Article
Pharmacology & Pharmacy
Yoshihiro Kobashigawa, Mana Namikawa, Mitsuhiro Sekiguchi, Yuki Inada, Soichiro Yamauchi, Yuu Kimoto, Kyo Okazaki, Yuya Toyota, Takashi Sato, Hiroshi Morioka
Summary: The constitutive active/androstane receptor (CAR) is a nuclear receptor involved in drug metabolism regulation. A novel system was developed for rapid evaluation of drug interactions with CAR, using differential scanning fluorometry (DSF) to confirm direct interactions. This method is easy to set up and beneficial for drug discovery purposes.
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2021)
Article
Nutrition & Dietetics
Dicson Sheeja Malar, Mani Iyer Prasanth, Kanika Verma, Anchalee Prasansuklab, Tewin Tencomnao
Summary: In this study, the mode of toxicity of Phenanthrene (Phe) in human keratinocytes was investigated, along with the protective effect of the ethanol extract of Hibiscus sabdariffa calyxes (HS). The results showed that Phe induced cytotoxicity through CAR/PXR/RXR-mediated activation of CYP1A1, leading to alterations in phase I and II metabolism genes. However, pre-treatment with HS extract inhibited CYP1A1 and attenuated the pathological changes caused by Phe exposure.
Article
Medicine, Research & Experimental
Sydney Stern, Dongdong Liang, Linhao Li, Ritika Kurian, Caitlin Lynch, Srilatha Sakamuru, Scott Heyward, Junran Zhang, Kafayat Ajoke Kareem, Young Wook Chun, Ruili Huang, Menghang Xia, Charles C. Hong, Fengtian Xue, Hongbing Wang
Summary: CN06 is a dual activator of CAR and Nrf2, enhancing the bioactivation of CPA and decreasing the cytotoxicity of DOX in vitro. In a multicellular coculture model, CN06 increased the toxicity of CPA/DOX towards TNBC cells, while protecting cardiomyocytes from DOX-induced cardiotoxicity by selectively activating Nrf2-antioxidant signaling.
Review
Cell Biology
Leonida Rakateli, Rosanna Huchzermeier, Emiel P. C. van der Vorst
Summary: Xenobiotic receptors play a crucial role in both chemical sensing and detoxification as well as lipid metabolism regulation, particularly in relation to dyslipidemia.
Review
Agriculture, Multidisciplinary
Jia Yu, Haoyang Zou, Tiehua Zhang, Jie Zhang
Summary: This review examines the molecular mechanisms by which non-phthalate plasticizers modulate nuclear receptor activity, emphasizing the importance of evaluating their endocrine-disrupting effects and laying the foundation for the development of safer alternatives within the plastic industry.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Hangxing Huang, Change Cao, Zhimin Miao, Xiaoli Yang, Yong Lai
Summary: In this study, it was found that scutellarin can affect the expression of CYP3A4 and CYP2C19 in HepG2 and Caco-2 cells by regulating nuclear receptors PXR and CAR. Scutellarin inhibits the expression of CYP3A4 through PXR, and up-regulates CYP2C19 through CAR.
CURRENT MOLECULAR PHARMACOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Cassandra Winz, Wei-Xing Zong, Nanjoo Suh
Summary: Endocrine-disrupting chemicals, due to their structural similarity to hormones like estrogen, can interfere with endocrine signaling and contribute to the development of breast cancer. They may dysregulate cell signaling pathways related to cellular metabolism, which play a role in cancer progression. Studying these altered pathways through metabolomic analysis can provide insights into the mechanisms by which these chemicals promote breast cancer development.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2023)
Article
Endocrinology & Metabolism
Ronald Biemann, Matthias Blueher, Berend Isermann
Summary: Research shows that endocrine-disrupting compounds may play a role in the obesity epidemic, especially when prenatal exposure affects metabolism and leads to obesity in later generations.
BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM
(2021)
Article
Pharmacology & Pharmacy
Maike Gaehrs, Dieter Schrenk
Summary: NDL-PCBs can suppress UV-induced apoptosis in rat hepatocytes by activating CAR and PXR, and the effects on apoptosis by CAR or PXR activators are specific to CAR or PXR.
Article
Food Science & Technology
Yuan Liang, Qiuyan Jiang, Yiyao Gong, Yifan Yu, Haoyang Zou, Jingqi Zhao, Tiehua Zhang, Jie Zhang
Summary: As a promiscuous xenobiotic receptor, PXR participates in various physiological processes. It serves as an alternative target for environmental chemical contaminants. This study reveals the endocrine disrupting effects of typical food contaminants through PXR-mediated signaling.
FOOD AND CHEMICAL TOXICOLOGY
(2023)
Article
Environmental Sciences
Eepsita Priyadarshini, Ajith Manayil Parambil, Paulraj Rajamani, Vinoth Kumar Ponnusamy, Yi-Hsun Chen
Summary: Endocrine-disrupting compounds (EDC) are exogenous chemicals that mimic hormones and interfere with hormonal signaling, leading to adverse health effects. This review examines the scientific literature from 1990 to 2023, discussing EDC exposure, molecular mechanisms, and toxicological effects on biological systems. The need for alternative techniques to identify and estimate EDC is emphasized, with a focus on in vitro detection methods and the potential of designing nano-architectonic-sensor substrates for on-site detection in contaminated aqueous environments.
ENVIRONMENTAL RESEARCH
(2023)
Article
Environmental Sciences
Chi Zhang, Jinqiu Wu, Qinchang Chen, Haoyue Tan, Fuyan Huang, Jing Guo, Xiaowei Zhang, Hongxia Yu, Wei Shi
Summary: This study systematically summarizes the allosteric interactions between different EDCs and NRs, focusing on drugs belonging to the PPCP class, and discusses the advantages and hurdles of this new mechanism. Additionally, two strategies for virtual screening of numerous EDCs are highlighted, aiming to drive high-throughput and accurate screening of potential EDCs with non-competitive effects.
ENVIRONMENT INTERNATIONAL
(2022)
Article
Pharmacology & Pharmacy
Han Li, Yu-Guang Wang, Zeng-Chun Ma, Gao Yun-Hang, Song Ling, Chen Teng-Fei, Zhang Guang-Ping, Yue Gao
Summary: The research established stable AhR, CAR, and PXR-responsive HepG2 cell lines for rapid screening of CYP450 enzyme induction and validated their response to different inducers. There was a positive correlation between the induction activities and endogenous CYP mRNA expression.
Article
Biochemistry & Molecular Biology
Yue Leng, Yonghai Sun, Wei Huang, Chengyu Lv, Jingyan Cui, Tiezhu Li, Yongjun Wang
Summary: The study showed that dicyclohexyl phthalate (DCHP) acts as a GR antagonist in vitro, exerting endocrine effects by inhibiting GR nuclear translocation and gene expression.
MOLECULAR BIOLOGY REPORTS
(2021)
Article
Pharmacology & Pharmacy
Yabing Du, Xiaoyi Shi, Wang Ma, Peihao Wen, Pu Yu, Xin Wang, Pengli Fang, Aixia Chen, Zhiqiang Gao, Kang Cui
Summary: Phthalates, considered endocrine-disrupting chemicals, play a role in hepatocellular carcinoma cells by enhancing the interaction between pregnane X receptor and E26 transformation specific sequence 1, leading to the activation of invasion-related ETS-1 target genes. This study reveals a novel mechanism for the role of PAEs in cancer progression and sheds light on the extended roles of endocrine-disrupting chemicals in regulating human malignancies.
PHARMACOLOGICAL RESEARCH
(2021)