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Updated: Apr 27, 2026

Characterization of G Protein-coupled Receptors by a Fluorescence-based Calcium Mobilization Assay
Published on: July 28, 2014
Reverse pharmacology and the de-orphanization of 7TM receptors
Knut Kotarsky1, Niclas E Nilsson2
1Section of Immunology, Department of Cellular and Molecular Biology, Lund University, BMC I13, Tornavägen 10 221 84 Lund, Sweden.
Abstract:
Approximately 800 genes coding for seven-transmembrane, G-protein-coupled receptors have so far been recognized. In spite of this, many of these receptors are defined by their sequence only, and are therefore classified as orphan receptors. Without knowing what their endogenous ligands are, we lack the information needed to understand their physiological role and hence cannot make use of them as drug targets. In this communication, we discuss different strategies, as well as difficulties in the deorphanizing process.:
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