Calcium Sensor Family Related Drug Discovery Products
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
The parathyroid glands and the kidneys are two examples of calcitropic tissues that express the calcium sensing receptor (CaSR). It plays a crucial role in bone and mineral metabolism. In response to changes in extracellular calcium concentrations, the CaSR enables modulation of parathyroid hormone (PTH) release and renal tubular calcium re-absorption. The CaSR is also expressed in other tissues, including the intestines, pancreatic islets, lungs, brain, skin, and vasculature. It plays a role in physiological regulation of enteroendocrine hormone secretion, cardiac function, vascular tone, and lung and neuronal development as well as noncalcitropic actions that regulate molecular and cellular processes.
Creative Biolabs is a leader in drug discovery and development, we can offer calcium sensor family drug discovery assays and products to help our clients accelerate drug discovery:
Overview of Calcium Sensor Receptor
CaSR contains an important ICD of 216 amino acids, a 7TMD of 250 amino acids, and an ECD of 612 amino acids. A bilobed structure with a fissure between the lobes that are structurally similar to the Venus Flytrap (VFT) domain of bacterial periplasmatic binding proteins makes up a cysteine-rich region (CRR) that connects the large ECD of the CaSR to the 7TMD. The CaSR is a homodimeric receptor that is mostly present on the surface of cells. It is connected by hydrophobic interactions and disulfide bridges formed of two cysteine residues. The interaction favors an active state of the CaSR, which interacts with and activates several intracellular proteins, including G proteins and -arrestins. Calcium binds to the orthosteric binding sites of the CaSR. The extracellular calcium circumstances are transmitted to a cellular response by the stimulation of these intracellular proteins, which starts signaling pathway cascades.
CaSR Signaling
The CaSR couples to heterotrimeric guanine nucleotide binding proteins to initiate downstream signaling cascades. For the transmission of the CaSR signal, the Gq/11 proteins are essential. The CaSR stimulates phospholipase C to break down phosphatidylinositol 4,5-bisphosphate into diacylglycerol and inositol 1,4,5-trisphosphate through the Gq/11 family of proteins. The CaSR promotes the activity of MAPKs while suppressing adenylyl cyclase activation and cAMP generation by connecting to the pertussis toxin-sensitive Gi/o proteins. The ERK1 and/or ERK2 arm of the MAPK pathway can also be stimulated by the CaSR through a G protein-independent method involving the β-arrestin proteins.
Calcium Sensor Receptor Drug Discovery
The CaSR is expressed in all tissues involved in preserving calcium homeostasis and is a crucial component of this balance. CaSR is a potent therapeutic target for controlling PTH secretion in PTH-related illnesses due to its expression and strong regulatory features of PTH secretion in the parathyroid glands.
