Review
Cardiac & Cardiovascular Systems
Rajiv Agarwal, Peter Kolkhof, George Bakris, Johann Bauersachs, Hermann Haller, Takashi Wada, Faiez Zannad
Summary: This review covers the development of mineralocorticoid receptor antagonists (MRAs) over the last 80 years, discussing the differences in mechanisms and effects between nonsteroidal and steroidal MRAs. Nonsteroidal MRAs demonstrate important distinctions in distribution, binding mode, and gene expression compared to steroidal MRAs.
EUROPEAN HEART JOURNAL
(2021)
Review
Cardiac & Cardiovascular Systems
Rajiv Agarwal, Peter Kolkhof, George Bakris, Johann Bauersachs, Hermann Haller, Takashi Wada, Faiez Zannad
Summary: This review summarizes the development of mineralocorticoid receptor antagonists over the past 80 years, focusing on the mechanisms of action and advantages of nonsteroidal MRAs.
EUROPEAN HEART JOURNAL
(2021)
Review
Endocrinology & Metabolism
Gianluigi Savarese, Felix Lindberg, Gerasimos Filippatos, Javed Butler, Stefan D. Anker
Summary: The overactivation of mineralocorticoid receptors affects multiple physiological systems, and the use of classical MR antagonists has shown improvements in heart failure. However, concerns about side effects and limited tolerability have hindered their implementation in other settings. Non-steroidal MR antagonists have shown potential benefits and better safety profiles. This review provides an overview of the impact of MR overactivation and discusses the potential of non-steroidal MR antagonists.
Article
Biochemistry & Molecular Biology
F. Saritha, N. Aiswarya, R. Aswath Kumar, K. V. Dileep
Summary: Uterine fibroids are benign smooth muscle tumors that significantly impact women's quality of life. Traditional treatments have high recurrence rates and selective progesterone receptor modulators have been withdrawn due to side effects. Therefore, there is a need for novel, highly efficient, and low side effect therapeutics for the treatment of uterine fibroids.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Multidisciplinary
Xin Chai, Xue-ping Hu, Xin-yue Wang, Hua-ting Wang, Jin-ping Pang, Wen-fang Zhou, Jia-ning Liao, Lu-hu Shan, Xiao-hong Xu, Lei Xu, Hong-guang Xia, Ting-jun Hou, Dan Li
Summary: This study discovered an AR-GR dual binder H18 and identified the AR-GR dual antagonist HD57 with antagonistic activity towards both AR and GR. It provides an efficient and rational strategy for discovering novel AR-GR dual antagonists and important clues for developing new therapeutics for castration-resistant PCa.
ACTA PHARMACOLOGICA SINICA
(2023)
Review
Oncology
Juberiya M. Azeez, Thachapillil Ramakrishnan Susmi, Viji Remadevi, Vini Ravindran, Anjana Sasikumar Sujatha, Raveendran Nair Sobha Ayswarya, Sreeharshan Sreeja
Summary: Progesterone, an ovarian steroid hormone, plays a crucial role in regulating biological processes in various tissues. Understanding its role in diseases, particularly breast cancer, is a topic of debate due to conflicting evidence. Further research is needed to explore how progesterone affects breast cancer progression and its impact on different molecular pathways.
AMERICAN JOURNAL OF CANCER RESEARCH
(2021)
Review
Obstetrics & Gynecology
Kathryn L. Shaia, Benjamin S. Harris, Jessica H. Selter, Thomas M. Price
Summary: The classic transcriptional regulation by nuclear progesterone receptors A and B has been well-studied, but the mitochondrial progesterone receptor (PR-M) responsible for non-nuclear activities has received less attention. PR-M, derived from the progesterone receptor gene, binds to the mitochondrial outer membrane and increases cellular respiration to meet the metabolic demands of pregnancy, spermatozoa activation, and myometrial growth. Its presence may play a role in extended gestation and brain development in primates.
REPRODUCTIVE SCIENCES
(2023)
Review
Food Science & Technology
Jie Zhang, Petr Pavek, Rajamanikkam Kamaraj, Li Ren, Tiehua Zhang
Summary: As a review, this paper summarizes the types and mechanisms of plant-derived pregnane X receptor (PXR) modulators and provides crystal structure information related to PXR binding. Furthermore, it summarizes the agonists, partial agonists, and antagonists of PXR from botanical sources. Further research is needed to screen more plant-derived PXR antagonists for antagonizing PXR function.
CRITICAL REVIEWS IN FOOD SCIENCE AND NUTRITION
(2023)
Article
Biochemistry & Molecular Biology
Jing Qin, Sifeng Qu, Kongkai Zhu, Yahong Cheng, Ge Pan, Weiqiang Jing, Xigong Liu, Xia Sun, Lei Liu
Summary: Novel non-steroidal PR antagonists with potent anti-cancer efficacy were synthesized using a metal-free oxidative C-H arylation method. Compounds 32 and 34 showed significant inhibition of MCF-7 cell proliferation, inducing cell cycle arrest and apoptosis through activation of p53 pathway. These derivatives also exhibited potent PR antagonistic activity and may serve as potential anti-cancer drug candidates for breast cancer therapy.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Review
Medicine, General & Internal
Luca Di Lullo, Carlo Lavalle, Alessia Scatena, Marco Valerio Mariani, Claudio Ronco, Antonio Bellasi
Summary: Chronic kidney disease (CKD) is a common complication of diabetes mellitus and a risk factor for cardiovascular disease. Current medications have not effectively reduced the risk associated with CKD and type 2 diabetes due to inflammation and fibrosis. This review discusses the differences between finerenone and other treatments, as well as potential therapeutic combinations.
JOURNAL OF CLINICAL MEDICINE
(2023)
Article
Chemistry, Medicinal
Xueping Hu, Jinping Pang, Changwei Chen, Dejun Jiang, Chao Shen, Xin Chai, Liu Yang, Xujun Zhang, Lei Xu, Sunliang Cui, Tingjun Hou, Dan Li
Summary: This study identified a group of selective glucocorticoid receptor modulators (SGRMs) through virtual screening, which showed good transrepression activity without transactivation activity, suggesting their potential as novel anti-inflammatory drugs.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Fateme Zare, Aida Solhjoo, Hossein Sadeghpour, Amirhossein Sakhteman, Ali Dehshahri
Summary: Glucocorticoids have wide therapeutic effects but are limited by side effects. This study identified three novel compounds with potential glucocorticoid effects through virtual screening and molecular docking. Molecular dynamics simulations confirmed their binding stability.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Oncology
Danian Dai, Hongmei Wu, Hongkai Zhuang, Rong Chen, Cheng Long, Bo Chen
Summary: This study investigated the clinical and genetic characteristics of ER + / PR- breast cancer patients in China. Different PR statuses indicated diverse biological processes of ER + breast cancer and survival outcomes. Tailored treatment strategies may be needed for ER + / PR- patients.
Review
Nutrition & Dietetics
Edmund Przegalinski, Kacper Witek, Karolina Wydra, Jolanta H. Kotlinska, Malgorzata Filip
Summary: Obesity is a significant health and economic issue, and the serotonin system, specifically the 5-HT2C receptors, plays a crucial role in regulating body weight. This review focuses on the use of 5-HT2C receptor agonists as antiobesity medications, such as fenfluramines, sibutramine, and lorcaserin, and discusses the potential of 5-HT2C receptor positive allosteric modulators as safer alternatives. More research is needed to determine the efficacy of these drugs in obesity prevention and treatment.
Article
Biochemistry & Molecular Biology
Takeshi Tenno, Kohki Kataoka, Natsuko Goda, Hidekazu Hiroaki
Summary: The article discusses the potential application of select non-steroidal anti-inflammatory drugs as tight junction modulators by regulating the PDZ domain of zonula occludens-1. This can lead to decreased epithelial barrier function and improved paracellular absorption of drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
