Tools for investigating functional interactions between lipid-derived autacoids and their receptors

Michael R. Lerner, Lina Golovyan, Gerard F. Graminski, Kristine Harris, Liquan Huang, Channa K. Jayawickreme, Suresh Karne, Timothy S. McClintock, Marc N. Potenza, Alison Roby-Shemkovitz, Marc Quillan

Research output: Contribution to journalArticlepeer-review

1 Scopus citations


A method for rapidly evaluating functional interactions between ligands and G-protein-coupled receptors has been developed. The technology is based on the ability of animals to change color by controlling the position of pigmented organelles within skin cells called melanophores cDNA coding for a receptor to be studied is expressed in immortalized frog melanophores. Stimulation of a receptor that normally functions to activate either adenyl cyclase or phospholipase C induces centrifugal melanosome translocation and cell darkening. Conversely, application of an agonist to cells expressing a receptor that operates to inhibit adenyl cyclase induces centripetal pigment movement and cell lightening. The simple optical change can be used to investigate ligand-receptor interactions at several levels, including single- cell analysis and high-throughput chemical screening. Current efforts are focused on (1) identifying small peptides that activate or block thromboxane A2 and platelet-activating factor (PAF) receptors and (2) cleaning eicosanoid receptors.

Original languageEnglish
Pages (from-to)280-286
Number of pages7
JournalAmerican Journal of Therapeutics
Issue number4
StatePublished - Apr 1996


  • G-proteins
  • functional interactions
  • ligands
  • melanophores

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


Dive into the research topics of 'Tools for investigating functional interactions between lipid-derived autacoids and their receptors'. Together they form a unique fingerprint.

Cite this