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NPS Pharmaceuticals, Inc., Toronto, Ontario M5G 1L8, Canada
Key Words: calcimimetics calcium receptor allosteric modulators drug discovery
Address for correspondence: E.F. Nemeth, NPS Pharmaceuticals, Inc., 101 College Street, South Tower, Suite 800, Toronto, ON M5G 1L8 Canada. Voice: 416-849-5605; fax: 416-929-0610. e-mail: enemeth{at}npsp.com
Calcimimetics are ligands that activate the calcium receptor. Some are small molecules and of these, the most extensively studied are phenylalkylamines like cinacalcet. This compound is a positive allosteric modulator that selectively targets the parathyroid calcium receptor to inhibit the secretion of parathyroid hormone. Cinacalcet is the first calcimimetic compound to attain regulatory approval for the treatment of hyperparathyroidism resulting from end-stage renal disease. The discovery of calcimimetics and the receptor they act on are considered with the intent of extracting lessons relevant to medical research and the discovery of new drugs.
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