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A Cost-effective Workflow for High-Throughput Screening of G-Protein Coupled Receptors ( GPCRs ) Monitoring Receptor Mediated Calcium Flux
| Content Provider | Semantic Scholar |
|---|---|
| Author | Shen, Dee Schultz, Joanne B. Patton, Wayne F. |
| Copyright Year | 2011 |
| Abstract | Cell-based assays that monitor the functional activation of GPCRs are considered a critical part of the drug discovery process. Many of these receptors initiate signaling cascades that can result in changes in calcium levels within the cell [1]. GPCRs are a super-family of transmembrane receptor genes the exact number of which is unknown but has been suggested to consist of over 1000 proteins [2]. GPCRs are integral membrane proteins characterized by an extracellular N-terminus, followed with seven transmembrane a-helices connected by three intracellular and three extracellular loops and an intracellular C-terminus [2]. The GPCR system is modular, consisting of an a-subunit which binds and hydrolyzes GTP, as well as b and γ subunits which form a complex. The complex is modular and with each subunit having several different subtypes, the mix and match of which provides much of the functional versatility of the GPCRs. The a-subunits can be divided into four families of which the Gaq/ Ga11 family interacts with phospholipase C, leading to the mobilization of intracellular calcium [2]. |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | https://www.biotek.com/assets/tech_resources/Enzo_GPCR_App_Note.pdf |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
