We have succeeded in the synthesis of ZTA-261, a thyroid hormone receptor-selective beta-subtype agonist,, and our results have been published in Communications Medicine.

Thyroid hormone (TH) promotes lipid metabolism via the thyroid hormone β-receptor (THRβ) and has been expected to be a therapeutic agent for hyperlipidemia, fatty liver, and other lipid disorders. However, it has been problematic because it causes serious side effects such as decreased bone density and abnormally increased heart rate via the α-receptor (THRα).

In this study, we developed a new thyroid hormone analog, ZTA-261, which selectively binds to THRβ. When this compound was administered to obese model mice raised on a high-fat diet, a decrease in liver and blood lipids was observed. In addition, compared to the natural thyroid hormone T3 and the  THRβ-selective compound GC-1, side effects such as liver dysfunction, cardiac hypertrophy, and decreased bone density were significantly reduced.

This compound is expected to be used as a new therapeutic agent for dyslipidemia.

Congratulations to Dr. Ariki, Dr. Muhammad, Dr. Yim!!

This research was conducted in collaboration with Profs. Takashi Yoshimura, Taeko Ohkwa, and Ayato Sato (ITbM).

https://www.nature.com/articles/s43856-024-00574-z

Click here to read the press release article from Nagoya University.

https://www.nagoya-u.ac.jp/researchinfo/result-en/2024/08/20240807-01.html

This research was introduced in the Chunichi Shimbun and Nikkan Kogyo Shimbun!