Article
Backbone Modification of a Parathyroid Hormone Receptor-1 Antagonist/Inverse Agonist.
ACS chemical biology - 21 Oct 2016
Cheloha Ross W, Watanabe Tomoyuki, Dean Thomas, Gellman Samuel H, Gardella Thomas J
Abstract excerpt
A backbone-modified peptide derived from parathyroid hormone (PTH) is shown to function as an inhibitor and inverse agonist of parathyroid hormone receptor-1 (PTHR1) signaling. This receptor acts to regulate calcium and phosphate homeostasis, as well as bone turnover and development. PTH is a natural agonist of PTHR1, and PTH(1-34) displays full activity relative to the natural 84-residue hormone. PTH(1-34) is...
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