NAME Due Ap DIREC questions. response, and then create f and elegant. Proof read
ID: 3167103 • Letter: N
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NAME Due Ap DIREC questions. response, and then create f and elegant. Proof read va a respor your an: CLARI TYPE tes Astiva G CRITERION activaactiva ylates signal m tiv tes kinase C open IP,gated channel IP,) lumen of Question 1: Given the following G-protein coupled receptor (GPCR) signaling pathway: a) (5 pts) You want to find a drug which inhibits this calcium response pathway in normal cells where it is activated by a signal molecule (red dot). You decide to do mass screening to find that drug. You obtain a large collection of chemical compounds to screen. You make sure that they do not kill the cells and you test them in the following way: you treat the cells with the compounds and then stimulate them with the signal molecule (red dot) and analyze the response. Only one compound had an effect you call it drug#1 When the cells are treated with drug#1, and then stimulated with the signal molecule, you find that: PLC is active and cytoplasmic calcium concentration is low Give a possible mechanism of action of this drug. Answer:Explanation / Answer
G-protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes. These cell surface receptors act like an inbox for messages in the form of light energy, peptides, lipids, sugars, and proteins.
Such messages inform cells about the presence or absence of life-sustaining light or nutrients in their environment, or they convey information sent by other cells.
GPCRs play a role in an incredible array of functions in the human body, and increased understanding of these receptors has greatly affected modern medicine.
The activated G? interacts and regulates many effector molecules such as calcium, potassium channels, adenylyl cyclase, phospholipase C (PLC), PLD and protein kinases. Initially it was hypothesized that the ?? dimer acts as negative regulator and can block activation of adenylyl cyclase by this mechanism
A calcimimetic drug, inhibits the secretion of parathyroid hormone in postmenopausal women with mild primary hyperparathyroidism. These preliminary data suggest the possibility that a drug of this type may become a useful alternative to parathyroidectomy in patients with primary hyperparathyroidism.
Recent efforts to reduce parathyroid hormone secretion are based on the molecular mechanism by which the parathyroid cell senses perturbations in extracellular calcium. The G-protein–coupled calcium-sensing receptor and its ligand, ionic calcium, are central to this mechanism.
In the early 1990s, in parallel with the cloning of the calcium-sensing receptor, compounds were identified that could activate this receptor. One such compound, the phenylalkylamine used in this study, was found to increase cytoplasmic calcium and decrease parathyroid hormone secretion in vitro.
It was also found to inhibit parathyroid hormone secretion and decrease serum calcium concentrations in rats and in normal postmenopausal women. In vitro this drug inhibited parathyroid hormone secretion from adenomatous and hyperplastic parathyroid cells.
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