GPR 40 and GPR 120 are members of 7 trans-membrane receptor family. 7TM receptors are ubiquitously expressed in human tissues. GPR40/120 among others, are expressed in the gastrointestinal tract and in the endocrine pancreas and are believed to be involved in the control of the secretion of for example insulin and glucagon like peptide-1.

Growing numbers of these receptors are identified as “constitutively active” – they signal through natural signaling pathways in absence of ligand. Interfering or modulation of this phenomenon proves to be interesting as new drug target.

To understand mechanisms of GPR40 & GPR 120 intra-cellular signalization we have conducted studies which allowed identification of G protein subunits responsible for trafficking of GPR40/120 signals. We have studied ligand independent (constitutive) signaling through CREB and SRE pathways in cells after exposition to forskolin and pertussis toxin. This procedure employs co-transfection of cells with promiscous G proteins which enhances cellular response after receiving signals from receptors. Proper recognition of proteins involved in signal transduction is necessary for development of sensitive and accurate screening of compounds which are suggested ligands for studied receptors.

Recently it has been proposed that GPR40 constitutive activity was an effect of endogenous ligands (e.g. fatty acids) being bound to BSA. We have conducted a series of experiments in which this possibility was checked. Obtained results indicated that fatty acids bound to BSA do not influence activity of GPR 40 receptors.

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