Phenotype-Based High-Content Screening Using Fluorescent Chemical Bioprobes: Lipid Droplets and Glucose Uptake...

Phenotypic screening in live cells has emerged as a promising strategy for drug discovery in pharmaceutical communities. For relevant phenotype-based screening setups, it is critical to develop adequate reporters in order to selectively visualize subcellular compartments or phenotypic changes that represent disease-related characteristics during compound screening. In this chapter, we introduce two phenotype-based high-content/high-throughput assays using fluorescent bioprobes that have been designed and refined to selectively stain cellular lipid droplets (LDs) and to show cellular glucose uptake. In conjunction with target identification process for the hit compounds from phenotypic screening, these fluorescent chemical probe-based screening techniques are expected to drive a great advancement for the discovery of novel first-in-class therapeutics.