G-protein coupled receptors (GPCRs) are currently the most popular therapeutic targets. With our leading techniques and rich experience, Creative Biolabs now launches the world-leading GPCR stable cell lines engineered with calcium-activated fluorescent biosensors for receptor function evaluation of therapeutic drugs against various GPCRs. Our cell lines cover a wide range of GPCRs (e.g. CCK1, CCK2, M5, NK1, NK3) to meet the different needs of customers.
Bombesin is a tetradecapeptide, originally isolated from the skin of frogs. The corresponding analogs of human are neuromedin B (NMB) and gastrin-releasing peptide (GRP). Human bombesin (Bn) receptors belong to the GPCR family and are divided into three categories: BB1, BB2, BB3.
BB2 is activated by the endogenous ligands gastrin-releasing peptide (GRP), neuromedin B (NMB) and GRP-(18-27). Binding with either of these ligands can activate BB2 and stimulate the calcium signaling pathway. It is evidenced that BB2 receptor is widely expressed in the CNS as well as in the reproductive organs and gastrointestinal tract. Activation of the BB2 receptor can lead to a series of physiological effects, ranging from the stimulation of normal and neoplastic tissue growth, smooth-muscle contraction to many central nervous system effects.
Fig.1 Receptors for the bombesin family.1
Magic™ BB2 stable cell line was transformed with the calcium-activated biosensor and label-free human Bombesin Receptor 2 (BB2) in U2OS cells, providing a convenient and sensitive tool for evaluating various compounds targeting BB2 in high-throughput format. Fluorescent biosensors on the plasma membrane will translocate into cytosol momentarily in response to calcium activation, thus real-time monitoring BB2 activities. Such assay can be easily quantified on living cells by image analysis of fluorescence location and intensity.
In addition to the BB2 stable cell line, we also provide stable cell lines with high expression of different GPCRs, including calcium-activated, cAMP-activated, and DAG-activated.
Creative Biolabs spares no effort in developing the innovative strategies to facilitate drug discovery against various GPCR targets. We are also happy to construct custom cell lines upon request. Of note, we also offer many other Magic™ engineered cell lines to assess calcium-, cAMP-, DAG-related as well as multiplex pathway events. If you cannot find your desired target in our catalog, we are always happy to construct a custom cell line for you. Please contact us for more information and a detailed quote.
Reference
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