An ultrasensitive biosensor for high-resolution kinase activity imaging in awake mice

Nat Chem Biol. 2021 Jan;17(1):39-46. doi: 10.1038/s41589-020-00660-y. Epub 2020 Sep 28.

Abstract

Protein kinases control nearly every facet of cellular function. These key signaling nodes integrate diverse pathway inputs to regulate complex physiological processes, and aberrant kinase signaling is linked to numerous pathologies. While fluorescent protein-based biosensors have revolutionized the study of kinase signaling by allowing direct, spatiotemporally precise kinase activity measurements in living cells, powerful new molecular tools capable of robustly tracking kinase activity dynamics across diverse experimental contexts are needed to fully dissect the role of kinase signaling in physiology and disease. Here, we report the development of an ultrasensitive, second-generation excitation-ratiometric protein kinase A (PKA) activity reporter (ExRai-AKAR2), obtained via high-throughput linker library screening, that enables sensitive and rapid monitoring of live-cell PKA activity across multiple fluorescence detection modalities, including plate reading, cell sorting and one- or two-photon imaging. Notably, in vivo visual cortex imaging in awake mice reveals highly dynamic neuronal PKA activity rapidly recruited by forced locomotion.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Alprostadil / pharmacology
  • Animals
  • Biosensing Techniques*
  • Cyclic AMP-Dependent Protein Kinases / genetics*
  • Cyclic AMP-Dependent Protein Kinases / metabolism
  • Dihydroxyphenylalanine / pharmacology
  • Dinoprostone / pharmacology
  • Fluorescent Dyes / chemistry
  • Gene Expression
  • Gene Library
  • Genes, Reporter
  • Glucagon-Like Peptide 1 / pharmacology
  • HEK293 Cells
  • HeLa Cells
  • High-Throughput Screening Assays
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Hippocampus / enzymology
  • Humans
  • Mice
  • Microscopy, Fluorescence, Multiphoton
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / enzymology*
  • Myocytes, Cardiac / ultrastructure
  • Neurons / drug effects
  • Neurons / enzymology*
  • Neurons / ultrastructure
  • Optical Imaging / methods*
  • Primary Cell Culture
  • Signal Transduction

Substances

  • Fluorescent Dyes
  • Dihydroxyphenylalanine
  • Glucagon-Like Peptide 1
  • Cyclic AMP-Dependent Protein Kinases
  • Alprostadil
  • Dinoprostone