Research

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Research

The GPRC6A receptor belongs to the Family C of G protein-coupled receptors which includes other well studied receptors like the eight metabotropic glutamate receptors, the calcium sensing receptor, two GABA-B receptors and three taste receptors (1). All of these receptors have a characteristic large extracellular domain and a seven-transmembrane domain and can form oligomeric receptor complexes that have profound importance for their pharmacological signaling and localization (2).

 

The GPRC6A project is a highly interdisciplinary study with a group of chemists, computer chemists and pharmacologists (in vivo and in vitro) trying to decipher the importance of this receptor. The GPRC6A receptor was cloned in 2004 and shown to be activated by L-amino acids (3,4). However the physiological function of the receptor is still largely unknown.

 

(1) Schioth, H.B., and Fredriksson, R. Gen Comp Endocrinol, 142, 94-101 (2005).

(2) Kniazeff, J. et al. Pharmacol. Ther. 130, 9-25. (2011).

(3) Wellendorph, P. and Bräuner-Osborne, H. Gene, 335, 37-46 (2004).

(4) Wellendorph, P. et al. Mol. Pharmacol., 76, 453-65 (2009).

HTRF(C) technology

 

One of the technologies I have used a lot during my PhD project is the so-called Homogenous Time-resolved Förster Resonance Energy Transfer - short HTRF. It has been developed by the French company Cisbio Bioassays. It's kind of a modified version of the more traditional FRET (Förster Resonance Energy Transfer) technology. This technology takes advantage of two fluorophores where one of them can transfer energy to the other one, if they are located closely together. This means you can shine light with a certain wavelenght upon the first fluorophore and then measure light shining out of the second one with a different wavelength.

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GPRC6A

 

Did you know that GPRC6A belongs to the class of proteins that are targeted by almost 50 % of all marketed drugs?