from the University of Saskatchewan have developed a novel theranostic candidate, [67Cu]EB-TATE, as an alternative to [177Lu]DOTATATE, for the imaging of gastroenteropancreatic neuroendocrine tumors (GEP-NET). EB-TATE, which is a derivative of octreotate with evans blue (EB), was radiolabeled with electron linear accelerator-produced 67CuCl2.
The suboptimal metabolic stability of radiolabeled gastrin-releasing peptide receptor (GRPR) antagonists has been a hindering factor of these promising theranostic candidates for prostate cancer. Uppsala University researchers have recently reported the development of [111In]DOTAGA-PEG-2-SAR11-RM-26, after replacement of Gly11 by Sar11 in the peptidic chain.
mPGES-1 is overexpressed in the dopaminergic neurons of the substantia nigra pars compacta of post-mortem brain tissue from patients with Parkinson’s disease (PD) as well as in 6-hydroxydopamine (6-OHDA)-injected PD mice.
Researchers have detailed the development and preclinical characterization of a novel heterobivalent radiotracer targeting prostate-specific membrane antigen (PSMA) and the gastrin-releasing peptide receptor (GRPR).