针对甲状腺激素受体 β (THRβ) 的药物研发,用于治疗肝脏疾病和其他医疗适应症

IF 14.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Acta Pharmaceutica Sinica. B Pub Date : 2024-08-02 DOI:10.1016/j.apsb.2024.07.025
Kean Wang, Feiyang Chen, Jiang Wang, Hong Liu
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引用次数: 0

摘要

甲状腺激素受体(THR)是一个重要的核受体蛋白家族,主要由受体和受体两类组成。其中,THR是对肝脏有益的甲状腺激素的主要亚型。近二十年来,人们一直在努力开发THR激动剂,以选择性地产生对肝脏有益的作用,如降低甘油三酯和胆固醇,同时减少对心脏、肌肉和骨骼的不利影响。本文系统回顾了提高 THR 激动剂治疗 MASH 的安全性的策略,重点是提高 THR 的选择性和增加药物在肝脏中的分布。此外,我们还探讨了这一靶点在其他医疗适应症中的潜在应用。
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Drug discovery targeting thyroid hormone receptor β (THRβ) for the treatment of liver diseases and other medical indications
Thyroid hormone receptors (THRs), a crucial nuclear receptor protein family, primarily consist of two categories: receptors and receptors. Among them, THR is the primary subtype of thyroid hormone that confers benefits to the liver. In the last two decades, there have been efforts to develop THR agonists that selectively yield beneficial effects on the liver, such as lowering triglycerides and cholesterol, while reducing adverse effects on the heart, muscle, and bone. This paper systematically reviews strategies to enhance the safety of THR agonists for the treatment of MASH, with a focus on improving the selectivity of THR and increasing the distribution of the drug in the liver. Additionally, we explore the potential application of this target in addressing other medical indications.
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来源期刊
Acta Pharmaceutica Sinica. B
Acta Pharmaceutica Sinica. B Pharmacology, Toxicology and Pharmaceutics-General Pharmacology, Toxicology and Pharmaceutics
CiteScore
22.40
自引率
5.50%
发文量
1051
审稿时长
19 weeks
期刊介绍: The Journal of the Institute of Materia Medica, Chinese Academy of Medical Sciences, and the Chinese Pharmaceutical Association oversees the peer review process for Acta Pharmaceutica Sinica. B (APSB). Published monthly in English, APSB is dedicated to disseminating significant original research articles, rapid communications, and high-quality reviews that highlight recent advances across various pharmaceutical sciences domains. These encompass pharmacology, pharmaceutics, medicinal chemistry, natural products, pharmacognosy, pharmaceutical analysis, and pharmacokinetics. A part of the Acta Pharmaceutica Sinica series, established in 1953 and indexed in prominent databases like Chemical Abstracts, Index Medicus, SciFinder Scholar, Biological Abstracts, International Pharmaceutical Abstracts, Cambridge Scientific Abstracts, and Current Bibliography on Science and Technology, APSB is sponsored by the Institute of Materia Medica, Chinese Academy of Medical Sciences, and the Chinese Pharmaceutical Association. Its production and hosting are facilitated by Elsevier B.V. This collaborative effort ensures APSB's commitment to delivering valuable contributions to the pharmaceutical sciences community.
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