Bestrophin (BEST) Inhibitors

Bestrophins (BESTs) are a family of ion channels found in various tissues of the human body, with prominent expression in the retina, where they play a crucial role in maintaining the ionic balance required for proper visual function. BESTs are classified as calcium-activated chloride channels, and they are implicated in the regulation of fluid and ion transport across cellular membranes. These channels are essential for the normal function of the retinal pigment epithelium (RPE), which is crucial for maintaining the health and integrity of photoreceptor cells in the eye. Dysfunctional BEST channels have been associated with certain inherited retinal disorders, such as Best vitelliform macular dystrophy (BVMD), indicating their significance in maintaining retinal homeostasis.

Bestrophin inhibitors are compounds that can modulate the activity of BEST channels, either by blocking or altering their ion conductance properties. These inhibitors may function through various mechanisms, such as directly binding to the BEST channel proteins or interfering with the calcium-dependent activation of these channels. The development and study of BEST inhibitors are essential for gaining insights into the physiological roles of BEST channels and for potential research applications.