A Clickable Oxysterol Photolabel Retains NMDA Receptor Activity and Accumulates in Neurons.

ABSTRACT: Oxysterol analogs that modulate NMDA receptor function are candidates for therapeutic development to treat neuropsychiatric disorders. However, the cellular actions of these compounds are still unclear. For instance, how these compounds are compartmentalized or trafficked in neurons is unknown. In this study, we utilized a chemical biology approach combining photolabeling and click chemistry. We introduce a biologically active oxysterol analog that contains: (1) a diazirine group, allowing for the permanent labeling of cellular targets, and (2) an alkyne group, allowing for subsequent in situ visualization using Cu2+ catalyzed cycloaddition of an azide-conjugated fluorophore. The physiological properties of this analog at NMDA receptors resemble those of other oxysterols, including occlusi

SUBMITTER: Chen DM 

PROVIDER: S-EPMC6291516 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature