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Ciclopirox inhibits SARS-CoV-2 replication by promoting the degradation of the nucleocapsid protein Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-12 Xiafei Wei, Yuzheng Zhou, Xiaotong Shen, Lujie Fan, Donglan Liu, Xiang Gao, Jian Zhou, Yezi Wu, Yunfei Li, Wei Feng, Zheng Zhang
The nucleocapsid protein (NP) plays a crucial role in SARS-CoV-2 replication and is the most abundant structural protein with a long half-life. Despite its vital role in severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) assembly and host inflammatory response, it remains an unexplored target for drug development. In this study, we identified a small-molecule compound (ciclopirox) that promotes
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ASF1A-dependent P300-mediated histone H3 lysine 18 lactylation promotes atherosclerosis by regulating EndMT Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-12 Mengdie Dong, Yunjia Zhang, Minghong Chen, Yongkang Tan, Jiao Min, Xian He, Fuhao Liu, Jiaming Gu, Hong Jiang, Longbin Zheng, Jiajing Chen, Quanwen Yin, Xuesong Li, Xiang Chen, Yongfeng Shao, Yong Ji, Hongshan Chen
Endothelial-to-mesenchymal transition (EndMT) is a key driver of atherosclerosis. Aerobic glycolysis is increased in the endothelium of atheroprone areas, accompanied by elevated lactate levels. Histone lactylation, mediated by lactate, can regulate gene expression and participate in disease regulation. However, whether histone lactylation is involved in atherosclerosis remains unknown. Here, we report
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Idebenone alleviates doxorubicin-induced cardiotoxicity by stabilizing FSP1 to inhibit ferroptosis Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-11 Hongliang Qiu, Sihui Huang, Yuting Liu, Libo Liu, Fengming Guo, Yingying Guo, Dan Li, Xianfeng Cen, Yajie Chen, Meng Zhang, Yan Che, Man Xu, Qizhu Tang
Doxorubicin (DOX)-mediated cardiotoxicity can exacerbate mortality in oncology patients, but related pharmacotherapeutic measures are relatively limited. Ferroptosis was recently identified as a major mechanism of DOX-induced cardiotoxicity. Idebenone, a novel ferroptosis inhibitor, is a well-described clinical drug widely used. However, its role and pathological mechanism in DOX-induced cardiotoxicity
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Complications and comorbidities associated with antineoplastic chemotherapy: Rethinking drug design and delivery for anticancer therapy Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-11 Xiaoman Mao, Shuang Wu, Dandan Huang, Chong Li
Despite the considerable advancements in chemotherapy as a cornerstone modality in cancer treatment, the prevalence of complications and pre-existing diseases is on the rise among cancer patients along with prolonged survival and aging population. The relationships between these disorders and cancer are intricate, bearing significant influence on the survival and quality of life of individuals with
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An antibiotic-free platform for eliminating persistent Helicobacter pylori infection without disrupting gut microbiota Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-10 Yongkang Lai, Tinglin Zhang, Xiaojing Yin, Chunping Zhu, Yiqi Du, Zhaoshen Li, Jie Gao
( infection remains the leading cause of gastric adenocarcinoma, and its eradication primarily relies on the prolonged and intensive use of two antibiotics. However, antibiotic resistance has become a compelling health issue, leading to eradication treatment failure worldwide. Additionally, the powerlessness of antibiotics against biofilms, as well as intracellular and the long-term damage of antibiotics
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Disruption of cyclin D1 degradation leads to the development of mantle cell lymphoma Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-10 Ke Lu, Ming Zhang, Hongyu Qin, Siyu Shen, Haiqing Song, Hua Jiang, Chunxiang Zhang, Guozhi Xiao, Liping Tong, Qing Jiang, Di Chen
Cyclin D1 has been recognized as an oncogene due to its abnormal upregulation in different types of cancers. Here, we demonstrated that cyclin D1 is SUMOylated, and we identified Itch as a specific E3 ligase recognizing SUMOylated cyclin D1 and mediating SUMO-induced ubiquitination and proteasome degradation of cyclin D1. We generated cyclin D1 mutant mice with mutations in the SUMOylation site, phosphorylation
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Glucagon-like peptide-1 receptor agonists rescued diabetic vascular endothelial damage through suppression of aberrant STING signaling Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-10 Xuemin He, Siying Wen, Xixiang Tang, Zheyao Wen, Rui Zhang, Shasha Li, Rong Gao, Jin Wang, Yanhua Zhu, Dong Fang, Ting Li, Ruiping Peng, Zhaotian Zhang, Shiyi Wen, Li Zhou, Heying Ai, Yan Lu, Shaochong Zhang, Guojun Shi, Yanming Chen
Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) protect against diabetic cardiovascular diseases and nephropathy. However, their activity in diabetic retinopathy (DR) remains unclear. Our retrospective cohort study involving 1626 T2DM patients revealed superior efficacy of GLP-1 RAs in controlling DR compared to other glucose-lowering medications, suggesting their advantage in DR treatment. By
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Pharmacokinetic enhancement of oncolytic virus M1 by inhibiting JAK‒STAT pathway Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-10 Jingyi Tan, Jiayu Zhang, Cheng Hu, Gongwei Wang, Qianyao Ren, Chaoqun Wang, Jia Dan, Zexin Zeng, Jun Hu, Wenbo Zhu, Jiankai Liang, Jing Cai, Ying Liu, Guangmei Yan, Yuan Lin
Oncolytic viruses (OVs), a group of replication-competent viruses that can selectively infect and kill cancer cells while leaving healthy cells intact, are emerging as promising living anticancer agents. Unlike traditional drugs composed of non-replicating compounds or biomolecules, the replicative nature of viruses confer unique pharmacokinetic properties that require further studies. Despite some
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Dendritic nanomedicine enhances chemo-immunotherapy by disturbing metabolism of cancer-associated fibroblasts for deep penetration and activating function of immune cells Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-09 Yunkun Li, Xiaoding Shen, Haitao Ding, Yuxin Zhang, Dayi Pan, Liping Su, Yahui Wu, Zaixiang Fang, Jie Zhou, Qiyong Gong, Kui Luo
Inefficient drug penetration hurdled by the stroma in the tumor tissue leads to a diminished therapeutic effect for drugs and a reduced infiltration level of immune cells. Herein, we constructed a PEGylated dendritic epirubicin (Epi) prodrug (Epi-P4D) to regulate the metabolism of cancer-associated fibroblasts (CAFs), thus enhancing Epi penetration into both multicellular tumor spheroids (MTSs) and
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A novel marine-derived anti-acute kidney injury agent targeting peroxiredoxin 1 and its nanodelivery strategy based on ADME optimization Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-08 Ping Yu, Tanwei Gu, Yueyang Rao, Weimin Liang, Xi Zhang, Huanguo Jiang, Jindi Lu, Jianglian She, Jianmin Guo, Wei Yang, Yonghong Liu, Yingfeng Tu, Lan Tang, Xuefeng Zhou
Insufficient therapeutic strategies for acute kidney injury (AKI) necessitate precision therapy targeting its pathogenesis. This study reveals the new mechanism of the marine-derived anti-AKI agent, piericidin glycoside S14, targeting peroxiredoxin 1 (PRDX1). By binding to Cys83 of PRDX1 and augmenting its peroxidase activity, S14 alleviates kidney injury efficiently in -overexpression (-OE) mice.
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M1-polarized macrophage-derived cellular nanovesicle-coated lipid nanoparticles for enhanced cancer treatment through hybridization of gene therapy and cancer immunotherapy Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-07 Ha Eun Shin, Jun-Hyeok Han, Seungyong Shin, Ga-Hyun Bae, Boram Son, Tae-Hyung Kim, Hee Ho Park, Chun Gwon Park, Wooram Park
Optimum genetic delivery for modulating target genes to diseased tissue is a major obstacle for profitable gene therapy. Lipid nanoparticles (LNPs), considered a prospective vehicle for nucleic acid delivery, have demonstrated efficacy in human use during the COVID-19 pandemic. This study introduces a novel biomaterial-based platform, M1-polarized macrophage-derived cellular nanovesicle-coated LNPs
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In silico off-target profiling for enhanced drug safety assessment Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-06 Jin Liu, Yike Gui, Jingxin Rao, Jingjing Sun, Gang Wang, Qun Ren, Ning Qu, Buying Niu, Zhiyi Chen, Xia Sheng, Yitian Wang, Mingyue Zheng, Xutong Li
Ensuring drug safety in the early stages of drug development is crucial to avoid costly failures in subsequent phases. However, the economic burden associated with detecting drug off-targets and potential side effects through safety screening and animal testing is substantial. Drug off-target interactions, along with the adverse drug reactions they induce, are significant factors affecting drug safety
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Development of an active-site titrant for SARS-CoV-2 main protease as an indispensable tool for evaluating enzyme kinetics Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-06 Rabea Voget, Julian Breidenbach, Tobias Claff, Alexandra Hingst, Katharina Sylvester, Christian Steinebach, Lan Phuong Vu, Renato H. Weiße, Ulrike Bartz, Norbert Sträter, Christa E. Müller, Michael Gütschow
A titrant for the SARS-CoV-2 main protease (M) was developed that enables, for the first time, the exact determination of the concentration of the enzymatically active M by active-site titration. The covalent binding mode of the tetrapeptidic titrant was elucidated by the determination of the crystal structure of the enzyme–titrant complex. Four fluorogenic substrates of M, including a prototypical
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Transcription factor EHF interacting with coactivator AJUBA aggravates malignancy and acts as a therapeutic target for gastroesophageal adenocarcinoma Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-04 Li Peng, Yanyi Jiang, Hengxing Chen, Yongqiang Wang, Qiusheng Lan, Shuiqin Chen, Zhanwang Huang, Jingyuan Zhang, Duanqing Tian, Yuntan Qiu, Diankui Cai, Jiangyun Peng, Daning Lu, Xiaoqing Yuan, Xianzhu Yang, Dong Yin
Transcriptional dysregulation of genes is a hallmark of tumors and can serve as targets for cancer drug development. However, it is extremely challenging to develop small-molecule inhibitors to target abnormally expressed transcription factors (TFs) except for the nuclear receptor family of TFs. Little is known about the interaction between TFs and transcription cofactors in gastroesophageal adenocarcinoma
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Di-PEGylated insulin: A long-acting insulin conjugate with superior safety in reducing hypoglycemic events Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-04 Zhipeng Zeng, Runcheng Tan, Shi Chen, Haolin Chen, Zhijia Liu, Lixin Liu, Mingqiang Li, Yongming Chen
Although the discovery of insulin 100 years ago revolutionized the treatment of diabetes, its therapeutic potential is compromised by its short half-life and narrow therapeutic index. Current long-acting insulin analogs, such as insulin-polymer conjugates, are mainly used to improve pharmacokinetics by reducing renal clearance. However, these conjugates are synthesized without sacrificing the bioactivity
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Sequential dual-locking strategy using photoactivated Pt(IV)-based metallo-nano prodrug for enhanced chemotherapy and photodynamic efficacy by triggering ferroptosis and macrophage polarization Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-04 Jun Li, Qiang Zhang, Hao Yang, Wenli Lu, Yulong Fu, Yingcai Xiong, Xuan Wang, Tianming Lu, Yanlin Xin, Zejuan Xie, Weichao Chen, Guoqiang Wang, Yuanyuan Guo, Ruogu Qi
Selective activation of Pt(IV) prodrugs within tumors has emerged as a promising strategy in tumor treatment. Although progress has been made with photo- and ultrasound-activated Pt(IV) prodrugs, concerns remain over the non-specific activation of photosensitizers (PS) and the potential for phototoxicity and chemical toxicity. In this study, a sequential dual-locked Pt(IV) nano-prodrug that can be
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Glycnsisitin A: A promising bicyclic peptide against heart failure that facilitates TFRC-mediated uptake of iron in cardiomyocytes Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-03 Jichao Zhou, Yuanyuan Liu, Xiaoli Wei, Meng Yuan, Xu Zhang, Lingfeng Qin, Bing Cui, Pingping Li, Jing Zhang, Ziming Feng, Jianshuang Jiang, Xiang Yuan, Ruibing Xu, Zhimeng Zhang, Peicheng Zhang, Xiaowei Zhang, Yanan Yang
Zhigancao decoction is a traditional prescription for treating irregular pulse and palpitations in China. As the monarch drug of Zhigancao decoction, the bioactive molecules of licorice against heart diseases remain elusive. We established the HRESIMS-guided method leading to the isolation of three novel bicyclic peptides, glycnsisitins A–C (–), with distinctive C–C and C–O–C side-chain-to-side-chain
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Carrimycin inhibits coronavirus replication by decreasing the efficiency of programmed –1 ribosomal frameshifting through directly binding to the RNA pseudoknot of viral frameshift-stimulatory element Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-03 Hongying Li, Jianrui Li, Jiayu Li, Hu Li, Xuekai Wang, Jing Jiang, Lei Lei, Han Sun, Mei Tang, Biao Dong, Weiqing He, Shuyi Si, Bin Hong, Yinghong Li, Danqing Song, Zonggen Peng, Yongsheng Che, Jian-Dong Jiang
The pandemic of SARS-CoV-2 worldwide with successive emerging variants urgently calls for small-molecule oral drugs with broad-spectrum antiviral activity. Here, we show that carrimycin, a new macrolide antibiotic in the clinic and an antiviral candidate for SARS-CoV-2 in phase III trials, decreases the efficiency of programmed –1 ribosomal frameshifting of coronaviruses and thus impedes viral replication
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Branched glycopolymer prodrug-derived nanoassembly combined with a STING agonist activates an immuno-supportive status to boost anti-PD-L1 antibody therapy Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-03-02 Zhilin Li, Qianfeng Zhang, Zhiqian Li, Long Ren, Dayi Pan, Qiyong Gong, Zhongwei Gu, Hao Cai, Kui Luo
Despite the great potential of anti-PD-L1 antibodies for immunotherapy, their low response rate due to an immunosuppressive tumor microenvironment has hampered their application. To address this issue, we constructed a cell membrane-coated nanosystem (mB4S) to reverse an immunosuppressive microenvironment to an immuno-supportive one for strengthening the anti-tumor effect. In this system, Epirubicin
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5S-Heudelotinone alleviates experimental colitis by shaping the immune system and enhancing the intestinal barrier in a gut microbiota-dependent manner Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-29 Qing Meng, Jianshuang Guo, Ke Lv, Yang Liu, Jin Zhang, Mingyue Li, Xirui Cheng, Shenghua Chen, Xiaoguang Huo, Quan Zhang, Yue Chen, Jing Li
Aberrant changes in the gut microbiota are implicated in many diseases, including inflammatory bowel disease (IBD). Gut microbes produce diverse metabolites that can shape the immune system and impact the intestinal barrier integrity, indicating that microbe-mediated modulation may be a promising strategy for preventing and treating IBD. Although fecal microbiota transplantation and probiotic supplementation
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Oral peptide therapeutics for diabetes treatment: State-of-the-art and future perspectives Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-28 Bingwen Ding, Zhu Zhu, Cong Guo, Jiaxin Li, Yong Gan, Miaorong Yu
Diabetes, characterized by hyperglycemia, is a major cause of death and disability worldwide. Peptides, such as insulin and glucagon-like peptide-1 (GLP-1) analogs, have shown promise as treatments for diabetes due to their ability to mimic or enhance insulin's actions in the body. Compared to subcutaneous injection, oral administration of anti-diabetic peptides is a preferred approach. However, biological
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Targeting RAF dimers in RAS mutant tumors: From biology to clinic Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-28 Huanhuan Yin, Qiulin Tang, Hongwei Xia, Feng Bi
RAS mutations occur in approximately 30% of tumors worldwide and have a poor prognosis due to limited therapies. Covalent targeting of KRAS G12C has achieved significant success in recent years, but there is still a lack of efficient therapeutic approaches for tumors with non-G12C KRAS mutations. A highly promising approach is to target the MAPK pathway downstream of RAS, with a particular focus on
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Radiation-based immunogenic vaccine combined with a macrophage “checkpoint inhibitor” for boosting innate and adaptive immunity against metastatic colon cancers Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-27 Hongbo Xu, Xianya Qin, Yuanyuan Guo, Siyu Zhao, Xingxing Feng, Runzan Zhang, Tianyi Tian, Li Kong, Conglian Yang, Zhiping Zhang
Immunogenic dying tumor cells hold promising prospects as cancer vaccines to activate systemic immunity against both primary and metastatic tumors. Especially, X-ray- induced dying tumor cells are rich in highly immunogenic tumor-associated antigens and self-generated dsDNA as potent adjuvants. However, we found that the X-ray induction process can result in the excessive exposure of phosphatidylserine
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A combined nanotherapeutic approach targeting farnesoid x receptor, ferroptosis, and fibrosis for nonalcoholic steatohepatitis treatment Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-26 Jiangtao Fu, Pingping Zhang, Zhiguo Sun, Guodong Lu, Qi Cao, Yiting Chen, Wenbin Wu, Jiabao Zhang, Chunlin Zhuang, Chunquan Sheng, Jiajun Xu, Ying Lu, Pei Wang
Obeticholic acid (OCA), a farnesoid X receptor (FXR) agonist with favorable effects on fatty and glucose metabolism, has been considered the leading candidate drug for nonalcoholic steatohepatitis (NASH) treatment. However, its limited effectiveness in resolving liver fibrosis and lipotoxicity-induced cell death remains a major drawback. Ferroptosis, a newly recognized form of cell death characterized
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Genome mining of sulfonated lanthipeptides reveals unique cyclic peptide sulfotransferases Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-26 Meng Wang, Wen-Wei Li, Zhe Cao, Jianong Sun, Jiang Xiong, Si-Qin Tao, Tinghong Lv, Kun Gao, Shangwen Luo, Shi-Hui Dong
Although sulfonation plays crucial roles in various biological processes and is frequently utilized in medicinal chemistry to improve water solubility and chemical diversity of drug leads, it is rare and underexplored in ribosomally synthesized and post-translationally modified peptides (RiPPs). Biosynthesis of RiPPs typically entails modification of hydrophilic residues, which substantially increases
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Targeting PKM2 signaling cascade with salvianic acid A normalizes tumor blood vessels to facilitate chemotherapeutic drug delivery Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-23 Cheng Qian, Yueke Zhou, Teng Zhang, Guanglu Dong, Mengyao Song, Yu Tang, Zhonghong Wei, Suyun Yu, Qiuhong Shen, Wenxing Chen, Jaesung P. Choi, Juming Yan, Chongjin Zhong, Li Wan, Jia Li, Aiyun Wang, Yin Lu, Yang Zhao
Aberrant tumor blood vessels are prone to propel the malignant progression of tumors, and targeting abnormal metabolism of tumor endothelial cells emerges as a promising option to achieve vascular normalization and antagonize tumor progression. Herein, we demonstrated that salvianic acid A (SAA) played a pivotal role in contributing to vascular normalization in the tumor-bearing mice, thereby improving
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Author correction to ‘VEGFR2-targeted antibody fused with IFNamut regulates the tumor microenvironment of colorectal cancer and exhibits potent anti-tumor and anti-metastasis activity’ [Acta Pharmaceutica Sinica B 11 (2021) 420-433] Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-22 Pengzhao Shang, Rui Gao, Yijia Zhu, Xiaorui Zhang, Yang Wang, Minji Guo, Hui Peng, Min Wang, Juan Zhang
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Author correction to ‘Pharmacologically targeting molecular motor promotes mitochondrial fission for anti-cancer’ [Acta Pharmaceutica Sinica B 11 (2021) 1853-1866] Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-21 Yi Qian, Meimei Zhao, Qinghua Han, Jingkang Wang, Lixi Liao, Heng Yang, Dan Liu, Pengfei Tu, Hong Liang, Kewu Zeng
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Spirohypertones A and B as potent antipsoriatics: Tumor necrosis factor-α inhibitors with unprecedented chemical architectures Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-20 Yulin Duan, Weiguang Sun, Yongqi Li, Zhengyi Shi, Lanqin Li, Yeting Zhang, Huang Kun, Zhiping Zhang, Changxing Qi, Yonghui Zhang
Tumor necrosis factor- (TNF-) is a promising target for inflammatory and autoimmune diseases. Spirohypertones A () and B (), two unprecedented polycyclic polyprenylated acylphloroglucinols with highly rearranged skeletons, were isolated from . The structures of and were confirmed through comprehensive spectroscopic analysis, single-crystal X-ray diffraction and electronic circular dichroism calculations
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First total synthesis, antitumor evaluation and target identification of mornaphthoate E: A new tubulin inhibitor template acting on PI3K/Akt signaling pathway Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-19 Peipei Shan, Tao Ye, Ying-De Tang, Hui Song, Chao Wang, Kongkai Zhu, Feifei Yang, Shi-Lei Zhang, Pei-Wen Su, Shuanhu Gao, Hua Zhang
Mornaphthoate E (MPE) is a prenylated naphthoic acid methyl ester isolated from the roots of a famous Chinese medicinal plant and show remarkable cytotoxicity against several human tumor cell lines. In the current project, the first total synthesis of (±)-MPE was achieved in seven steps and 5.6% overall yield. Then the activity of MPE was first assessed for both enantiomers in two breast cancer cells
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Bile acids and coronavirus disease 2019 Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-13 Xiaoru Huang, Xuening Liu, Zijian Li
The coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has been significantly alleviated. However, long-term health effects and prevention strategy remain unresolved. Thus, it is essential to explore the pathophysiological mechanisms and intervention for SARS-CoV-2 infection. Emerging research indicates a link between COVID-19 and bile
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Gas-propelled nanomotors alleviate colitis through the regulation of intestinal immunoenvironment-hematopexis-microbiota circuits Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-12 Bo Xiao, Yuqi Liang, Ga Liu, Lingshuang Wang, Zhan Zhang, Libin Qiu, Haiting Xu, Sean Carr, Xiaoxiao Shi, Rui L. Reis, Subhas C. Kundu, Zhenghua Zhu
The progression of ulcerative colitis (UC) is associated with immunologic derangement, intestinal hemorrhage, and microbiota imbalance. While traditional medications mainly focus on mitigating inflammation, it remains challenging to address multiple symptoms. Here, a versatile gas-propelled nanomotor was constructed by mild fusion of post-ultrasonic CaO nanospheres with CuO nanoblocks. The resulting
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Rhizoma Drynariae-derived nanovesicles reverse osteoporosis by potentiating osteogenic differentiation of human bone marrow mesenchymal stem cells via targeting ERα signaling Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-10 Qing Zhao, Junjie Feng, Fubin Liu, Qianxin Liang, Manlin Xie, Jiaming Dong, Yanfang Zou, Jiali Ye, Guilong Liu, Yue Cao, Zhaodi Guo, Hongzhi Qiao, Lei Zheng, Kewei Zhao
Although various anti-osteoporosis drugs are available, the limitations of these therapies, including drug resistance and collateral responses, require the development of novel anti-osteoporosis agents. Rhizoma Drynariae displays a promising anti-osteoporosis effect, while the effective component and mechanism remain unclear. Here, we revealed the therapeutic potential of Rhizoma Drynariae-derived
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Cisplatin-based miRNA delivery strategy inspired by the circCPNE1/miR-330-3p pathway for oral squamous cell carcinoma Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-10 Hua-yang Fan, Ming-da Zhao, Hong-jie Jiang, Zhen-wei Yu, Yu-jiang Fan, Xin-hua Liang, Ya-ling Tang, Yong Sun
Circular RNAs (circRNAs) are ideal biomarkers of oral squamous cell carcinoma (OSCC) because of their highly stable closed-loop structure, and they can act as microRNA (miRNA) sponges to regulate OSCC progression. By analyzing clinical samples, we identified circCPNE1, a dysregulated circRNA in OSCC, and its expression level was negatively correlated with the clinical stage of OSCC patients. Gain-of-function
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Molecular characterization and structure basis of a malonyltransferase with both substrate promiscuity and catalytic regiospecificity from Cistanche tubulosa Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-10 Xiao Liu, Yuyu Liu, Xiping Xu, Wenqian Huang, Yaru Yan, Yingxia Wang, Weisheng Tian, Ting Mo, Xiaoxue Cui, Jun Li, She-Po Shi, Pengfei Tu
Enzymatic malonylation of natural glycosides provided a promising alternative method for drug-like malonylated glycosides supply. However, the catalytic potential and structural basis of plant malonyltransferase are far from being fully elucidated. This work identified a new malonyltransferase CtMaT1 from It displayed unprecedented mono- and/or di-malonylation activity toward diverse glucosides with
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Directly targeting BAX for drug discovery: Therapeutic opportunities and challenges Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-10 Zhenwei Zhang, Linghui Hou, Dan Liu, Shenglin Luan, Min Huang, Linxiang Zhao
For over two decades, the development of B-cell lymphoma-2 (Bcl-2) family therapeutics has primarily focused on anti-apoptotic proteins, resulting in the first-in-class drugs called BH3 mimetics, especially for Bcl-2 inhibitor Venetoclax. The pro-apoptotic protein Bcl-2-associated X protein (BAX) plays a crucial role as the executioner protein of the mitochondrial regulated cell death, contributing
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ALS-linked C9orf72 dipeptide repeats inhibit starvation-induced autophagy through modulating BCL2-BECN1 interaction Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-07 Shiqiang Xu, Qilian Ma, Junwen Shen, Ningning Li, Shan Sun, Nana Wang, Yang Chen, Chunsheng Dong, Kin Yip Tam, Jochen H.M. Prehn, Hongfeng Wang, Zheng Ying
Growing evidences indicate that dysfunction of autophagy contributes to the disease pathogenesis of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD), two neurodegenerative disorders. The GGGGCC·GGCCCC repeat RNA expansion in chromosome 9 open reading frame 72 () is the most genetic cause of both ALS and FTD. According to the previous studies, GGGGCC·GGCCCC repeat undergoes the
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High-throughput discovery of highly selective reversible hMAO-B inhibitors based on at-line nanofractionation Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-06 Yu Fan, Jincai Wang, Jingyi Jian, Yalei Wen, Jiahao Li, Hao Tian, Jacques Crommen, Wei Bi, Tingting Zhang, Zhengjin Jiang
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Inhalable metal-organic framework-mediated cuproptosis combined with PD-L1 checkpoint blockade for lung metastasis synergistic immunotherapy Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-06 Chongzheng Yan, Ying Liu, Guozhi Zhao, Huatian Yang, Huaiyou Lv, Genju Li, Yuhan Li, Yaqing Fu, Fengqin Sun, Yafei Feng, Yizhe Li, Zhongxi Zhao
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DDAH1 promotes neurogenesis and neural repair in cerebral ischemia Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-06 Qiming Gao, Pinfei Ni, Yilin Wang, Peiyun Huo, Xiaojie Zhang, Sihan Wang, Fuyao Xiao, Yixuan Li, Wei Feng, Juntao Yuan, Teng Zhang, Qiang Li, Boyu Fan, Yuhao Kan, Zhirui Li, Yimiao Qi, Junfei Xing, Zhenghong Yang, Haixiao Cheng, Xinran Gao, Xiaoyan Feng, Ming Xue, Yang Liu, Yumin Luo, Zhongbing Lu, Yuming Zhao
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Enhanced optical imaging and fluorescent labeling for visualizing drug molecules within living organisms Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-05 Ting Sun, Huanxin Zhao, Luyao Hu, Xintian Shao, Zhiyuan Lu, Yuli Wang, Peixue Ling, Yubo Li, Kewu Zeng, Qixin Chen
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Transient induction of actin cytoskeletal remodeling associated with dedifferentiation, proliferation, and redifferentiation stimulates cardiac regeneration Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-03 Wenbin Fu, Qiao Liao, Yu Shi, Wujian Liu, Hongmei Ren, Chunmei Xu, Chunyu Zeng
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Deep simulated annealing for the discovery of novel dental anesthetics with local anesthesia and anti-inflammatory properties Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-02-02 Yihang Hao, Haofan Wang, Xianggen Liu, Wenrui Gai, Shilong Hu, Wencheng Liu, Zhuang Miao, Yu Gan, Xianghua Yu, Rongjia Shi, Yongzhen Tan, Ting Kang, Ao Hai, Yi Zhao, Yihang Fu, Yaling Tang, Ling Ye, Jin Liu, Xinhua Liang, Bowen Ke
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The raphe nuclei are the early lesion site of gastric α-synuclein propagation to the substantia nigra Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-29 Chenglu Zhang, Ruxue Bo, Tiantian Zhou, Naihong Chen, Yuhe Yuan
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Small molecule conjugates with selective estrogen receptor β agonism promote anti-aging benefits in metabolism and skin recovery Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-29 Tarik Zahr, Vijay K. Boda, Jian Ge, Lexiang Yu, Zhongzhi Wu, Jianwen Que, Wei Li, Li Qiang
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Exosomes derived from pulmonary metastatic sites enhance osteosarcoma lung metastasis by transferring the miR-194/215 cluster targeting MARCKS Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-27 Pei Yu, Yubao Han, Lulu Meng, Yanyuan Tian, Zhiwei Jin, Jun Luo, Chao Han, Wenjun Xu, Lingyi Kong, Chao Zhang
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Metal natural product complex Ru-procyanidins with quadruple enzymatic activity combat infections from drug-resistant bacteria Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-26 Jie Shan, Xu Jin, Cong Zhang, Muchen Huang, Jianghao Xing, Qingrong Li, Yuyu Cui, Qiang Niu, Xu Lin Chen, Xianwen Wang
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Engagement of N6-methyladenisine methylation of Gng4 mRNA in astrocyte dysfunction regulated by CircHECW2 Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-22 Ying Bai, Di Chang, Hui Ren, Minzi Ju, Yu Wang, Biling Chen, Han Li, Xue Liu, Daxing Li, Xinchen Huo, Xiaofei Guo, Mengze Tong, Ying Tan, Honghong Yao, Bing Han
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Hyperglycemia activates FGFR1 via TLR4/c-Src pathway to induce inflammatory cardiomyopathy in diabetes Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-22 Xiong Chen, Jinfu Qian, Shiqi Liang, Jianchang Qian, Wu Luo, Yujuan Shi, Hong Zhu, Xiang Hu, Gaojun Wu, Xiaokun Li, Guang Liang
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Endothelial phosphodiesterase 4B inactivation ameliorates endothelial-to-mesenchymal transition and pulmonary hypertension Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-22 Yanjiang Xing, Yangfeng Hou, Tianfei Fan, Ran Gao, Xiaohang Feng, Bolun Li, Junling Pang, Wenjun Guo, Ting Shu, Jinqiu Li, Jie Yang, Qilong Mao, Ya Luo, Xianmei Qi, Peiran Yang, Chaoyang Liang, Hongmei Zhao, Wenhui Chen, Jing Wang, Chen Wang
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Expanding the horizons of targeted protein degradation: A non-small molecule perspective Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-20 Xiaowei Huang, Fengbo Wu, Jing Ye, Lian Wang, Xiaoyun Wang, Xiang Li, Gu He
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Macrophage senescence in health and diseases Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-20 Longling Wang, Wenxiang Hong, Hong Zhu, Qiaojun He, Bo Yang, Jiajia Wang, Qinjie Weng
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Bispecific antibody drug conjugates: Making 1+1>2 Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-20 Yilin Gu, Zhijia Wang, Yuxi Wang
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Oligomerization of drug transporters: Forms, functions, and mechanisms Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-20 Chunxu Ni, Mei Hong
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Blockade of the deubiquitinating enzyme USP48 degrades oncogenic HMGA2 and inhibits colorectal cancer invasion and metastasis Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-17 Can Cheng, Hanhui Yao, Heng Li, Jingwen Liu, Zhengyi Liu, Yang Wu, Liang Zhu, Hejie Hu, Zhengdong Fang, Liang Wu
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Strategies that regulate LSD1 for novel therapeutics Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-10 Meng Li, Mengge Dai, Bing Cheng, Shaotong Li, Enhui Guo, Junwei Fu, Ting Ma, Bin Yu
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Discovery of GluN2A subtype-selective N-methyl-d-aspartate (NMDA) receptor ligands Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-10 Liyang Jiang, Na Liu, Fabao Zhao, Boshi Huang, Dongwei Kang, Peng Zhan, Xinyong Liu
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Single-cell transcriptomics reveals the ameliorative effect of Rosmarinic acid on diabetic nephropathy-induced kidney injury by modulating oxidative stress and inflammation Acta Pharm. Sin. B (IF 14.5) Pub Date : 2024-01-11 Junhui Chen, Qian Zhang, Jinan Guo, Di Gu, Jing Liu, Piao Luo, Yunmeng Bai, Jiayun Chen, Xinzhou Zhang, Sheng Nie, Chunbo Chen, Yulin Feng, Jigang Wang