Publications by authors named "Tracey L Boyden"
Article Synopsis
- PDE2A inhibitors have shown potential in improving cognitive function in preclinical models, sparking interest in their further development.
- Researchers developed a new, highly potent PDE2A inhibitor (PF-05085727) that effectively penetrates the brain and demonstrates significant biochemical changes related to PDE2A inhibition.
- The compound also reverses cognitive impairments caused by NMDA antagonists in rodents, suggesting it could enhance NMDA signaling and holds promise for future clinical applications in cognition.
Unlabelled: The enzyme phosphodiesterase 2A (PF-05270430) is a potential target for development of novel therapeutic agents for the treatment of cognitive impairments. The goal of the present study was to evaluate the PDE2A ligand (18)F-PF-05270430, 4-(3-fluoroazetidin-1-yl)-7-methyl-5-(1-methyl-5-(4-(trifluoromethyl)phenyl)-1H-pyrazol-4-yl)imidazo[1,5-f][1,2,4]triazine, in nonhuman primates.
Methods: (18)F-PF-05270430 was radiolabeled by 2 methods via nucleophilic substitution of its tosylate precursor.
Inhibitors of the Hedgehog signaling pathway have generated a great deal of interest in the oncology area due to the mounting evidence of their potential to provide promising therapeutic options for patients. Herein, we describe the discovery strategy to overcome the issues inherent in lead structure 1 that resulted in the identification of Smoothened inhibitor 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea (PF-04449913, 26), which has been advanced to human clinical studies.
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