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Emerging trends in small molecule inhibitors targeting aldosterone synthase: A new paradigm in cardiovascular disease treatment

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资源类型：
Pubmed体系：
作者：
Guo Cuiyu[1,2] ; Zhang Guangbing[3] ; Wu Chengyong[1,2] ; Lei Yi[4] ; Wang Yuxi[2] ; Yang Jinliang[1,5,*1] ;
机构： [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, Sichuan, China [2]Department of Pulmonary and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China [3]Frontier Innovation Center for Dental Medicine Plus, West China Hospital of Stomatology, Sichuan University, Chengdu, 610041, Sichuan, China [4]General Practice Ward/International Medical Center Ward, General Practice Medical Center, General Practice Research Institute, West China Hospital, Sichuan University, China [5]Research Unit of Gene and Immunotherapy, Chinese Academy of Medical Sciences, Chengdu, 610041, Sichuan, China
出处：
DOI： 10.1016/j.ejmech.2024.116521
ISSN：

关键词： Aldosterone synthase inhibitors CYP11B2 Drug design SAR

摘要：
Aldosterone synthase (CYP11B2) is the rate-limiting enzyme in aldosterone production. In recent years, CYP11B2 has become an appealing target for treating conditions associated with excess aldosterone, such as hypertension, heart failure, and cardiometabolic diseases. Several small-molecule inhibitors of CYP11B2 have demonstrated efficacy in both preclinical studies and clinical trials. Among them, the tetrahydroisoquinoline derivative Baxdrostat has entered clinical trial phases and demonstrated efficacy in treating patients with hypertension. However, the high homology (>93 %) between CYP11B2 and steroid-11β-hydroxylase (CYP11B1), which catalyzes cortisol production, implies that insufficient drug specificity can lead to severe side effects. Developing selective inhibitors for CYP11B2 remains a considerable challenge that requires ongoing attention. This review summarizes recent research progress on small-molecule inhibitors targeting CYP11B2, focusing on structure-activity relationships (SAR) and structural optimization. It discusses strategies for enhancing the specificity and inhibitory activity of inhibitors, while also exploring potential applications and future prospects for CYP11B2 inhibitors, providing a theoretical foundation for developing the new generation of CYP11B2-targeted medications.Copyright © 2024 Elsevier Masson SAS. All rights reserved.

基金：
This review was supported by Research Unit of Gene and Immunotherapy, Chinese Academy of Medical Sciences (No. 2019RU067).
语种：
外文
PubmedID：
中科院(CAS)分区：
出版当年[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
最新[2023]版：
大类 | 2 区 医学
小类 | 1 区 药物化学
第一作者：
第一作者机构： [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, Sichuan, China [2]Department of Pulmonary and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Research Center, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China
共同第一作者：
通讯作者：
通讯机构： [1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, Sichuan, China [5]Research Unit of Gene and Immunotherapy, Chinese Academy of Medical Sciences, Chengdu, 610041, Sichuan, China [*1]State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, West China Medical School, Sichuan University, Chengdu, 610041, Sichuan, China.
推荐引用方式(GB/T 7714)：
Guo Cuiyu,Zhang Guangbing,Wu Chengyong,et al.Emerging trends in small molecule inhibitors targeting aldosterone synthase: A new paradigm in cardiovascular disease treatment[J].European Journal Of Medicinal Chemistry.2024,274:116521.doi:10.1016/j.ejmech.2024.116521.
APA：
Guo Cuiyu,Zhang Guangbing,Wu Chengyong,Lei Yi,Wang Yuxi&Yang Jinliang.(2024).Emerging trends in small molecule inhibitors targeting aldosterone synthase: A new paradigm in cardiovascular disease treatment.European Journal Of Medicinal Chemistry,274,
MLA：
Guo Cuiyu,et al."Emerging trends in small molecule inhibitors targeting aldosterone synthase: A new paradigm in cardiovascular disease treatment".European Journal Of Medicinal Chemistry 274.(2024):116521

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