Recent patents on anti-cancer drug discovery最新文献

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Mechanisms of Anti-PD Therapy Resistance in Digestive System Neoplasms 消化系统肿瘤的抗-PD疗法耐药性机制
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-02-02 DOI: 10.2174/0115748928269276231120103256
Yuxia Wu, Xiangyan Jiang, Zeyuan Yu, Zongrui Xing, Yong Ma, Huiguo Qing
{"title":"Mechanisms of Anti-PD Therapy Resistance in Digestive System Neoplasms","authors":"Yuxia Wu, Xiangyan Jiang, Zeyuan Yu, Zongrui Xing, Yong Ma, Huiguo Qing","doi":"10.2174/0115748928269276231120103256","DOIUrl":"https://doi.org/10.2174/0115748928269276231120103256","url":null,"abstract":": Digestive system neoplasms are highly heterogeneous and exhibit complex resistance mechanisms that render anti-programmed cell death protein (PD) therapies poorly effective. The tumor microenvironment (TME) plays a pivotal role in tumor development, apart from supplying energy for tumor proliferation and impeding the body's anti-tumor immune response, the TME actively facilitates tumor progression and immune escape via diverse pathways, which include the modulation of heritable gene expression alterations and the intricate interplay with the gut microbiota. In this review, we aim to elucidate the mechanisms underlying drug resistance in digestive tumors, focusing on immune-mediated resistance, microbial crosstalk, metabolism, and epigenetics. We will highlight the unique characteristics of each digestive tumor and emphasize the significance of the tumor immune microenvironment (TIME). Furthermore, we will discuss the current therapeutic strategies that hold promise for combination with cancer immune normalization therapies. This review aims to provide a thorough understanding of the resistance mechanisms in digestive tumors and offer insights into potential therapeutic interventions.","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":"6 1","pages":""},"PeriodicalIF":2.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139666743","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
TPD52 as a Potential Prognostic Biomarker and its Correlation with Immune Infiltrates in Uterine Corpus Endometrial Carcinoma: Bioinformatic Analysis and Experimental Verification 作为潜在预后生物标记物的 TPD52 及其与子宫体子宫内膜癌免疫浸润的相关性:生物信息学分析与实验验证
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-02-02 DOI: 10.2174/0115748928267447231107101539
Lu Miao, Buze Chen, Li Jing, Tian Zeng, Youguo Chen
{"title":"TPD52 as a Potential Prognostic Biomarker and its Correlation with Immune Infiltrates in Uterine Corpus Endometrial Carcinoma: Bioinformatic Analysis and Experimental Verification","authors":"Lu Miao, Buze Chen, Li Jing, Tian Zeng, Youguo Chen","doi":"10.2174/0115748928267447231107101539","DOIUrl":"https://doi.org/10.2174/0115748928267447231107101539","url":null,"abstract":"Background: Aberrant expression of tumor protein D52 (TPD52) is associated with some tumors. The role of TPD52 in uterine corpus endometrial carcinoma (UCEC) remains uncertain. Objective: We aimed to investigate the involvement of TPD52 in the pathogenesis of UCEC. Methods: We employed bioinformatics analysis and experimental validation in our study. Results: Our findings indicated that elevated TPD52 expression in UCEC was significantly associated with various clinical factors, including clinical stage, race, weight, body mass index (BMI), histological type, histological grade, surgical approach, and age (p < 0.01). Furthermore, high TPD52 expression was a predictor of poorer overall survival (OS), progress-free survival (PFS), and disease-specific survival (DSS) (p = 0.011, p = 0.006, and p = 0.003, respectively). TPD52 exhibited a significant correlation with DSS (HR: 2.500; 95% CI: 1.153-5.419; p = 0.02). TPD52 was involved in GPCR ligand binding and formation of the cornified envelope in UCEC. Moreover, TPD52 expression was found to be associated with immune infiltration, immune checkpoints, tumor mutation burden (TMB)/ microsatellite instability (MSI), and mRNA stemness indices (mRNAsi). The somatic mutation rate of TPD52 in UCEC was 1.9%. A ceRNA network of AC011447.7/miR-1-3p/TPD52 was constructed. There was excessive TPD52 protein expression. The upregulation of TPD52 expression in UCEC cell lines was found to be statistically significant. Conclusion: TPD52 is upregulated in UCEC and may be a useful patent for prognostic biomarkers of UCEC, which may have important value for clinical treatment and supervision of UCEC patients.","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":"23 1","pages":""},"PeriodicalIF":2.8,"publicationDate":"2024-02-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139666910","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
LncRNA FAM83H-AS1 Contributes to the Radio-resistance and Proliferation in Liver Cancer through Stability FAM83H Protein. LncRNA FAM83H-AS1 通过稳定 FAM83H 蛋白促进肝癌的放射抗性和增殖
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892818666230427164227
Xiaocong Jiang, Yuhong Lan, Yingchun Zhang, Yuhong Dong, Ting Song
{"title":"LncRNA FAM83H-AS1 Contributes to the Radio-resistance and Proliferation in Liver Cancer through Stability FAM83H Protein.","authors":"Xiaocong Jiang, Yuhong Lan, Yingchun Zhang, Yuhong Dong, Ting Song","doi":"10.2174/1574892818666230427164227","DOIUrl":"10.2174/1574892818666230427164227","url":null,"abstract":"<p><strong>Background: </strong>Liver cancer (LC) is one of China's most common malignant tumors, with a high mortality rate, ranking third leading cause of death after gastric and esophageal cancer. Recent patents propose the LncRNA FAM83H-AS1 has been verified to perform a crucial role in the progression of LC. LncRNA FAM83H-AS1 has been verified to perform a crucial role in the progression of LC. However, the concrete mechanism remains to be pending further investigation.</p><p><strong>Objective: </strong>This study aimed to explore the embedding mechanism of FAM83H-AS1 molecules in terms of radio sensitivity of LC and provide potentially effective therapeutic targets for LC therapy.</p><p><strong>Methods: </strong>Quantitative real-time PCR (qRT-PCR) was conducted to measure the transcription levels of genes. Proliferation was determined via CCK8 and colony formation assays. Western blot was carried out to detect the relative protein expression. A xenograft mouse model was constructed to investigate the effect of LncRNA FAM83H-AS1 on tumor growth and radio-sensitivity <i>in vivo</i>.</p><p><strong>Results: </strong>The levels of lncRNA FAM83H-AS1 were remarkably increased in LC. Knockdown of FAM83H-AS1 inhibited LC cell proliferation and colony survival fraction. Deletion of FAM83H-AS1 increased the sensitivity of LC cells to 4 Gy of X-ray radiation. In the xenograft model, radiotherapy combined with FAM83H-AS1 silencing significantly reduced tumor volume and weight. Overexpression of FAM83H reversed the effects of FAM83H-AS1 deletion on proliferation and colony survival fraction in LC cells. Moreover, the over-expressing of FAM83H also restored the tumor volume and weight reduction caused by the knockdown of FAM83H-AS1 or radiation in the xenograft model.</p><p><strong>Conclusion: </strong>Knockdown of lncRNA FAM83H-AS1 inhibited LC growth and enhanced radiosensitivity in LC. It has the potential to be a promising target for LC therapy.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"316-327"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9399922","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
TGF-β Score based on Silico Analysis can Robustly Predict Prognosis and Immunological Characteristics in Lower-grade Glioma: The Evidence from Multicenter Studies. 基于 Silico 分析的 TGF-β 评分可准确预测下级胶质瘤的预后和免疫学特征:来自多中心研究的证据
IF 2.5 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892819666230915143632
Weizhong Zhang, Zhiyuan Yan, Feng Zhao, Qinggui He, Hongbo Xu
{"title":"TGF-β Score based on <i>Silico</i> Analysis can Robustly Predict Prognosis and Immunological Characteristics in Lower-grade Glioma: The Evidence from Multicenter Studies.","authors":"Weizhong Zhang, Zhiyuan Yan, Feng Zhao, Qinggui He, Hongbo Xu","doi":"10.2174/1574892819666230915143632","DOIUrl":"10.2174/1574892819666230915143632","url":null,"abstract":"<p><strong>Introduction: </strong>Nowadays, mounting evidence shows that variations in TGF-β signaling pathway-related components influence tumor development. Current research has patents describing the use of anti-TGF-β antibodies and checkpoint inhibitors for the treatment of proliferative diseases. Importantly, TGF-β signaling pathway is significant for lower-grade glioma (LGG) to evade host immunity. Loss of particular tumor antigens and shutdown of professional antigenpresenting cell activity may render the anti-tumor response ineffective in LGG patients. However, the prognostic significance of TGF-β related genes in LGG is still unknown.</p><p><strong>Methods: </strong>We collected RNA-seq data from the GTEx database (normal cortical tissues), the Cancer Genome Atlas database (TCGA-LGG), and the Chinese Glioma Genome Atlas database (CGGA-693 and CGGA-325) for conducting our investigation.</p><p><strong>Results: </strong>In addition, previous publications were explored for the 223 regulators of the TGF-β signaling pathway, and 30 regulators with abnormal expression in TCGA and GTEx database were identified. In order to identify hub prognostic regulators, least absolute shrinkage and selection operator (LASSO) regression and multivariate Cox regression analysis were used to screen from differentially expressed genes (DEGs). On the basis of 11 genes from LASSO-Cox regression analysis (NEDD8, CHRD, TGFBR1, TP53, BMP2, LRRC32, THBS2, ID1, NOG, TNF, and SERPINE1), TGF-β score was calculated. Multiple statistical approaches verified the predictive value of the TGF-β score for the training cohort and two external validation cohorts. Considering the importance of the TGF-β signaling pathway in immune regulation, we evaluated the prediction of the TGF-β score for immunological characteristics and the possible application of the immunotherapeutic response using six algorithms (TIMER, CIBERSORT, QUANTISEQ, MCP-counter, XCELL and EPIC) and three immunotherapy cohorts (GSE78820, Imvigor-210 and PRJEB23709). Notably, we compared our risk signature with the signature in ten publications in the meta-cohort (TCGA-LGG, CGGA-693 and CGGA-325), and the TGF-β score had the best predictive efficiency (C-index =0.812).</p><p><strong>Conclusion: </strong>In conclusion, our findings suggest that TGF-β signaling pathway-related signatures are prognostic biomarkers in LGG and provide a novel tool for tumor microenvironment (TME) assessment.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"610-621"},"PeriodicalIF":2.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10634610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Predictive Modelling of Overall Survival in Adult Patients with Primary Diffuse Large B-cell Lymphoma of the Breast Using the Surveillance, Epidemiology, and End Results (SEER) Database. 利用监测、流行病学和最终结果 (SEER) 数据库建立原发性乳腺弥漫性大 B 细胞淋巴瘤成人患者总生存期的预测模型。
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892818666230718153721
Yishuai Liu, Haifeng Han, Hong Wei, Xinlong Wang, Zhaotang Luan, Kun Jiang
{"title":"Predictive Modelling of Overall Survival in Adult Patients with Primary Diffuse Large B-cell Lymphoma of the Breast Using the Surveillance, Epidemiology, and End Results (SEER) Database.","authors":"Yishuai Liu, Haifeng Han, Hong Wei, Xinlong Wang, Zhaotang Luan, Kun Jiang","doi":"10.2174/1574892818666230718153721","DOIUrl":"10.2174/1574892818666230718153721","url":null,"abstract":"<p><strong>Objective: </strong>We aimed to identify critical clinical features to develop an accurate webbased prediction model for estimating the overall survival (OS) of primary breast diffuse large Bcell lymphoma (PB-DLBCL) adult patients.</p><p><strong>Methods: </strong>We first included all PB-DLBCL cases with available covariates retrieved from the Surveillance, Epidemiology, and End Results database. We sequentially performed univariate and multivariate Cox regression approaches to identify the predictors independently associated with prognosis, and all the predictors that passed these tests were then constructed to build a nomogram for predicting 3-, 5-, and 10-year survival rates of patients. The C-index and the receiver operating characteristic curve (ROC) were used to evaluate the prediction discrimination, and the calibration curve was applied to estimate the calibration.</p><p><strong>Results: </strong>A total of PB-DLBCL adult patients were included (median age was 69 with the interquartile range [IQR] of 57-79 years), of which 466 (70%) were randomly allocated to the development cohort, and the remaining cases were collected for validation. Using three identified independent predictors (i.e., age, stage, and radiation), an accurate nomogram for predicting OS was developed and validated. The C-indices of our nomogram were both relatively acceptable, with 0.74 (95% CI: 0.71-0.78) and 0.72 (95% CI: 0.70-0.75) for the development and validation cohorts, respectively. The calibration curves also accurately predicted the prognosis of PB-DLBCL in all cases. In addition, ROC curves showed our nomogram to possess superior predictive ability compared to any single variable. To visually present this prediction model, a convenient webbased tool was implemented based on our prognostic nomogram.</p><p><strong>Conclusion: </strong>For patients with PB-DLBCL, a more convenient and accurate web-based prediction model was developed and validated, which showed relatively good performances in both discrimination and calibration during model development and validation. External evaluation and validation are warranted by further independent studies.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"373-382"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10190069","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Adverse Effects of Gefitinib on Skin and Colon in a Lung Cancer Mouse Model. 吉非替尼对肺癌小鼠模型皮肤和结肠的不良影响
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892818666230727143750
Yalei Wang, Shuo Cheng, Huawei Zhang, Yali Zhang, Chengcheng Ding, Tiantian Peng, Weihang Chen, Ke Yang, Jiani Zhang, Yan Tan, Xu Wang, Zhaoheng Liu, Peng Wei, Miao Jiang, Qian Hua
{"title":"Adverse Effects of Gefitinib on Skin and Colon in a Lung Cancer Mouse Model.","authors":"Yalei Wang, Shuo Cheng, Huawei Zhang, Yali Zhang, Chengcheng Ding, Tiantian Peng, Weihang Chen, Ke Yang, Jiani Zhang, Yan Tan, Xu Wang, Zhaoheng Liu, Peng Wei, Miao Jiang, Qian Hua","doi":"10.2174/1574892818666230727143750","DOIUrl":"10.2174/1574892818666230727143750","url":null,"abstract":"<p><strong>Background: </strong>Gefitinib, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR-TKI), frequently causes side effects when used to treat non-small cell lung cancer.</p><p><strong>Objective: </strong>The purpose of this experiment was to investigate the side effect of gefitinib on the skin and colon of mice.</p><p><strong>Methods: </strong>Male Balb/c nu-nu nude mice aged 4-5 weeks were used as xenograft tumor models, and gefitinib at 150 mg/kg and 225 mg/kg was started at 9 days after the xenograft tumor grew out. The mice's weights and tumor volumes were tracked concurrently, and the mouse skin adverse reactions and diarrhea were observed during the treatment. The animal tissues were subjected to biochemical and pathological evaluations after 14 days.</p><p><strong>Results: </strong>Gefitinib effectively decreased the size and weight of transplanted tumors in nude mice, while also lowering body weight and raising indexes of the liver and spleen. Gefitinib could cause skin adverse reactions and diarrhea in mice. Further pathological investigation revealed tight junction- related markers in the mice's skin and colon to be reduced and macrophages and neutrophils to be increased after gefitinib treatment.</p><p><strong>Conclusion: </strong>The findings imply that gefitinib has negative effects on the skin and colon. Gefitinib- induced skin and colon adverse reactions in mice have been successfully modeled in this study.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"308-315"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10363175","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Development of a Novel Lipid Metabolism-related Gene Prognostic Signature for Patients with Colorectal Cancer. 为结直肠癌患者开发新的脂质代谢相关基因预后特征。
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892818666230731121815
Jing Zhan, Wei Cen, Junchang Zhu, Yunliang Ye
{"title":"Development of a Novel Lipid Metabolism-related Gene Prognostic Signature for Patients with Colorectal Cancer.","authors":"Jing Zhan, Wei Cen, Junchang Zhu, Yunliang Ye","doi":"10.2174/1574892818666230731121815","DOIUrl":"10.2174/1574892818666230731121815","url":null,"abstract":"<p><strong>Background: </strong>The purpose of this study was to explore the expression profiles of lipid metabolism-related genes in patients with Colorectal Cancer (CRC).</p><p><strong>Methods: </strong>The lipid metabolism statuses of CRC patients from The Cancer Genome Atlas (TCGA) were analyzed. Risk characteristics were constructed by univariate Cox regression and minimum Absolute contraction and Selection Operator (LASSO) Cox regression. A histogram was constructed based on factors such as age, sex, TNM stage, T stage, N stage, and risk score to provide a visual tool for clinicians to predict the probability of 1-year, 3-year, and 5-year OS for CRC patients. By determining Area Under Curve (AUC) values, the time-dependent Receiver Operating characteristic Curve (ROC) was used to evaluate the efficiency of our model in predicting prognosis.</p><p><strong>Results: </strong>A novel risk signal based on lipid metabolism-related genes was constructed to predict the survival of CRC patients. Risk characteristics were shown to be an independent prognostic factor in CRC patients (p <0.001). There were significant differences in the abundance and immune characteristics of tumor-filtering immune cells between high-risk and low-risk groups. The nomogram had a high potential for clinical application and the ROC AUC value was 0.827. Moreover, ROC analysis demonstrated that the nomogram model was more accurate to predict the survival of CRC patients than age, gender, stage and risk score.</p><p><strong>Conclusion: </strong>In this study, we demonstrated a lipid metabolism-related genes prognosis biomarker associated with the tumor immune micro-environment in patients with CRC.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"209-222"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10363171","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Integrating Bioinformatics and Drug Sensitivity Analyses to Identify Molecular Characteristics Associated with Targeting Necroptosis in Breast Cancer and their Clinical Prognostic Significance. 整合生物信息学和药物敏感性分析,识别与乳腺癌坏死相关的分子特征及其临床预后意义
IF 2.5 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892819666230831112815
Chang Zheng, Hanbin Guo, Yongpan Mo, Guowen Liu
{"title":"Integrating Bioinformatics and Drug Sensitivity Analyses to Identify Molecular Characteristics Associated with Targeting Necroptosis in Breast Cancer and their Clinical Prognostic Significance.","authors":"Chang Zheng, Hanbin Guo, Yongpan Mo, Guowen Liu","doi":"10.2174/1574892819666230831112815","DOIUrl":"10.2174/1574892819666230831112815","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Breast cancer accounts for over 1.8 million new cases worldwide annually, and prompt diagnosis and treatment are imperative to prevent mortality. Necroptosis, a form of programmed cell death, is thought to be a critical pathway for cancer cell apoptosis, yet, its relationship with breast cancer progression and molecular mechanisms remains largely unexplored.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Objectives: &lt;/strong&gt;Our study aims to investigate the molecular characteristics and clinical prognostic value of necroptosis-related genes in breast cancer using a comprehensive approach that involves integrated bioinformatics analysis along with drug sensitivity assessment.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Transcriptional, clinical, and tumor mutation burden (TMB) data related to breast cancer from the TCGA and GEO databases were integrated, and the necroptosis gene set was downloaded from the GSEA website for analysis. The screening conditions were set as adjusted p &lt; 0.05 and |log2FC(fold change)| &gt; 0.585 to screen for differential expression genes related to breast cancer necroptosis. Survival prognosis analysis was conducted on breast cancer necroptosis genes. Further analysis was conducted on prognosis-related necroptosis genes, including immune infiltration analysis and GO/KEGG enrichment analysis, to explore the potential biological functions and signaling pathway mechanisms of breast cancer necroptosis genes. Drug sensitivity screening was conducted on the prognosis-related necroptosis to identify potential drugs that target the promotion of necroptosis gene expression, and ultimately, single-gene analysis was performed on the core target genes obtained.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;Through integrated bioinformatics analysis, 29 differentially expressed mRNAs related to BRCA-Necroptosis were identified, including 18 upregulated mRNAs and 11 downregulated mRNAs. In addition, single-factor analysis of differential genes showed that the expression of HSPA4, PLK1, TNFRSF1B, FLT3, and LEF1 was closely related to BRCA survival prognosis. Based on the expression of these genes, a breast cancer prognosis model was constructed, and it was found that the area under the curve (AUC) of the curve of the risk genes for necroptosis was the largest, indicating that these genes have a certain clinical predictive significance for the occurrence and prognosis of BRCA. Additionally, there were significant differences in clinical characteristics of BRCA patients with different necroptosis gene expressions. Furthermore, GSVA and immune infiltration analysis revealed that Necroptosis-DEGs mainly affect the occurrence and progression of BRCA by participating in immune functions such as APC co-inhibition, APC costimulation, CCR, checkpoint, as well as infiltrating immune cells such as B cells naive, plasma cells, and T cells CD8. Moreover, the necroptosis gene group column chart indicated a 1-year survival rate of 0.979, a 3-year survival rate of 0.883, and a ","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"681-694"},"PeriodicalIF":2.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10129931","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New 1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-2-phenylisoquinoline-1(2H)-ones as Phosphoinositide 3-kinase Inhibitors for Treating Cancer and Other Diseases. 新的 1H-吡唑并[3,4-d]嘧啶-1-基)乙基)-2-苯基异喹啉-1(2H)-酮作为治疗癌症和其他疾病的磷酸肌酸 3-激酶抑制剂。
IF 2.8 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892818666230228153103
Surya K De
{"title":"New 1<i>H</i>-pyrazolo[3,4-<i>d</i>]pyrimidin-1-yl)ethyl)-2-phenylisoquinoline-1(2<i>H</i>)-ones as Phosphoinositide 3-kinase Inhibitors for Treating Cancer and Other Diseases.","authors":"Surya K De","doi":"10.2174/1574892818666230228153103","DOIUrl":"10.2174/1574892818666230228153103","url":null,"abstract":"<p><p>The patent describes novel useful compounds, such as PI3K protein kinase inhibitors, in particular as PI3K delta (δ) and/or gamma (γ) protein kinase modulators. The present disclosure also provides methods for preparing PI3K protein kinase inhibitors, pharmaceutical compositions containing them, and methods of treatment, prevention, and amelioration of PI3K kinase-mediated diseases, and disorders.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"253-255"},"PeriodicalIF":2.8,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10791262","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Natural STAT3 Inhibitors for Cancer Treatment: A Comprehensive Literature Review. 用于癌症治疗的天然 STAT3 抑制剂:综合文献综述
IF 2.5 4区 医学
Recent patents on anti-cancer drug discovery Pub Date : 2024-01-01 DOI: 10.2174/1574892818666230803100554
Seyed Mahdi Zarezadeh, Amir Mohammad Sharafi, Gisou Erabi, Arefeh Tabashiri, Navid Teymouri, Hoda Mehrabi, Seyyed Amirhossein Golzan, Arezoo Faridzadeh, Zahra Abdollahifar, Nafiseh Sami, Javad Arabpour, Zahra Rahimi, Arina Ansari, Mohammad Reza Abbasi, Nima Azizi, Amirhossein Tamimi, Mohadeseh Poudineh, Niloofar Deravi
{"title":"Natural STAT3 Inhibitors for Cancer Treatment: A Comprehensive Literature Review.","authors":"Seyed Mahdi Zarezadeh, Amir Mohammad Sharafi, Gisou Erabi, Arefeh Tabashiri, Navid Teymouri, Hoda Mehrabi, Seyyed Amirhossein Golzan, Arezoo Faridzadeh, Zahra Abdollahifar, Nafiseh Sami, Javad Arabpour, Zahra Rahimi, Arina Ansari, Mohammad Reza Abbasi, Nima Azizi, Amirhossein Tamimi, Mohadeseh Poudineh, Niloofar Deravi","doi":"10.2174/1574892818666230803100554","DOIUrl":"10.2174/1574892818666230803100554","url":null,"abstract":"<p><p>Cancer is one of the leading causes of mortality and morbidity worldwide, affecting millions of people physically and financially every year. Over time, many anticancer treatments have been proposed and studied, including synthetic compound consumption, surgical procedures, or grueling chemotherapy. Although these treatments have improved the daily life quality of patients and increased their survival rate and life expectancy, they have also shown significant drawbacks, including staggering costs, multiple side effects, and difficulty in compliance and adherence to treatment. Therefore, natural compounds have been considered a possible key to overcoming these problems in recent years, and thorough research has been done to assess their effectiveness. In these studies, scientists have discovered a meaningful interaction between several natural materials and signal transducer and activator of transcription 3 molecules. STAT3 is a transcriptional protein that is vital for cell growth and survival. Mechanistic studies have established that activated STAT3 can increase cancer cell proliferation and invasion while reducing anticancer immunity. Thus, inhibiting STAT3 signaling by natural compounds has become one of the favorite research topics and an attractive target for developing novel cancer treatments. In the present article, we intend to comprehensively review the latest knowledge about the effects of various organic compounds on inhibiting the STAT3 signaling pathway to cure different cancer diseases.</p>","PeriodicalId":20774,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":"403-502"},"PeriodicalIF":2.5,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10302436","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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