Recent patents on anti-cancer drug discovery最新文献

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The Present State and Potential Applications of Artificial Intelligence in Cancer Diagnosis and Treatment.
Recent patents on anti-cancer drug discovery Pub Date : 2025-02-03 DOI: 10.2174/0115748928361472250123105507
Anuja Mishra, Srishti Sharma, Swaroop Kumar Pandey
{"title":"The Present State and Potential Applications of Artificial Intelligence in Cancer Diagnosis and Treatment.","authors":"Anuja Mishra, Srishti Sharma, Swaroop Kumar Pandey","doi":"10.2174/0115748928361472250123105507","DOIUrl":"https://doi.org/10.2174/0115748928361472250123105507","url":null,"abstract":"<p><p>An aberrant increase in cancer incidences has demanded extreme attention globally despite advancements in diagnostic and management strategies. The high mortality rate is concerning, and tumour heterogeneity at the genetic, phenotypic, and pathological levels exacerbates the problem. In this context, lack of early diagnostic techniques and therapeutic resistance to drugs, sole awareness among the public, coupled with the unavailability of these modern technologies in developing and low-income countries, negatively impact cancer management. One of the prime necessities of the world today is the enhancement of early detection of cancers. Several independent studies have shown that screening individuals for cancer can improve patient survival but are bogged down by risk classification and major problems in patient selection. Artificial intelligence (AI) has significantly advanced the field of oncology, addressing various medical challenges, particularly in cancer management. Leveraging extensive medical datasets and innovative computational technologies, AI, especially through deep learning (DL), has found applications across multiple facets of oncology research. These applications range from early cancer detection, diagnosis, classification, and grading, molecular characterization of tumours, prediction of patient outcomes and treatment responses, personalized treatment, and novel anti-cancer drug discovery. Over the past decade, AI/ML has emerged as a valuable tool in cancer prognosis, risk assessment, and treatment selection for cancer patients. Several patents have been and are being filed and granted. Some of those inventions were explored and are being explored in clinical settings as well. In this review, we will discuss the current status, recent advancements, clinical trials, challenges, and opportunities associated with AI/ML applications in cancer detection and management. We are optimistic about the potential of AI/ML in improving outcomes for cancer and the need for further research and development in this field.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143124249","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
Unveiling miR-1468-5p: A New Prognostic Biomarker and Therapeutic Target in Lung Adenocarcinoma.
Recent patents on anti-cancer drug discovery Pub Date : 2025-02-03 DOI: 10.2174/0115748928344326240927071620
Yi Chen, Dongbing Li, Yueyu Fang
{"title":"Unveiling miR-1468-5p: A New Prognostic Biomarker and Therapeutic Target in Lung Adenocarcinoma.","authors":"Yi Chen, Dongbing Li, Yueyu Fang","doi":"10.2174/0115748928344326240927071620","DOIUrl":"https://doi.org/10.2174/0115748928344326240927071620","url":null,"abstract":"<p><strong>Background: </strong>miR-1468-5p, a type of microRNA, is acknowledged for its crucial involvement in a variety of cancerous processes. Nonetheless, the specific impact of this microRNA on lung adenocarcinoma (LUAD) has not yet been clearly defined.</p><p><strong>Objective: </strong>Our aim was to investigate how miR-1468-5p influences LUAD.</p><p><strong>Methods: </strong>The Cancer Genome Atlas (TCGA) offered specimens for our research. Employing statistical techniques, we assessed the diagnostic and prognostic significance of miR-1468-5p, as well as its association with clinical characteristics. Our analysis delved into the target genes and the regulatory mechanisms influenced by miR-1468-5p. The expression levels of miR-1468-5p in LUAD cell lines were validated through quantitative reverse transcription polymerase chain reaction (qRT-PCR).</p><p><strong>Results: </strong>The expression of miR-1468-5p varied significantly across different cancer types. The presence of reduced miR-1468-5p levels was correlated with a lower likelihood of overall survival in LUAD patients, with a statistically significant result (p = 0.005). miR-1468-5p demonstrated independent prognostic significance in LUAD and potentially contributes to disease progression via multiple pathways, including the HIF-1 signaling pathway and more. There was a significant reduction in miR-1468-5p expression in LUAD cell lines when compared to cells of the normal lung epithelium.</p><p><strong>Conclusion: </strong>miR-1468-5p may serve as a useful patent as a therapeutic intervention target and a prognostic indicator for LUAD patients.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143124252","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
Organosulfur Compounds in Garlic for Gastric Cancer Treatment: Anticancer Effects, Overcoming Drug Resistance, and Mechanisms.
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-29 DOI: 10.2174/0115748928367900250116074925
Xudong Yi, Jinrui Zhang, Yiman Yao, Junyu Liu, Mingyue Li, Min Zhang, Anat Elmann, Haixia Chen
{"title":"Organosulfur Compounds in Garlic for Gastric Cancer Treatment: Anticancer Effects, Overcoming Drug Resistance, and Mechanisms.","authors":"Xudong Yi, Jinrui Zhang, Yiman Yao, Junyu Liu, Mingyue Li, Min Zhang, Anat Elmann, Haixia Chen","doi":"10.2174/0115748928367900250116074925","DOIUrl":"https://doi.org/10.2174/0115748928367900250116074925","url":null,"abstract":"<p><p>Garlic <i>(Allium sativum L.)</i> has been consumed globally as a functional food and traditional medicine for various ailments. Its active organosulfur compounds (OSCs) have demonstrated significant anticancer properties, particularly against gastric cancer. However, a comprehensive review of these effects and the underlying molecular mechanisms, including their role in overcoming drug resistance, is currently lacking. This review systematically examines both preclinical and clinical studies on the anticancer effects of garlic and its organosulfur compounds against gastric cancer, with a focus on patents. Emphasis is placed on explaining the mechanisms of action, exploring how these compounds can overcome drug resistance, and highlighting relevant patents that have been granted in this field. The literature search included databases, like PubMed, Web of Science, Google Scholar, ScienceDirect, and patent databases, including articles and patents published up to October 2024. Preclinical studies demonstrate that garlic-derived organosulfur compounds possess anticancer activities against gastric cancer. They work through multiple mechanisms, including inducing apoptosis, causing cell cycle arrest, inhibiting cancer stem cell properties, suppressing epithelial-mesenchymal transition, and modulating key signaling pathways, like PI3K/Akt and NF-κB. These compounds also show potential in overcoming drug resistance by downregulating multidrug resistance proteins and enhancing the effectiveness of standard chemotherapy drugs. Clinical studies suggest that regular garlic consumption may reduce the risk of gastric cancer and improve outcomes in patients undergoing chemotherapy. This review highlights the significant potential of garlic's organosulfur compounds as complementary agents in gastric cancer prevention and treatment and emphasizes the relevance of existing patents and the need for further clinical trials to confirm these effects and develop effective therapeutic strategies.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143070488","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
A Three-agent Regimen for Triple Negative Breast Cancer Treatment. 三阴性乳腺癌的三药治疗方案。
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-17 DOI: 10.2174/0115748928350267250105153944
Shaojun Wang, Congxiu Huang, Ying Zhu, Min Wang, Wei Wang, Caixia Liu, Wuyun Su
{"title":"A Three-agent Regimen for Triple Negative Breast Cancer Treatment.","authors":"Shaojun Wang, Congxiu Huang, Ying Zhu, Min Wang, Wei Wang, Caixia Liu, Wuyun Su","doi":"10.2174/0115748928350267250105153944","DOIUrl":"https://doi.org/10.2174/0115748928350267250105153944","url":null,"abstract":"<p><strong>Background: </strong>Triple-negative breast cancer (TNBC) has a poor prognosis with current treatment options. Novel therapeutic strategies are urgently needed to enhance treatment outcomes for TNBC.</p><p><strong>Objective: </strong>This study evaluated the efficacy of a three-agent regimen compared to existing treatment regimens in a TNBC mouse model, and elucidated its potential mechanisms of action.</p><p><strong>Methods: </strong>The TNBC xenograft tumor mouse model was established using a 4T1 cell line in female BALB/c mice. Mice were treated with the three-agent regimen and other comparative treatments. Tumor volume was monitored to assess the anti-tumor effects. Biochemical and pathological evaluations were conducted to examine the impact of the regimen on anti-tumor immunity, anti- tumor angiogenesis, and tumor cell apoptosis.</p><p><strong>Results: </strong>The three-agent regimen consisting of SIN+BEV+PAB demonstrated significant anti-tumor efficacy compared to controls, PAB alone, SIN+PAB, and BEV+PAB groups from day 9 of drug administration. The superior anti-tumor effect of SIN+BEV+PAB was primarily attributed to enhanced anti-tumor immunity, evidenced by increased percentages of CD4+ and CD8+ T cells, elevated IFN-γ levels, and decreased percentages of Tregs, reduced levels of TGF-β, IL-6, and IL-10. Additionally, the regimen showed potent anti-angiogenic effects by reducing VEGF expression and micro vessel density (MVD). Furthermore, it promoted tumor cell apoptosis through upregulation of BAX and cleaved caspase3, while downregulating Bcl2.</p><p><strong>Conclusion: </strong>These findings suggest that the novel three-agent combination of SIN+BEV+PAB may prove beneficial in improving treatment outcomes for patients with TNBC. The development of this regimen, which may be eligible for patent protection, could facilitate its introduction as a new therapeutic option for advanced TNBC in clinical practice.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143019146","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
Ubiquitination-related Gene UBTD1 Mediates Poor Prognosis of Colorectal Cancer and Affects Colorectal Cancer Cell Proliferation and Ferroptosis. 泛素化相关基因UBTD1介导结直肠癌不良预后并影响结直肠癌细胞增殖和铁凋亡
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-15 DOI: 10.2174/0115748928323408241002131753
Yuzhao Jin, Luyu Liao, Qianping Chen, Bufu Tang, Jin Jiang, Ji Zhu, Minghua Bai, Lingjiao Guo
{"title":"Ubiquitination-related Gene UBTD1 Mediates Poor Prognosis of Colorectal Cancer and Affects Colorectal Cancer Cell Proliferation and Ferroptosis.","authors":"Yuzhao Jin, Luyu Liao, Qianping Chen, Bufu Tang, Jin Jiang, Ji Zhu, Minghua Bai, Lingjiao Guo","doi":"10.2174/0115748928323408241002131753","DOIUrl":"https://doi.org/10.2174/0115748928323408241002131753","url":null,"abstract":"<p><strong>Background: </strong>Colorectal cancer (CRC) is the third most common cancer worldwide, and its occurrence and progression are often regulated by genetic and hereditary factors. Ubiquitination and the associated ubiquitin-binding enzymes and ligases regulate the tumor microenvironment and antitumor immunity to mediate tumor pathogenesis and progression. In this study, we examined the molecular characteristics and immunomodulatory effects of ubiquitination-associated genes that mediate CRC prognosis.</p><p><strong>Methods: </strong>The ubiquitination-related gene ubiquitin domain-containing protein 1 (UBTD1) was identified using bioinformatics and single-cell analyses. Subsequently, the ability of UBTD1 to predict CRC prognosis and immune checkpoint correlation was analyzed, the potential drug telatinib targeting UBTD1 was explored, and the correlation between UBTD1 and ferroptosis was analyzed. The role of UBTD1 in CRC and ferroptosis was verified using immunohistochemistry, gene knockout, western blot, cell cloning, and immunofluorescence.</p><p><strong>Results: </strong>UBTD1 was identified as a significant prognostic and predictive gene for CRC and was involved in regulating immune checkpoint levels and immune cell function of CRC patients with CRC. High UBTD1 expression was found to enhance the presence of immune checkpoints that induce immune escape and inhibit ferroptosis onset. Telatinib may be a potential therapeutic drug targeting UBTD1.</p><p><strong>Conclusion: </strong>Our study demonstrated that UBTD1 is a prognostic marker for CRC in the regulation of ubiquitination and the tumor immune microenvironment and may serve as a modulator of ferroptosis.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143019150","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
Effect of Oral Posaconazole on Venetoclax Plasma Concentration and its Efficacy in Patients with Acute Myeloid Leukemia. 口服泊沙康唑对急性髓系白血病患者Venetoclax血药浓度及疗效的影响。
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-08 DOI: 10.2174/0115748928330206241104161111
Mengqi Guo, Yingzhi He, Jingwen Du, Dezhi Qiu, Yinjie Qin, Yuxian Huang
{"title":"Effect of Oral Posaconazole on Venetoclax Plasma Concentration and its Efficacy in Patients with Acute Myeloid Leukemia.","authors":"Mengqi Guo, Yingzhi He, Jingwen Du, Dezhi Qiu, Yinjie Qin, Yuxian Huang","doi":"10.2174/0115748928330206241104161111","DOIUrl":"https://doi.org/10.2174/0115748928330206241104161111","url":null,"abstract":"<p><strong>Background: </strong>BCL-2 was the first gene identified to have antiapoptotic effects, and venetoclax is an oral selective BCL-2 inhibitor, which has great potential in the treatment of patients with acute myeloid leukemia (AML) who are not candidates for intensive therapy. Notably, posaconazole, an oral antifungal drug, is also a strong factor that can affect blood venetoclax concentrations. To the best of our knowledge, the relationship between BCL-2 expression, posaconazole, and venetoclax, as well as their influence on treatment efficacy and the prognosis of patients with AML, has not been reported.</p><p><strong>Objectives: </strong>In this single-center retrospective study, the relationship between BCL-2 expression and blood venetoclax concentration was analyzed in 35 patients with AML. After that, we explored the differences in curative effect, adverse reactions, and outcomes between patients with different BCL-2 expression levels and patients with different venetoclax concentration levels, respectively.</p><p><strong>Methods: </strong>BCL-2 mRNA expression levels were examined by reverse transcription quantitative PCR. Blood venetoclax concentrations were measured using high-performance liquid chromatography- tandem mass spectrometry.</p><p><strong>Results: </strong>The results revealed that among patients with AML, those with lower primary BCL-2 expression had a higher complete remission (CR) rate (p =0.005), overall response (OR) rate (p <0.0001), and progression-free survival time (p =0.04). Posaconazole was revealed to be a strong factor that was able to increase blood venetoclax concentration (p <0.001) and CR rate in the venetoclax plus posaconazole group compared to that in the venetoclax monotherapy group (p =0.002); however, no significant difference was identified in the occurrence of adverse reactions between these groups. Among low and high-blood venetoclax concentration groups, the event-free survival of the former group was significantly higher (p =0.013).</p><p><strong>Conclusion: </strong>Higher levels of BCL-2 expression at initial diagnosis may have adverse effects on the efficacy and prognosis of patients, and higher levels of venetoclax concentration may advance the time of adverse reactions in patients, thus adversely affecting event-free survival (EFS).</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142960581","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
A Single-Arm, Open-Label, Phase Ib Clinical Study Evaluating the Efficacy and Safety of Durvalumab in Combination with Albumin-Bound Paclitaxel and Carboplatin as Neoadjuvant Therapy for Resectable Stage III Non-Small Cell Lung Cancer. 一项单臂、开放标签、Ib期临床研究评估Durvalumab联合白蛋白结合紫杉醇和卡铂作为可切除的III期非小细胞肺癌的新辅助治疗的有效性和安全性。
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-06 DOI: 10.2174/0115748928304000240429120252
Yuejiao Zhong, Tao Li, Zhaoshi Bai, Ninglei Qiu, Siwen Liu, Wenjia Xia, Qiang Wei, Lingxiang Chen
{"title":"A Single-Arm, Open-Label, Phase Ib Clinical Study Evaluating the Efficacy and Safety of Durvalumab in Combination with Albumin-Bound Paclitaxel and Carboplatin as Neoadjuvant Therapy for Resectable Stage III Non-Small Cell Lung Cancer.","authors":"Yuejiao Zhong, Tao Li, Zhaoshi Bai, Ninglei Qiu, Siwen Liu, Wenjia Xia, Qiang Wei, Lingxiang Chen","doi":"10.2174/0115748928304000240429120252","DOIUrl":"https://doi.org/10.2174/0115748928304000240429120252","url":null,"abstract":"<p><strong>Objective: </strong>This study aimed to explore the clinical efficacy and safety of durvalumab combined with albumin-bound paclitaxel and carboplatin as neoadjuvant therapy for resectable stage III Non-small Cell Lung Cancer (NSCLC).</p><p><strong>Methods: </strong>A single-arm open-label phase Ib study was conducted. A total of 40 patients with driver gene-negative resectable stage III NSCLC were enrolled. All patients received neoadjuvant treatment with durvalumab in combination with albumin-bound paclitaxel and carboplatin. The clinical efficacy, Major Pathological Response (MPR), Complete Pathological Response (pCR), and safety were assessed. Flow cytometry was used to detect the expression of programmed cell death receptor 1 (PD-1) on total T, helper T, and cytotoxic T lymphocytes in peripheral blood before and after neoadjuvant treatment. Adverse reactions during the treatment were recorded. Disease- free Survival (DFS) and Overall Survival (OS) curves were constructed.</p><p><strong>Results: </strong>After the neoadjuvant treatment, the overall Objective Response Rate (ORR) in the 40 patients with NSCLC was 65.00%. MPR was achieved in 27 patients (67.50%), and pCR was achieved in nine patients (22.50%). The expression levels of PD-1 on total T, helper T, and cytotoxic T lymphocytes in patients with NSCLC significantly decreased after treatment (all p < 0.05). The most common adverse events were hair loss (47.50%), nausea and vomiting (42.50%), and fatigue (40.00%). The majority of adverse events were grades 1 and 2, with a small number of events being grades 3 and 4. At the end of the follow-up period, the average DFS was 21.49 ± 0.99 months, and the average OS was 24.79 ± 0.53 months.</p><p><strong>Conclusion: </strong>Neoadjuvant treatment with durvalumab combined with albumin-bound paclitaxel and carboplatin as first-line therapy for driver gene-negative stage III NSCLC achieved a high pathological response rate and improved immune function. It is expected to extend patient survival with good tolerability.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142960575","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
Differential Expression and Distribution of Slco4a1 and Slco1b2 in an Internal Environment Disorder-induced Hepatocellular Carcinoma Mouse Model. Slco4a1和Slco1b2在内环境紊乱性肝癌小鼠模型中的差异表达和分布
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-03 DOI: 10.2174/0115748928351523241204071335
Haoxuan Luo, Yang Xie, Shan Huang, Yu Zhang
{"title":"Differential Expression and Distribution of Slco4a1 and Slco1b2 in an Internal Environment Disorder-induced Hepatocellular Carcinoma Mouse Model.","authors":"Haoxuan Luo, Yang Xie, Shan Huang, Yu Zhang","doi":"10.2174/0115748928351523241204071335","DOIUrl":"https://doi.org/10.2174/0115748928351523241204071335","url":null,"abstract":"<p><strong>Objective: </strong>This study aims to enhance the understanding of underlying mechanisms and potential therapies of the solute carrier organic anion (SLCO) transporter family in internal environment disorder (IED)-induced hepatocellular carcinoma (HCC). This could lead to new therapeutic strategies and offer new directions for the creation of new patents for HCC treatment products.</p><p><strong>Methods: </strong>The orthotopic transplantation (OT), IED and IED-based OT (IED-OT) mouse models were established. Expression patterns of Slco4a1 and Slco1b2 were determined using reverse transcriptionquantitative polymerase chain reaction (RT-qPCR), western blotting (WB) and immunohistochemistry (IHC) in various tissues, including lung, stomach, liver, spleen, kidney, colon, small intestine, HCC tissues and adjacent non-cancerous tissues.</p><p><strong>Results: </strong>Animals exhibited symptoms, including weight loss, lethargy, chills, dyspnea, altered hair texture, and gastrointestinal disturbances, confirming the successful establishment of the IED model. The analysis demonstrated differential expression and tissue-specific distribution of Slco4a1 and Slco1b2, which are associated with IED-induced changes. These alterations potentially disrupt organ transport functions, thereby promoting the development of HCC. Additionally, they suggest a role in rebalancing the tumor microenvironment and mitigating damage resulting from abnormal substance accumulation.</p><p><strong>Conclusions: </strong>Changes in SLCO expression and distribution induced by IED may play pivotal roles in the development of HCC. These findings contribute insights that could inform novel therapeutic strategies against HCC.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142960578","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
Covalent Inhibitor Screening for Targeting LOXL2: Studied by Virtual Screening and Experimental Validation. 针对LOXL2的共价抑制剂筛选:虚拟筛选和实验验证研究。
Recent patents on anti-cancer drug discovery Pub Date : 2025-01-02 DOI: 10.2174/0115748928356643241216132041
Lirui Lin, Kai Lin, Lichun Chen, Yiwen Wang, Li-Yan Xu, En-Min Li, Qingping Liu, Haiying Zou, Geng Dong
{"title":"Covalent Inhibitor Screening for Targeting LOXL2: Studied by Virtual Screening and Experimental Validation.","authors":"Lirui Lin, Kai Lin, Lichun Chen, Yiwen Wang, Li-Yan Xu, En-Min Li, Qingping Liu, Haiying Zou, Geng Dong","doi":"10.2174/0115748928356643241216132041","DOIUrl":"https://doi.org/10.2174/0115748928356643241216132041","url":null,"abstract":"<p><strong>Background: </strong>Lysyl oxidase-like 2 (LOXL2) is a metalloenzyme that catalyzes oxidative deamination ε-amino group of lysine. It has been found that LOXL2 is a promotor for the metastasis and invasion in kinds of tumors. Previous studies show that disulfide bonds are important components in LOXL2, and their bioactivity can be regulated by those bonds. In this way, a small molecule covalently binds to the thiol group of cysteine residue could be an effective way to change the function of LOXL2 by blocking the formation of the disulfide bond.</p><p><strong>Objective: </strong>This investigation is aiming to screen covalent inhibitor for LOXL2.</p><p><strong>Methods: </strong>Covalent molecule libraries of Life Chemical and Enamine were used. The structures of those molecules were optimized by using LigPrep module of Schrödinger. Then optimized by using the LigPrep module of Schrödinger to generate optimal conformations. For covalent docking, CovDock in Glide module was used for the virtual screening. Finally, wound-healing assays were performed to examine the effects of the potential inhibitors.</p><p><strong>Results: </strong>Eight potential small molecules were selected by covalent docking from the databases (in total 7,908 candidates). ADMET evaluation indicated that all those eight small molecules satisfy the general standard. Furthermore, wound healing experiments showed that the compound (F50972176) significantly inhibits the migration of cancer cells.</p><p><strong>Conclusion: </strong>Virtual screening and experimental verification methods were used to screen covalent inhibitors of LOXL2 by targeting functional disulfide bonds. The compound (F50972176) effectively inhibited the migration of esophageal squamous cell carcinoma cells.</p>","PeriodicalId":94186,"journal":{"name":"Recent patents on anti-cancer drug discovery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142934149","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
Selinexor as a Therapeutic Target: Advances in Non-small Cell and Small Cell Lung Cancer Treatment Strategies. 作为治疗靶点的 Selinexor:非小细胞和小细胞肺癌治疗策略的进展》。
Recent patents on anti-cancer drug discovery Pub Date : 2024-10-29 DOI: 10.2174/0115748928322627241016120142
Bosheng Zheng, Wenqi Zhang, Shaonan Xie, Yaqing Han, Guangjie Liu, Yanjie Liu, Maogang Gao, Shize Wang, Qingyi Liu
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