Cell Line

Recombinant CHO-K1 cells stably overexpress G15 alpha subunit protein (Gα15), which belongs to Gq/11/14/15 alpha subunit family. When Gα15 and Gs-coupled or Gi/o-coupled receptor are co-expressed in cells, the cells not only can be triggered to stimulate or inhibit the cAMP pathway based on the coupled G alpha subunit types, but also can conduct Gq-coupled signal transduction and mobilize intracellular calcium following certain ligand binding. This cell line is recommended to use as a host cell line for transient or stable expression of Gs and Gi/o -coupled receptors, which is able to provide more readouts to study G protein-coupled receptors.

Muscarinic acetylcholine receptors belong to a superfamily of seven-TM-domain receptors that interact with G-proteins to initiate intracellular responses. Five muscarinic receptor subtypes have been identified and named from M1 to M5. The M2 muscarinic receptor couples to G_i/o to inhibit cAMP production. GenScript co-transfected human M2 with Gα15 in the CHO-K1 which supports high levels of recombinant M2 expression on the cell surface and contains high levels of Gα15 to couple the receptor to the calcium signaling pathway.

Muscarinic acetylcholine receptors belong to a superfamily of seven-TM-domain receptors that interact with G-proteins to initiate intracellular responses. Five muscarinic receptor subtypes have been identified and named from M1 to M5. The M3 muscarinic receptors are located at many places in the body, e.g. smooth muscles, endocrine, exocrine glands, as well as lungs. They are also found in the CNS, where it induces emesis. They generally cause smooth muscle contraction and increased glandular secretions.

The α₁-adrenergic receptor (AR) family consists of three closely related gene products (α_1A, α_1B, and α_1D). They mediate the actions of norepinephrine (NE) and epinephrine in sympathetically innervated tissues and brain. Α₁-ARs belong to the G protein-coupled receptor family and consist of single polypeptide chains that are predicted to form seven transmembrane spanning domains. With similar pharmacological and signaling properties, α₁-AR subtypes act through G_q/11 proteins to activate phospholipase C, increase inositol 1,4,5-trisphosphate production, and increase intracellular Ca²⁺. ADRA1B functions in diverse settings include vasoconstriction and myocardial contractility, neuronal dopaminergic responses, dendritic cell migration and inflammatory responses, as well as neuroendocrine regulation of fertility.

The platelet-activating factor (PAF) receptor (PTAFR) is a G protein coupled receptor that signals through multiple pathways and mediates several cellular responses including cell motility, smooth muscle contraction, and releases of cytokine and leukotriene (Stafforini et al., 2003). In humans, various diseases have been associated with PAF, such as allergic asthma, endotoxic shock, atherosclerosis and psoriasis.

The ß-adrenergic receptors are linked to G proteins. The ß-receptor has three known subtypes. Beta-1 receptors primarily regulate myocardial tissue and affect the rate of contraction via impulse conduction. Beta-2 receptors regulate smooth muscle tone and influence vascular and bronchiolar relaxation. Beta-3 receptors are less well studied but are thought to primarily affect lypolysis and may have effects on cardiac inotropy (Greene Shepherd，2006). In the human heart, beta (1)- and beta (2)AR are the most powerful physiologic mechanism to acutely increase cardiac performance. Changes in betaAR play an important role in chronic heart failure (CHF). Thus, due to increased sympathetic activity in CHF, betaAR are chronically (over) stimulated, and that results in beta (1) AR desensitization and alterations of down-stream mechanisms (Brodde OE，2006).

Cholecystokinin (CCK)-A and CCK-B receptors are highly homologous members of the seven transmembrane domain G-protein-coupled receptor super-family. Peptides in the cholecystokinin (CCK) family have a variety of biological functions in the central and peripheral nervous systems as well as in the gastrointestinal tract. The CCKA receptor has a more limited distribution with the highest densities in the hypothalamic nuclei, areas of the hippocampus, the septum, dorsal motor vagal nucleus, and interpeduncular nucleus of the brain stem. It also occurs in numerous gastro-intestinal tissues. Binding of ligands to CCK1 stimulates mobilization of intracellular calcium by activation of Gq/11. CCKA receptors affect satiety, pancreatitis, and gut motility and have growth-promoting effects on some tumors.

CHO-K1/MC4/Gα15 Stable Cell Line,2vials

Free fatty acid G protein coupled receptor family consists of four members and plays significant roles in nutrition regulation. GPR40 and GPR120 are activated by medium and long-chain FFAs, whereas GPR41 and GPR43 can be activated by short-chain FFAs. GPR40 is preferentially expressed in pancreatic beta-cells and mediates the majority of the effects of FFAs on insulin secretion. Researches show that GPR40 is a potential therapeutic target and plays an important role in the chain of events linking obesity and type2 diabetes.