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    Identification of Lauric Acid as a Potent Sodium Channel NaV1.5 Blocker from Compound Chinese Medicine Wenxin Keli by Xie W, Gao J, Liang Y, Huang C, Zhang B, Chen X, Yao X, Nan G, Wu H, Wang Y, Wu L, Wang T, Zhu Y

    Published 2025-01-01
    “…Mechanistically, lauric acid acts on the fast inactivation of NaV 1.5 alter electrophysiology conduction of hiPSC-derived cardiomyocytes and contribute to the antiarrhythmic effect of WXKL.Conclusion: Lauric acid is a potent blocker for sodium channel NaV 1.5 and alleviates arrhythmia via inhibiting INa. …”
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    ZSH‐2208: A novel retinoid with potent anti‐tumour effects on ESCC stem cells via RARγ–TNFAIP3 axis by Ruoxue Chen, Xuan Huang, Jiayun Hou, Junjie Ni, Wenrui Zhao, Quanlin Li, Heng Jiao, Xin Cao

    Published 2025-01-01
    “…Therefore, our team developed a series of novel retinoids that target retinoic acid receptors (RARs), with enhanced potency, broader efficacy and minimised toxic side effects against CSCs. …”
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    Study on SHP2 Conformational Transition and Structural Characterization of Its High-Potency Allosteric Inhibitors by Molecular Dynamics Simulations Combined with Machine Learning by Baerlike Wujieti, Mingtian Hao, Erxia Liu, Luqi Zhou, Huanchao Wang, Yu Zhang, Wei Cui, Bozhen Chen

    Published 2024-12-01
    “…These studies not only enhance our understanding of SHP2’s conformational switch mechanism but also offer crucial insights for designing potent allosteric SHP2 inhibitors and addressing drug resistance issues.…”
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  19. 279

    New Approach Methodologies (NAMs) to assess killer whale (Orcinus orca) estrogen receptor alpha (ERα) transactivation potencies by DDTs and their risks by Dave Arthur R. Robledo, Takahito Kumagawa, Mari Ochiai, Hisato Iwata

    Published 2025-02-01
    “…This study aimed to assess kwERα transactivation potencies in response to various DDTs (p,p′-DDT, o,p′-DDT, p,p′-DDD, o,p′-DDD, p,p′-DDE, o,p′-DDE, and p,p′-DDOH) by New Approach Methodologies (NAMs). …”
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    WY-14643, a Potent Peroxisome Proliferator Activator Receptor-α PPAR-α Agonist Ameliorates the Inflammatory Process Associated to Experimental Periodontitis by Enrico Briguglio, Rosanna Di Paola, Irene Paterniti, Emanuela Mazzon, Giacomo Oteri, Giancarlo Cordasco, Salvatore Cuzzocrea

    Published 2010-01-01
    “…We have investigated the effects of WY14643, a potent peroxisome proliferator activator receptor-α (PPAR-α) agonist, in a rat model of ligature-induced periodontitis. …”
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