Scientists at Nagoya University in Japan have made a significant breakthrough in treating lipid disorders.
Institute of Transformative Bio-Molecules , Nagoya UniversityAug 6 2024 They have developed a new compound, ZTA-261, which selectively binds to the thyroid hormone receptor beta . THRβ plays an important role in the regulation of lipid metabolism, which affects lipid levels in the blood. Mice administered the drug showed decreased lipid levels in the liver and blood, with fewer side effects in the liver, heart, and bones compared to existing compounds.
There is growing interest in developing treatments for dyslipidemia that leverage the properties of thyroid hormones. Thyroid hormones increase overall metabolism through binding to two types of receptors: alpha and beta . The brain, heart, and muscle contain the α-subtype, whereas the liver and pituitary gland primarily express the β-subtype.
As a result, THRβ has become a desirable target for treating metabolic disorders such as dyslipidemia. However, common treatments, such as the natural thyroid hormone T3, show almost no selectivity between the α and β receptors, making it difficult to avoid the severe side effects caused by binding to THRα.
They found that ZTA-261 had almost 100 times higher selectivity for THRβ than THRα. In comparison, GC-1 showed only a 20-fold difference in affinity, showing ZTA-261's superior selectivity. This was confirmed by the significant increase in heart weight and bone damage indicators in T3-treated mice but not in those treated with ZTA-261.
Blood Bone Brain Chest Pain Compound Dyslipidemia Heart Heart Attack Hormone Lipids Liver Medicine Metabolism Muscle Pain Preclinical Receptor Research Stroke Technology Thyroid
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