1.Fibroblast activation protein targeting radiopharmaceuticals: From drug design to clinical translation.
Yuxuan WU ; Xingkai WANG ; Xiaona SUN ; Xin GAO ; Siqi ZHANG ; Jieting SHEN ; Hao TIAN ; Xueyao CHEN ; Hongyi HUANG ; Shuo JIANG ; Boyang ZHANG ; Yingzi ZHANG ; Minzi LU ; Hailong ZHANG ; Zhicheng SUN ; Ruping LIU ; Hong ZHANG ; Ming-Rong ZHANG ; Kuan HU ; Rui WANG
Acta Pharmaceutica Sinica B 2025;15(9):4511-4542
The activation proteins released by fibroblasts in the tumor microenvironment regulate tumor growth, migration, and treatment response, thereby influencing tumor progression and therapeutic outcomes. Owing to the proliferation and metastasis of tumors, fibroblast activation protein (FAP) is typically highly expressed in the tumor stroma, whereas it is nearly absent in adult normal tissues and benign lesions, making it an attractive target for precision medicine. Radiolabeled agents targeting FAP have the potential for targeted cancer diagnosis and therapy. This comprehensive review aims to describe the evolution of FAPI-based radiopharmaceuticals and their structural optimization. Within its scope, this review summarizes the advances in the use of radiolabeled small molecule inhibitors for tumor imaging and therapy as well as the modification strategies for FAPIs, combined with insights from structure-activity relationships and clinical studies, providing a valuable perspective for radiopharmaceutical clinical development and application.
2.Impact and clinical potential of RNA modifications in the development and progression of renal cancer
Huiting YANG ; Lu LU ; Qian LI ; Boyang LIU ; Shenglan GAO ; Bitang HUANG ; Chunlong YANG ; Qingjun PAN
Chinese Journal of Comparative Medicine 2025;35(7):128-147
Renal cancer is a common and increasingly prevalent malignancy with a complex pathogenesis influenced by genetics,smoking,and obesity.Current treatment mainly involves surgery with adjunctive chemotherapy,radiation,and immunotherapy,but high rates of recurrence and metastasis indicate its limited effectiveness,emphasizing the need for better therapeutic targets.Growing evidence indicates that epigenetic modifications,particularly RNA modifications,play a critical role in renal cancer development and progression.This review highlights recent advances in renal cancer epigenetics,focusing on RNA modifications such as N6-methyladenosine(m6 A),N7-methylguanosine(m7G),5-methylcytosine(m5C),N1-methyladenosine(m1A),adenosine-to-inosine(A-to-I),N6,2'-O-dimethyladenosine(m6Am),and N4-acetylcytidine(ac4C),along with their regulatory factors.It also explores the diagnostic and therapeutic potential of targeting RNA modifications and associated proteins.
3.Role and mechanism of m7G methylation modification in tumor drug resistance
Lu LU ; Huiting YANG ; Boyang LIU ; Qian LI ; Bitang HUANG ; Shenglan GAO ; Chunlong YANG ; Qingjun PAN
Chinese Journal of Comparative Medicine 2025;35(8):120-130
N7-methylguanosine(m7G)modification occurs at the 5'cap of mRNA in eukaryotes,and is also found at specific sites on tRNA and rRNA,showing wide conservation across various biological organisms.Aberrant m7G modification is involved in the dysregulation of gene expression and serves as a biomarker for multiple cancers,with significant potential for applications in tumor diagnosis and therapy.This review summarizes the biological functions and regulatory mechanisms of m7G modification,and outlines its potential clinical applications.It also highlights the oncogenic roles of aberrant m7G modification and its association with prognosis,providing a detailed discussion of the role and molecular mechanisms of abnormal m7G modification in regulating drug resistance in various cancers.
4.Impact and clinical potential of RNA modifications in the development and progression of renal cancer
Huiting YANG ; Lu LU ; Qian LI ; Boyang LIU ; Shenglan GAO ; Bitang HUANG ; Chunlong YANG ; Qingjun PAN
Chinese Journal of Comparative Medicine 2025;35(7):128-147
Renal cancer is a common and increasingly prevalent malignancy with a complex pathogenesis influenced by genetics,smoking,and obesity.Current treatment mainly involves surgery with adjunctive chemotherapy,radiation,and immunotherapy,but high rates of recurrence and metastasis indicate its limited effectiveness,emphasizing the need for better therapeutic targets.Growing evidence indicates that epigenetic modifications,particularly RNA modifications,play a critical role in renal cancer development and progression.This review highlights recent advances in renal cancer epigenetics,focusing on RNA modifications such as N6-methyladenosine(m6 A),N7-methylguanosine(m7G),5-methylcytosine(m5C),N1-methyladenosine(m1A),adenosine-to-inosine(A-to-I),N6,2'-O-dimethyladenosine(m6Am),and N4-acetylcytidine(ac4C),along with their regulatory factors.It also explores the diagnostic and therapeutic potential of targeting RNA modifications and associated proteins.
5.Role and mechanism of m7G methylation modification in tumor drug resistance
Lu LU ; Huiting YANG ; Boyang LIU ; Qian LI ; Bitang HUANG ; Shenglan GAO ; Chunlong YANG ; Qingjun PAN
Chinese Journal of Comparative Medicine 2025;35(8):120-130
N7-methylguanosine(m7G)modification occurs at the 5'cap of mRNA in eukaryotes,and is also found at specific sites on tRNA and rRNA,showing wide conservation across various biological organisms.Aberrant m7G modification is involved in the dysregulation of gene expression and serves as a biomarker for multiple cancers,with significant potential for applications in tumor diagnosis and therapy.This review summarizes the biological functions and regulatory mechanisms of m7G modification,and outlines its potential clinical applications.It also highlights the oncogenic roles of aberrant m7G modification and its association with prognosis,providing a detailed discussion of the role and molecular mechanisms of abnormal m7G modification in regulating drug resistance in various cancers.
6.Study on the medication law of TCM compounds used in the treatment of non-small cell lung cancer
Ying CHEN ; Ziming ZHANG ; Yong ZHU ; Yuan GAO ; Shina ZHANG ; Boyang SHENG ; Junfeng YAN
International Journal of Traditional Chinese Medicine 2024;46(5):642-649
Objective:To explore the medication law of TCM compounds used in the treatment of non-small cell lung cancer (NSCLC).Methods:Clinical literature about TCM compounds in the treatment of NSCLC was retrieved from CNKI, Wanfang Data, PubMed and Web of Science core collection database from January 1st, 2003 to May 1st, 2023. The Python and the ancient and modern medical record cloud platform V2.3.7 were used to analyses frequency statistics and properties, and clustering analysis, factor analysis and association rule analysis were performed.Results:A total of 866 articles were included, with 660 effective TCM compounds, 647 kinds of Chinese materia medica. There were 36 kinds of high-frequency Chinese materia medica, such as Astragali Radix, Atractylodis Macrocephalae Rhizoma and Poria; the efficacy categories of Chinese materia medica mainly included tonics and phlegm resolving cough relieving and asthma relieving drugs. Cluster analysis obtained 4 clusters, factor analysis extracted 11 common factors, and association rule analysis obtained 37 highly supported combinations of Chinese materia medica. The most reliable triple drug combination among them was Astragali Radix-Atractylodis Macrocephalae Rhizoma-Hedyotis diffusa willd, and the double drug combination was Astragali Radix-Ligustri Lucidi Fructus.Conclusion:TCM for the treatment of NSCLC mainly focuses on strengthening the healthy qi, clearing heat, resolving phlegm and detoxifying toxins, supplemented by tonifying qi and activating blood circulation, dispelling dampness and resolving phlegm.
7.The enlightenment of artificial intelligence large-scale model on the research of intelligent eye diagnosis in traditional Chinese medicine
Yuan GAO ; Zixuan WU ; Boyang SHENG ; Fu ZHANG ; Yong CHENG ; Junfeng YAN ; Qinghua PENG
Digital Chinese Medicine 2024;7(2):101-107
Eye diagnosis is a method for inspecting systemic diseases and syndromes by observing the eyes.With the development of intelligent diagnosis in traditional Chinese medicine(TCM),artificial intelligence(AI)can improve the accuracy and efficiency of eye diagnosis.However,the research on intelligent eye diagnosis still faces many challenges,including the lack of standardized and precisely labeled data,multi-modal information analysis,and artificial in-telligence models for syndrome differentiation.The widespread application of AI models in medicine provides new insights and opportunities for the research of eye diagnosis intelli-gence.This study elaborates on the three key technologies of AI models in the intelligent ap-plication of TCM eye diagnosis,and explores the implications for the research of eye diagno-sis intelligence.First,a database concerning eye diagnosis was established based on self-su-pervised learning so as to solve the issues related to the lack of standardized and precisely la-beled data.Next,the cross-modal understanding and generation of deep neural network models to address the problem of lacking multi-modal information analysis.Last,the build-ing of data-driven models for eye diagnosis to tackle the issue of the absence of syndrome dif-ferentiation models.In summary,research on intelligent eye diagnosis has great potential to be applied the surge of AI model applications.
8.METTL14 is a chromatin regulator independent of its RNA N6-methyladenosine methyltransferase activity.
Xiaoyang DOU ; Lulu HUANG ; Yu XIAO ; Chang LIU ; Yini LI ; Xinning ZHANG ; Lishan YU ; Ran ZHAO ; Lei YANG ; Chuan CHEN ; Xianbin YU ; Boyang GAO ; Meijie QI ; Yawei GAO ; Bin SHEN ; Shuying SUN ; Chuan HE ; Jun LIU
Protein & Cell 2023;14(9):683-697
METTL3 and METTL14 are two components that form the core heterodimer of the main RNA m6A methyltransferase complex (MTC) that installs m6A. Surprisingly, depletion of METTL3 or METTL14 displayed distinct effects on stemness maintenance of mouse embryonic stem cell (mESC). While comparable global hypo-methylation in RNA m6A was observed in Mettl3 or Mettl14 knockout mESCs, respectively. Mettl14 knockout led to a globally decreased nascent RNA synthesis, whereas Mettl3 depletion resulted in transcription upregulation, suggesting that METTL14 might possess an m6A-independent role in gene regulation. We found that METTL14 colocalizes with the repressive H3K27me3 modification. Mechanistically, METTL14, but not METTL3, binds H3K27me3 and recruits KDM6B to induce H3K27me3 demethylation independent of METTL3. Depletion of METTL14 thus led to a global increase in H3K27me3 level along with a global gene suppression. The effects of METTL14 on regulation of H3K27me3 is essential for the transition from self-renewal to differentiation of mESCs. This work reveals a regulatory mechanism on heterochromatin by METTL14 in a manner distinct from METTL3 and independently of m6A, and critically impacts transcriptional regulation, stemness maintenance, and differentiation of mESCs.
Animals
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Mice
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Methylation
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Chromatin
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Histones/metabolism*
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RNA, Messenger/genetics*
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Methyltransferases/metabolism*
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RNA/metabolism*
9.Recent advance in prognostic indicators of primary central nervous system lymphoma
Yuting GAO ; Boyang LIU ; Hua YOU
Chinese Journal of Neuromedicine 2022;21(8):831-836
Primary central nervous system lymphoma (PCNSL) is a kind of highly aggressive and rare extranodal non-Hodgkin lymphoma, and the treatment effect and survival prognosis of these patients are still not satisfied. In recent years, domestic and foreign researchers have devoted themselves to find more effective prognostic indicators from clinical hematological indicators, as well as gene and protein levels, so as to guide the diagnosis and treatment of PCNSL more accurately in clinical practice and improve the prognosis of PCNSL patients to a greater extent. This paper provides a review of such studies by reviewing PubMed.
10.Application of TTI in quality control of the military thermo-sensitive drugs
Boyang WANG ; Jie LI ; Jin GAO ; Zidong WANG
Journal of Pharmaceutical Practice 2020;38(3):282-285
To ensure the safety and efficacy of the military thermo-sensitive drugs, it is necessary to monitor the temperature changes through the whole process of production, transportation, storage, distribution and application. The characteristics of various commercial TTI were analyzed. The applications of TTI technology in the quality control for military thermo-sensitive drugs were reviewed in order to provide accurate quality assurance for those drugs.

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