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  1. No Access

    Article

    FXR activation remodels hepatic and intestinal transcriptional landscapes in metabolic dysfunction-associated steatohepatitis

    The escalating obesity epidemic and aging population have propelled metabolic dysfunction-associated steatohepatitis (MASH) to the forefront of public health concerns. The activation of FXR shows promise to co...

    Ying-quan Wen, Zi-yuan Zou, Guan-guan Zhao, Meng-jiao Zhang in Acta Pharmacologica Sinica (2024)

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    Article

    ErbB4 deficiency exacerbates olfactory dysfunction in an early-stage Alzheimer’s disease mouse model

    Olfactory dysfunction is increasingly recognized as an early indicator of Alzheimer’s disease (AD). Aberrations in GABAergic function and the excitatory/inhibitory (E/I) balance within the olfactory bulb (OB) ...

    **an-hua Deng, **ng-yang Liu, Yi-hua Wei, Ke Wang in Acta Pharmacologica Sinica (2024)

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    Article

    Discovery of a selective TRF2 inhibitor FKB04 induced telomere shortening and senescence in liver cancer cells

    Telomere repeat binding factor 2 (TRF2), a critical element of the shelterin complex, plays a vital role in the maintenance of genome integrity. TRF2 overexpression is found in a wide range of malignant cancer...

    Yin-da Qiu, Qi Yan, Yi Wang, Yan-fei Ye, Yan Wang in Acta Pharmacologica Sinica (2024)

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    Article

    CircNSD1 promotes cardiac fibrosis through targeting the miR-429-3p/SULF1/Wnt/β-catenin signaling pathway

    Cardiac fibrosis is a detrimental pathological process, which constitutes the key factor for adverse cardiac structural remodeling leading to heart failure and other critical conditions. Circular RNAs (circRNA...

    Dong-ni Ji, Sai-di **, Yuan Jiang, Fei-yong Xu, Shu-wei Fan in Acta Pharmacologica Sinica (2024)

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    Article

    Phenethyl isothiocyanate inhibits metastasis potential of non-small cell lung cancer cells through FTO mediated TLE1 m6A modification

    N6-methyladenosine (m6A) modification is a prevalent RNA epigenetic modification, which plays a crucial role in tumor progression including metastasis. Isothiocyanates (ITCs) are natural compounds and inhibit the...

    Qi-cheng Zhang, Yong-mei Qian, Ying-hui Ren, Meng-meng Chen in Acta Pharmacologica Sinica (2024)

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    Article

    COX17 restricts renal fibrosis development by maintaining mitochondrial copper homeostasis and restoring complex IV activity

    Renal fibrosis relies on multiple proteins and cofactors in its gradual development. Copper is a cofactor of many enzymes involved in renal microenvironment homeostasis. We previously reported that intracellul...

    Sai-ya Zhu, Wen-qian Zhou, Yang-yang Niu, Chao Zheng, ** Liu in Acta Pharmacologica Sinica (2023)

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    Article

    Celastrol attenuates hepatitis C virus translation and inflammatory response in mice by suppressing heat shock protein 90β

    Hepatitis C virus (HCV) infection is one of the major factors to trigger a sustained hepatic inflammatory response and hence hepatocellular carcinoma (HCC), but direct-acting-antiviral (DAAs) was not efficient...

    Shao-ru Chen, Zheng-qing Li, Jun Xu, Mo-yu Ding, Ya-ming Shan in Acta Pharmacologica Sinica (2023)

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    Article

    Discovery and characterization of a novel cGAS covalent inhibitor for the treatment of inflammatory bowel disease

    Cyclic GMP-AMP synthase (cGAS), a cytosolic DNA sensor, acts as a nucleotidyl transferase that catalyzes ATP and GTP to form cyclic GMP-AMP (cGAMP) and plays a critical role in innate immunity. Hyperactivation...

    Jia Song, Rui-rui Yang, Jie Chang, Ya-dan Liu, Cheng-hao Lu in Acta Pharmacologica Sinica (2023)

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    Article

    Discovery and identification of a novel small molecule BCL-2 inhibitor that binds to the BH4 domain

    The B-cell lymphoma 2 (BCL-2) protein family plays a pivotal role in regulating the apoptosis process. BCL-2, as an antiapoptotic protein in this family, mediates apoptosis resistance and is an ideal target fo...

    **g-yi Zhou, Rui-rui Yang, Jie Chang, Jia Song, Zi-sheng Fan in Acta Pharmacologica Sinica (2023)

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    Article

    PRMT5 confers lipid metabolism reprogramming, tumour growth and metastasis depending on the SIRT7-mediated desuccinylation of PRMT5 K387 in tumours

    The protein arginine methyltransferase 5 (PRMT5), which is highly expressed in tumour tissues, plays a crucial role in cancer development. However, the mechanism by which PRMT5 promotes cancer growth is poorly...

    Hong-feng Yuan, Man Zhao, Li-na Zhao, Hao-lin Yun, Guang Yang in Acta Pharmacologica Sinica (2022)

  11. Article

    Open Access

    NFAT inhibitor 11R-VIVIT ameliorates mouse renal fibrosis after ischemia-reperfusion-induced acute kidney injury

    Acute kidney injury (AKI) with maladaptive tubular repair leads to renal fibrosis and progresses to chronic kidney disease (CKD). At present, there is no curative drug to interrupt AKI-to-CKD progression. The ...

    Zhi-yong **e, Wei Dong, Li Zhang, Meng-jie Wang in Acta Pharmacologica Sinica (2022)

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    Article

    Novel treatment for refractory rheumatoid arthritis with total glucosides of paeony and nobiletin codelivered in a self-nanoemulsifying drug delivery system

    Patients with refractory rheumatoid arthritis (RA) remain a substantial clinical problem, while the overexpression of P-glycoprotein (P-gp) on their lymphocytes may contribute to resistance to anti-rheumatic d...

    Biao Qu, **ao-lin Wang, De-chong Zheng, Chu-tian Mai in Acta Pharmacologica Sinica (2022)

  13. Article

    Author Correction: CDER167, a dual inhibitor of URAT1 and GLUT9, is a novel and potent uricosuric candidate for the treatment of hyperuricemia

    Ze-an Zhao, Yu Jiang, Yan-yu Chen, Ting Wu, Qun-sheng Lan in Acta Pharmacologica Sinica (2022)

  14. No Access

    Article

    IFN-α inhibits HBV transcription and replication by promoting HDAC3-mediated de-2-hydroxyisobutyrylation of histone H4K8 on HBV cccDNA minichromosome in liver

    The epigenetic modification of hepatitis B virus (HBV) covalently closed circular DNA (cccDNA) plays a crucial role in cccDNA transcription and viral persistence. Interferon-α (IFN-α) is a pivotal agent agains...

    Li-na Zhao, Hong-feng Yuan, Yu-fei Wang, Hao-lin Yun in Acta Pharmacologica Sinica (2022)

  15. No Access

    Article

    CDER167, a dual inhibitor of URAT1 and GLUT9, is a novel and potent uricosuric candidate for the treatment of hyperuricemia

    Urate transporter 1 (URAT1) and glucose transporter 9 (GLUT9) are important targets for the development of uric acid-lowering drugs. We previously showed that the flexible linkers of URAT1 inhibitors could enh...

    Ze-an Zhao, Yu Jiang, Yan-yu Chen, Ting Wu, Qun-sheng Lan in Acta Pharmacologica Sinica (2022)

  16. No Access

    Article

    MicroRNA-17-3p suppresses NF-κB-mediated endothelial inflammation by targeting NIK and IKKβ binding protein

    Nuclear factor kappa B (NF-κB) activation contributes to many vascular inflammatory diseases. The present study tested the hypothesis that microRNA-17-3p (miR-17-3p) suppresses the pro-inflammatory responses v...

    Yin Cai, Yu Zhang, Hui Chen, **ng-hui Sun, Peng Zhang in Acta Pharmacologica Sinica (2021)

  17. No Access

    Article

    Inhibition of miR-135a-5p attenuates vascular smooth muscle cell proliferation and vascular remodeling in hypertensive rats

    Proliferation of vascular smooth muscle cells (VSMCs) greatly contributes to vascular remodeling in hypertension. This study is to determine the roles and mechanisms of miR-135a-5p intervention in attenuating ...

    Chao Ye, Ying Tong, Nan Wu, Guo-wei Wan, Fen Zheng in Acta Pharmacologica Sinica (2021)

  18. No Access

    Article

    Lipid/PAA-coated mesoporous silica nanoparticles for dual-pH-responsive codelivery of arsenic trioxide/paclitaxel against breast cancer cells

    Nanomedicine has attracted increasing attention and emerged as a safer and more effective modality in cancer treatment than conventional chemotherapy. In particular, the distinction of tumor microenvironment a...

    Bing-bing Zhang, **ao-jie Chen, Xu-dong Fan, **g-**g Zhu in Acta Pharmacologica Sinica (2021)

  19. No Access

    Article

    β-arrestin 2 is essential for fluoxetine-mediated promotion of hippocampal neurogenesis in a mouse model of depression

    Over the last decade, the roles of β-arrestins in the treatment of neuropsychological diseases have become increasingly appreciated. Fluoxetine is the first selective serotonin reuptake inhibitor developed and...

    Chen-xin Li, Ying Zheng, Hong Zhu, Cheng-wu Li, Zhang He in Acta Pharmacologica Sinica (2021)

  20. No Access

    Article

    LW-213 induces cell apoptosis in human cutaneous T-cell lymphomas by activating PERK–eIF2α–ATF4–CHOP axis

    Cutaneous T-cell lymphoma (CTCL) is characterized by a heterogeneous group of extranodal non-Hodgkin lymphomas, in which monoclonal T lymphocytes infiltrate the skin. LW-213, a derivative of wogonin, was found...

    **ao-xuan Yu, Meng-yuan Zhu, Jia-rong Wang, Hui Li, Po Hu in Acta Pharmacologica Sinica (2021)

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