Article
Identification of an orally active small-molecule PTHR1 agonist for the treatment of hypoparathyroidism.
Nature communications - 18 Nov 2016
Tamura Tatsuya, Noda Hiroshi, Joyashiki Eri, Hoshino Maiko, Watanabe Tomoyuki, Kinosaki Masahiko, Nishimura Yoshikazu, Esaki Tohru, Ogawa Kotaro, Miyake Taiji, Arai Shinichi, Shimizu Masaru, Kitamura Hidetomo, Sato Haruhiko, Kawabe Yoshiki
Abstract excerpt
Parathyroid hormone (PTH) is essential for calcium homeostasis and its action is mediated by the PTH type 1 receptor (PTHR1), a class B G-protein-coupled receptor. Hypoparathyroidism and osteoporosis can be treated with PTH injections; however, no orally effective PTH analogue is available. Here we show that PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1. PCO371 does not...
Topics
- Animals
- Dogs
- Female
- Gene Expression Regulation
- Humans
- Hypoparathyroidism
- Imidazolidines
- Male
- Molecular Structure
- Mutation
- Parathyroid Glands
- Rats
- Receptor, Parathyroid Hormone, Type 1