Drug repurposing analyses show that citalopram exerts anti-tumor effects by targeting C5aR1 on tumor-associated macrophages to enhance phagocytosis and CD8+ T cell immunity.
Establishment of AA263 analogs with improved potential for correcting pathologic disruptions of endoplasmic reticulum proteostasis implicated in the onset and pathogenesis of etiologically diverse diseases.
Liudmyla Arifova, Brian S MacTavish ... Douglas J Kojetin
Covalent PPARγ inhibitors that better stabilize a repressive conformation are more effective inhibitors, but structural plasticity still allows ligand cobinding by enabling a shift back to an active conformation.