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A fluorescent reporter of ATP binding-competent receptor kinases

Renaud Sicard1, Jyothi Dhuguru, Wenjun Liu

  • 1Department of Biochemistry and Molecular Biology, University of Miami, Miami, FL 33101-6129, United States.

Bioorganic & Medicinal Chemistry Letters
|August 8, 2012
PubMed

Insights

Researchers developed DMAQ, a fluorescent probe for ERBB receptor kinases. This

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Chemical Biology

Background:

  • ERBB receptor kinases are vital in cellular development and cancer.
  • Receptor modifications create distinct subpopulations with varied functions.
  • Assessing ERBB activation via tyrosine phosphorylation is complex.

Purpose of the Study:

  • To create optical tools for investigating ERBB populations and activation states.
  • To develop a fluorescent 'turn-on' probe targeting the ERBB ATP binding pocket.

Main Methods:

  • Synthesis of a novel fluorescent probe, DMAQ.
  • Utilizing DMAQ's increased emission in hydrophobic/restricted ERBB2 kinase environments.
  • Assaying cellular ERBB2 autophosphorylation inhibition kinetics.

Main Results:

  • DMAQ exhibits increased fluorescence upon binding to ERBB2.
  • The probe allows analysis of receptor states at low occupancy without probe removal.
  • Cellular ERBB2 autophosphorylation inhibition correlates with DMAQ fluorescence.

Conclusions:

  • DMAQ is a novel 'turn-on' fluorescent probe for ERBB kinases.
  • This probe enables the study of receptor kinase populations in vitro and in live cells.
  • DMAQ offers a new method for analyzing ERBB activation states.

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