Functional GPCR microarrays

Yulong Hong, Brian L. Webb, Hui Su, Eric J. Mozdy, Ye Fang, Qi Wu, Li Liu, Jonathan Beck, Ann M. Ferrie, Srikanth Raghavan, John Mauro, Alain Carre, Dirk Müeller, Fang Lai, Brian Rasnow, Michael Johnson, Hosung Min, John Salon, Joydeep Lahiri

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34 Scopus citations

Abstract

This paper describes G-protein-coupled receptor (GPCR) microarrays on porous glass substrates and functional assays based on the binding of a europium-labeled GTP analogue. The porous glass slides were made by casting a glass frit on impermeable glass slides and then coating with γ-aminopropyl silane (GAPS). The emitted fluorescence was captured on an imager with a time-gated intensified CCD detector. Microarrays of the neurotensin receptor 1, the cholinergic receptor muscarinic 2, the opioid receptor mu, and the cannabinoid receptor 1 were fabricated by pin printing. The selective agonism of each of the receptors was observed. The screening of potential antagonists was demonstrated using a cocktail of agonists. The amount of activation observed was sufficient to permit determinations of EC50 and IC50. Such microarrays could potentially streamline drug discovery by helping integrate primary screening with selectivity and safety screening without compromising the essential functional information obtainable from cellular assays.

Original languageEnglish (US)
Pages (from-to)15350-15351
Number of pages2
JournalJournal of the American Chemical Society
Volume127
Issue number44
DOIs
StatePublished - Nov 9 2005

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All Science Journal Classification (ASJC) codes

  • Catalysis
  • Chemistry(all)
  • Biochemistry
  • Colloid and Surface Chemistry

Cite this

Hong, Y., Webb, B. L., Su, H., Mozdy, E. J., Fang, Y., Wu, Q., Liu, L., Beck, J., Ferrie, A. M., Raghavan, S., Mauro, J., Carre, A., Müeller, D., Lai, F., Rasnow, B., Johnson, M., Min, H., Salon, J., & Lahiri, J. (2005). Functional GPCR microarrays. Journal of the American Chemical Society, 127(44), 15350-15351. https://doi.org/10.1021/ja055101h