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  1. Article

    Publisher Correction: E3 ubiquitin ligase UBR5 modulates circadian rhythm by facilitating the ubiquitination and degradation of the key clock transcription factor BMAL1

    Chun-yan Duan, Yue Li, Hao-yu Zhi, Yao Tian, Zheng-yun Huang in Acta Pharmacologica Sinica (2024)

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    Article

    E3 ubiquitin ligase UBR5 modulates circadian rhythm by facilitating the ubiquitination and degradation of the key clock transcription factor BMAL1

    The circadian clock is the inner rhythm of life activities and is controlled by a self-sustained and endogenous molecular clock, which maintains a ~ 24 h internal oscillation. As the core element of the circad...

    Chun-yan Duan, Yue Li, Hao-yu Zhi, Yao Tian, Zheng-yun Huang in Acta Pharmacologica Sinica (2024)

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    Article

    A novel bispecific antibody drug conjugate targeting HER2 and HER3 with potent therapeutic efficacy against breast cancer

    Antibody drug conjugate (ADC) therapy has become one of the most promising approaches in cancer immunotherapy. Bispecific targeting could enhance the efficacy and safety of ADC by improving its specificity, af...

    Hui-fang Zong, ** Li, Lei Han, Lei Wang, Jun-jun Liu in Acta Pharmacologica Sinica (2024)

  4. Article

    Author Correction: Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition

    Kai-long Jiang, Chang-mei Liu, Li-tong Nie, Hai-ni Jiang in Acta Pharmacologica Sinica (2023)

  5. Article

    Long-term passaging of pseudo-typed SARS-CoV-2 reveals the breadth of monoclonal and bispecific antibody cocktails

    The continuous emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants poses challenges to the effectiveness of neutralizing antibodies. Rational design of antibody cocktails is a re...

    Hang Ma, Hui-fang Zong, Jun-jun Liu, Ya-li Yue, Yong Ke in Acta Pharmacologica Sinica (2023)

  6. Article

    Skullcapflavone II, a novel NQO1 inhibitor, alleviates aristolochic acid I-induced liver and kidney injury in mice

    Aristolochic acid I (AAI) is a well established nephrotoxin and human carcinogen. Cytosolic NAD(P)H quinone oxidoreductase 1 (NQO1) plays an important role in the nitro reduction of aristolochic acids, leading...

    Ya-** Dong, Shu-zhen Chen, Hui-si He, Zhuo-ran Sun 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

    Discovery of toxoflavin, a potent IRE1α inhibitor acting through structure-dependent oxidative inhibition

    Inositol-requiring enzyme 1α (IRE1α) is the most conserved endoplasmic reticulum (ER) stress sensor with two catalytic domains, kinase and RNase, in its cytosolic portion. IRE1α inhibitors have been used to im...

    Kai-long Jiang, Chang-mei Liu, Li-tong Nie, Hai-ni Jiang in Acta Pharmacologica Sinica (2023)

  10. Article

    Open Access

    Safety, tolerability, and pharmacokinetics of VV116, an oral nucleoside analog against SARS-CoV-2, in Chinese healthy subjects

    VV116 (JT001) is an oral drug candidate of nucleoside analog against SARS-CoV-2. The purpose of the three phase I studies was to evaluate the safety, tolerability, and pharmacokinetics of single and multiple a...

    Hong-jie Qian, Yu Wang, Meng-qi Zhang, Yuan-chao **e in Acta Pharmacologica Sinica (2022)

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    Article

    Dihydroartemisinin suppresses renal fibrosis in mice by inhibiting DNA-methyltransferase 1 and increasing Klotho

    Renal fibrosis is an unavoidable end result of all forms of progressive chronic kidney diseases (CKD). Discovery of efficacious drugs against renal fibrosis is in crucial need. In a preliminary study we found ...

    Wei Zhou, Min-min Chen, Hui-ling Liu, Zi-lin Si, Wen-hui Wu in Acta Pharmacologica Sinica (2022)

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    Article

    Downregulation of c-Myc expression confers sensitivity to CHK1 inhibitors in hematologic malignancies

    Checkpoint kinase 1 inhibitors (CHK1i) have shown impressive single-agent efficacy in treatment of certain tumors, as monotherapy or potentiators of chemotherapy in clinical trials, but the sensitive tumor typ...

    Kai-long Jiang, Le-xian Tong, Tao Wang, Han-lin Wang in Acta Pharmacologica Sinica (2022)

  13. Article

    Clinical characteristics and related risk factors of disease severity in 101 COVID-19 patients hospitalized in Wuhan, China

    Coronavirus disease 2019 (COVID-19) broke out in December 2019. Due its high morbility and mortality, it is necessary to summarize the clinical characteristics of COVID-19 patients to provide more theoretical ...

    Xue-qing Liu, Shan Xue, Jia-bo Xu, Heng Ge, Qing Mao in Acta Pharmacologica Sinica (2022)

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    Article

    FGF21 Enhances Therapeutic Efficacy and Reduces Side Effects of Dexamethasone in Treatment of Rheumatoid Arthritis

    In order to investigate efficacy of FGF21 combine dexamethasone (Dex) on rheumatoid arthritis (RA) meanwhile reduce side effects of dexamethasone. We used combination therapy (Dex 15 mg/kg + FGF21 0.25 mg/kg, ...

    Xu Sun, Yin-zhuo **e, Yuan-yuan Jiang, Guan-ying Wang, Yu-jia Wang, Yu Mei in Inflammation (2021)

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    Article

    23,24-Dihydrocucurbitacin B promotes lipid clearance by dual transcriptional regulation of LDLR and PCSK9

    23,24-Dihydrocucurbitacin B (designated as C95 in this article) is a cucurbitane triterpenoid that has been shown to possess a variety of pharmacological activities, such as anti-inflammatory and anti-HIV-1 ac...

    Hui-hui Li, Jun Li, **an-**g Zhang, Jiao-meng Li, Cong ** in Acta Pharmacologica Sinica (2020)

  16. Article

    Discovery of potent 2,4-difluoro-linker poly(ADP-ribose) polymerase 1 inhibitors with enhanced water solubility and in vivo anticancer efficacy

    Poly (ADP-ribose) polymerase 1 (PARP1) is overexpressed in a variety of cancers, especially in breast and ovarian cancers; tumor cells that are deficient in breast cancer gene 1/2 (BRCA1/2) are highly sensitive t...

    Wen-hua Chen, Shan-shan Song, Ming-hui Qi, **a-juan Huan in Acta Pharmacologica Sinica (2017)

  17. Article

    The flavonoid TL-2-8 induces cell death and immature mitophagy in breast cancer cells via abrogating the function of the AHA1/Hsp90 complex

    The flavonoid quercetin exhibits significant anticancer activities with few side effects. In the current study, we characterized TL-2-8, a quercetin derivative, as a novel anticancer agent in vitro and in vivo. C...

    Hui-juan Liu, **ao-xiao Jiang, Yi-zhen Guo, Fang-hui Sun in Acta Pharmacologica Sinica (2017)

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    Article

    Foxp3, Regulatory T Cell, and Autoimmune Diseases

    Regulatory T cells (Tregs) represent a cell type that promotes immune tolerance to autologous components and maintains immune system homeostasis. The abnormal function of Tregs is relevant to the pathogenesis ...

    **-Hui Tao, Miao Cheng, Jiang-** Tang, Qin Liu, Fan Pan, **ang-Pei Li in Inflammation (2017)

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    Article

    Artesunate Protects Against Sepsis-Induced Lung Injury Via Heme Oxygenase-1 Modulation

    Artesunate, a derivative of artemisinin, has anti-inflammatory properties and exerts protective roles in sepsis. Heme oxygense-1 (HO-1) inhibits the inflammatory response through reduction of proinflammatory c...

    Tian-hui Cao, Song-gen **, Dong-sheng Fei, Kai Kang, Lei Jiang in Inflammation (2016)

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    Article

    Relationship of Serum Mannose-Binding Lectin Levels with the Development of Sepsis: a Meta-analysis

    Many studies have evaluated the association between serum levels of mannose-binding lectin (MBL) and sepsis; however, the findings are inconclusive and conflicting. For a better understanding of MBL in sepsis,...

    Dong-Na Gao, Yu Zhang, Yan-Bo Ren, Jian Kang, Li Jiang, Zhuo Feng in Inflammation (2015)

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