Acta materia medica最新文献

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New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives. 乳腺癌中的新一代雌激素受体靶向药物:现状与前景。
Acta materia medica Pub Date : 2024-02-21 Epub Date: 2024-03-15 DOI: 10.15212/amm-2024-0006
Jian Min, Xin Liu, Rouming Peng, Chun-Chi Chen, Wei Wang, Rey-Ting Guo
{"title":"New generation estrogen receptor-targeted agents in breast cancer: present situation and future prospectives.","authors":"Jian Min, Xin Liu, Rouming Peng, Chun-Chi Chen, Wei Wang, Rey-Ting Guo","doi":"10.15212/amm-2024-0006","DOIUrl":"https://doi.org/10.15212/amm-2024-0006","url":null,"abstract":"<p><p>Endocrine therapy which blocking the signaling of estrogen receptor, has long been effective for decades as a primary treatment choice for breast cancer patients expressing ER. However, the issue of drug resistance poses a significant clinical challenge. It's critically important to create new therapeutic agents that can suppress ERα activity, particularly in cases of ESR1 mutations. This review highlights recent efforts in drug development of next generation ER-targeted agents, including oral selective ER degraders (SERDs), proteolysis targeting chimera (PROTAC) ER degraders, other innovative molecules such as complete estrogen receptor antagonists (CERANs) and selective estrogen receptor covalent antagonists (SERCAs). The drug design, efficacy and clinical trials for each compound were detailed.</p>","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11450757/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142382585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Application of PROTACs in Target Identification and Target Validation. PROTACs 在目标识别和目标验证中的应用。
Acta materia medica Pub Date : 2024-02-21 Epub Date: 2024-03-21 DOI: 10.15212/amm-2024-0010
Yang Liu, Jing Liang, Rui Zhu, Yueying Yang, Yali Wang, Wenyi Wei, Hua Li, Lixia Chen
{"title":"Application of PROTACs in Target Identification and Target Validation.","authors":"Yang Liu, Jing Liang, Rui Zhu, Yueying Yang, Yali Wang, Wenyi Wei, Hua Li, Lixia Chen","doi":"10.15212/amm-2024-0010","DOIUrl":"https://doi.org/10.15212/amm-2024-0010","url":null,"abstract":"<p><p>PROTAC, as a novel therapeutic drug model, has received widespread attention from the academic and pharmaceutical industries. At the same time, PROTAC technology has led many researchers to focus on developing chemical biology tool properties due to its unique operating mechanism and protein dynamic regulatory properties. In recent years, the rapid development of PROTAC technology has gradually made it an essential tool for target identification and target validation. To further promote the application of PROTAC tools in drug discovery and basic medical sciences research, this review distinguished between target identification and target validation concepts. It summarized the research progress of PROTAC technology in these aspects.</p>","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11452161/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142383320","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
PROTACs Targeting Epigenetic Proteins. 针对表观遗传蛋白质的 PROTACs。
Acta materia medica Pub Date : 2023-10-26 Epub Date: 2023-12-06 DOI: 10.15212/amm-2023-0039
Chao Zhang, Yuna He, Xiuyun Sun, Wenyi Wei, Yanlong Liu, Yu Rao
{"title":"PROTACs Targeting Epigenetic Proteins.","authors":"Chao Zhang, Yuna He, Xiuyun Sun, Wenyi Wei, Yanlong Liu, Yu Rao","doi":"10.15212/amm-2023-0039","DOIUrl":"10.15212/amm-2023-0039","url":null,"abstract":"<p><p>Epigenetics, a field that investigates alterations in gene function that can be inherited without changes in DNA sequence, encompasses molecular pathways such as histone variants, posttranslational modifications of amino acids, and covalent modifications of DNA bases. These pathways modulate the transformation of genotypes into specific phenotypes. Epigenetics plays a substantial role in cell growth, development, and differentiation by dynamically regulating gene transcription and ensuring genomic stability. This regulation is carried out by three key players: writers, readers, and erasers. In recent years, epigenetic proteins have played a crucial role in epigenetic regulation and have gradually become important targets in drug research and development. Targeted therapy is an essential strategy; however, the effectiveness of targeted drugs is often limited by drug resistance, posing a significant dilemma in clinical practice. Targeted protein degradation technologies, including proteolysis-targeting chimeras (PROTACs), have great potential in overcoming drug resistance and targeting undruggable targets. These areas of research are gaining increasing attention to various epigenetic related disease. In this review, we have provided a summary of the recently developed degraders targeting epigenetic readers, writers, and erasers. Additionally, we have outlined new applications for epigenetic protein degraders. Finally, we have addressed several unresolved challenges within the PROTAC field and offered potential solutions from our perspective. As the field continues to advance, the integration of these innovative methodologies holds great promise for addressing the challenges associated with PROTAC development.</p>","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11364368/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142115475","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Exploitation of platelets for antitumor drug delivery and modulation of the tumor immune microenvironment 血小板用于抗肿瘤药物递送和调节肿瘤免疫微环境
Acta materia medica Pub Date : 2023-05-13 DOI: 10.15212/amm-2023-0005
Jie Guo, Meng Wang, Yong Zhu, F. Watari, Yonghong Xu, Xiao Chen
{"title":"Exploitation of platelets for antitumor drug delivery and modulation of the tumor immune microenvironment","authors":"Jie Guo, Meng Wang, Yong Zhu, F. Watari, Yonghong Xu, Xiao Chen","doi":"10.15212/amm-2023-0005","DOIUrl":"https://doi.org/10.15212/amm-2023-0005","url":null,"abstract":"Platelets are blood components traditionally believed to have fundamental roles in vascular hemostasis and thrombosis. In recent years, platelets have received new attention for their roles in tumorigenesis and progression. On the one hand, platelets are actively recruited by various tumors and comprise a crucial part of the tumor microenvironment (TME), thus inspiring the use of platelets for tumor-targeted drug delivery. To this end, various platelet-based devices have been proposed, such as natural platelets, engineered platelets, platelet membranes, and platelet-derived microparticles. On the other hand, platelets are involved in tumor immunosuppression mechanisms, by directing and/or assisting various tumor-associated immune cells. However, in the context of inflammation and autoimmune diseases, platelets can amplify immune responses by promoting immune cell mobilization and activation, thereby exacerbating tissue damage. Thus, interest is growing in the use of tumor-associated platelets as targets for therapeutic modulation of the TME and augmenting anti-tumor immune responses. In this review, we summarize current advances in exploiting platelets for both antitumor drug delivery and immune modulation of the TME.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41947171","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Emerging role of HJURP as a therapeutic target in cancers HJURP作为癌症治疗靶点的新作用
Acta materia medica Pub Date : 2023-05-06 DOI: 10.15212/amm-2023-0008
Jiaqi Tan, Lertnimitphun Peeraphong, Chattarin Ruchawapol, Juan Zhang, Juan Zhao, Wenwei Fu, Li Zhang, Hongxi Xu
{"title":"Emerging role of HJURP as a therapeutic target in cancers","authors":"Jiaqi Tan, Lertnimitphun Peeraphong, Chattarin Ruchawapol, Juan Zhang, Juan Zhao, Wenwei Fu, Li Zhang, Hongxi Xu","doi":"10.15212/amm-2023-0008","DOIUrl":"https://doi.org/10.15212/amm-2023-0008","url":null,"abstract":"Holliday junction recognition protein (HJURP) is a key molecular chaperone for centromere protein A (CENP-A), which is essential for chromosome separation during mitosis and cell cycle regulation. Recent studies have identified the essential role of HJURP in carcinogenesis. Abnormal upregulation of HJURP expression has been observed in various human cancers, such as non-small cell lung cancer (NSCLC), hepatocellular carcinoma (HCC), bladder cancer, and breast cancer, and is associated with poor pathologic development and prognosis. In vitro and in vivo studies have shown that HJURP mainly exerts oncogenic functions by regulating the cell cycle, cellular senescence, and epithelial-mesenchymal transition (EMT). The purpose of this review was to evaluate the prognostic significance of HJURP in human cancers and summarize anti-tumor studies targeting HJURP. The factors regulating HJURP in carcinogenesis and the corresponding effects are also discussed to provide new insight into targeting HJURP as a promising strategy for cancer treatment.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45854186","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Inhalable ciprofloxacin/polymyxin B dry powders in respiratory infection therapy 可吸入环丙沙星/多粘菌素B干粉治疗呼吸道感染
Acta materia medica Pub Date : 2023-04-29 DOI: 10.15212/amm-2022-0050
Zhengqi Xu, Hriday Bera, Hengzhuang Wang, Junwei Wang, Dongmei Cun, Yu Feng, Mingshi Yang
{"title":"Inhalable ciprofloxacin/polymyxin B dry powders in respiratory infection therapy","authors":"Zhengqi Xu, Hriday Bera, Hengzhuang Wang, Junwei Wang, Dongmei Cun, Yu Feng, Mingshi Yang","doi":"10.15212/amm-2022-0050","DOIUrl":"https://doi.org/10.15212/amm-2022-0050","url":null,"abstract":"The current study focused on the formulation, physicochemical characterization, and antibacterial susceptibility testing of inhalable spray dried powders containing ciprofloxacin (CIP) and polymyxin B sulfate (PMB). CIP nanosuspensions with an average particle diameter of 435.9 ± 9.3 nm were initially obtained using the wet-milling protocol and subsequently co-spray dried with PMB solutions to yield inhalable dry powders. The Powder X-Ray Diffraction (P-XRD) results showed that the wet-milled CIP nanoparticles were in a 4.8 hydrate state, which were transformed to 3.7 hydrates and amorphous materials after co-spray drying. The PMB remained in an amorphous state in the dry powders. Differential Scanning Calorimetry (DSC) analyses revealed that the glass transition temperatures (Tgs) of the co–spray dried formulations were higher than the Tg of CIP, but lower than the Tg of PMB. Fourier Transform Infrared Spectrometer (FTIR) studies suggested the existence of π - π interactions between CIP and PMB in the co-spray dried powders. These powders also retained antimicrobial effects against Pseudomonas aeruginosa strain PAO1. In addition, the spray-dried powder formulations exhibited satisfactory solid-state stability and aerodynamic characteristics when stored under 3% relative humidity and 20 ± 5 °C for 4 months. Overall, the newly developed inhalable CIP/PMB dry powders are a promising therapeutic strategy for respiratory tract infections.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44299684","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Molecular networking as a natural products discovery strategy 分子网络作为一种天然产物发现策略
Acta materia medica Pub Date : 2023-04-25 DOI: 10.15212/amm-2023-0007
Mi Zhang, Kouharu Otsuki, Wei Li
{"title":"Molecular networking as a natural products discovery strategy","authors":"Mi Zhang, Kouharu Otsuki, Wei Li","doi":"10.15212/amm-2023-0007","DOIUrl":"https://doi.org/10.15212/amm-2023-0007","url":null,"abstract":"The rapid development of bioinformatics tools has recently broken through the bottleneck in natural products research. These advances have enabled natural products researchers to rapidly separate and efficiently target and discover previously undescribed molecules. Among these advances, tandem mass spectrometry molecular networking is a promising method for rapidly de-replicating complex natural mixtures, thus leading to an accelerated revolution in the “art of natural products isolation” field. In this review we describe the current molecular networking-based metabolite analysis methods that are widely applied or implementable in natural products discovery research, metabolomics, and related fields. The main objective of this review was to summarize strategies that can be rapidly implemented as alternative de-replication approaches for efficient natural products discovery and to list examples of successful applications that combine networking with other techniques.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46125839","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Multi-component Chinese medicine formulas for drug discovery: State of the art and future perspectives 用于药物发现的多组份中药配方:现状和未来展望
Acta materia medica Pub Date : 2023-03-30 DOI: 10.15212/amm-2022-0049
Cheng Zhang, Guoming Chen, Guoyi Tang, Xiaoyu Xu, Z. Feng, Yuanjun Lu, Y. Chan, Junyu Wu, Yuanyuan Chen, Lin Xu, Qing-li Ren, Hongchao Yuan, Dong Yang, Zhe-Sheng Chen, Ning Wang, Yibin Feng
{"title":"Multi-component Chinese medicine formulas for drug discovery: State of the art and future perspectives","authors":"Cheng Zhang, Guoming Chen, Guoyi Tang, Xiaoyu Xu, Z. Feng, Yuanjun Lu, Y. Chan, Junyu Wu, Yuanyuan Chen, Lin Xu, Qing-li Ren, Hongchao Yuan, Dong Yang, Zhe-Sheng Chen, Ning Wang, Yibin Feng","doi":"10.15212/amm-2022-0049","DOIUrl":"https://doi.org/10.15212/amm-2022-0049","url":null,"abstract":"For hundreds of years, the drug discovery and development industry has aimed at identifying single components with a clear mechanism of action as desirable candidates for potential drugs. However, this conventional strategy of drug discovery and development has faced challenges including a low success rate and high development costs. Herein, we critically review state-of-the-art drug discovery and development based on multi-component Chinese medicine formulas. We review the policies and application status of new drugs based on multi-component Chinese medicines in the US, China, and the European Union. Moreover, we illustrate several excellent cases of ongoing applications. Biomedical technologies that may facilitate drug discovery and development based on multi-component Chinese medicine formulas are discussed, including network pharmacology, integrative omics, CRISPR gene editing, and chemometrics. Finally, we discuss potential problems and solutions in pre-clinical and clinical research in drug discovery and development based on multi-component Chinese medicine formulas. We hope that this review will promote discussion of the roles of multi-component Chinese medicine formulas in the discovery and development of new drugs for the treatment of human diseases.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43989988","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 5
Discovery of a pyridophenoselenazinium-based photosensitizer with high photodynamic efficacy against breast cancer cells 发现一种对乳腺癌症细胞具有高光动力效应的基于吡啶并苯并氮嗪的光敏剂
Acta materia medica Pub Date : 2023-03-23 DOI: 10.15212/amm-2023-0002
Guiling Li, Peixia Li, Qiaoyun Jiang, Qianqian Zhang, Jingru Qiu, Donghai Li, Gang Shan
{"title":"Discovery of a pyridophenoselenazinium-based photosensitizer with high photodynamic efficacy against breast cancer cells","authors":"Guiling Li, Peixia Li, Qiaoyun Jiang, Qianqian Zhang, Jingru Qiu, Donghai Li, Gang Shan","doi":"10.15212/amm-2023-0002","DOIUrl":"https://doi.org/10.15212/amm-2023-0002","url":null,"abstract":"Development of efficient photosensitizers with minimal side effects is highly desirable for photodynamic therapy. Reported herein is the discovery of a novel pyridophenoselenazinium-based NIR-I photosensitizer, termed PPSe, that efficiently generated both type I and II reactive oxygen species (ROS) upon appropriate light irradiation. PPSe exhibited potent phototoxicity as well as excellent phototherapeutic indices against several breast cancer cell lines. PPSe induced DNA damage and breast cancer cell apoptosis via photo-triggered intracellular ROS generation.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43118388","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Potential pharmacokinetic interactions in fixed-dose combinations of perindopril/indapamide/amlodipine compared with perindopril/indapamide and amlodipine in healthy Chinese volunteers 培哚普利/吲达帕胺/氨氯地平固定剂量联合用药与培哚普利/吲达帕胺和氨氯地平在中国健康志愿者体内的潜在药代动力学相互作用比较
Acta materia medica Pub Date : 2023-03-18 DOI: 10.15212/amm-2022-0045
Huitao Gao, Hongzhong Liu, Xin Zheng, X. Cui, S. Bricout-Hennel, A. Lucien, Pauline Lauruol, Yaqin Wang, Xue Wang, Hongyun Wang, Chen Rui
{"title":"Potential pharmacokinetic interactions in fixed-dose combinations of perindopril/indapamide/amlodipine compared with perindopril/indapamide and amlodipine in healthy Chinese volunteers","authors":"Huitao Gao, Hongzhong Liu, Xin Zheng, X. Cui, S. Bricout-Hennel, A. Lucien, Pauline Lauruol, Yaqin Wang, Xue Wang, Hongyun Wang, Chen Rui","doi":"10.15212/amm-2022-0045","DOIUrl":"https://doi.org/10.15212/amm-2022-0045","url":null,"abstract":"S05590 is a fixed-dose combination of perindopril tert-butylamine 4 mg/indapamide 1.25 mg, and S06593 is a fixed-dose combination of perindopril arginine 5 mg/indapamide 1.25 mg/amlodipine 5 mg. The purpose of this study was to determine whether pharmacokinetic interactions exist among the components of S06593, compared with S05590 and amlodipine as reference drugs, in healthy Chinese male volunteers after a single oral administration under fasting conditions. A single-center, open-label, randomized, three-period, six-way crossover study was conducted. A total of 42 participants were enrolled and randomized to receive S05590 plus amlodipine, or S06593. The doses of perindopril were 3.34 mg in both S05590 and S06593, calculated as free acid. Blood samples were collected in each treatment period to determine the plasma concentrations of perindopril, indapamide and amlodipine, as well as perindoprilat, the main metabolite of perindopril. A total of 39 participants completed this study. The 90% confidence intervals of the geometric mean ratios of Cmax, AUC0-t and AUC0-∞ for perindopril, perindoprilat, indapamide and amlodipine were all within 80.00–125.00%, thus indicating that S05590 plus amlodipine and S06593 were pharmacokinetically equivalent. During the study, only one serious emergent adverse event was reported, which was deemed not to be associated with the study drug. No serious treatment-associated adverse events were observed.","PeriodicalId":72055,"journal":{"name":"Acta materia medica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43836076","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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