The integral membrane serine hydrolase KIAA1363 is elevated in aggressive cancer cells where it plays a role in pro-tumorigenic lipid metabolism. To more thoroughly understand the function of KIAA1363 in cancer and other biological processes, new tools are required to characterize the activity and cellular distribution of this enzyme in living systems. Here, we describe the synthesis and biological application of a small-molecule imaging probe, JW576, that selectively targets KIAA1363 in cells and animals. We use JW576 to determine that KIAA1363 is predominantly localized to intracellular membrane compartments in cancer cells that include, but are not restricted to the endoplasmic reticulum. We also show that JW576 can be used to measure the cellular half-life of KIAA1363 activity and for profiling this enzyme in peripheral mouse tissues in vivo.

Activity-based imaging probe for the integral membrane hydrolase KIAA1363

243rd National Meeting (2012)

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