Anti-cancer agents in medicinal chemistry最新文献

{"title":"ATP5B Expression as a Prognostic Biomarker in Solid Tumors: A Systematic Review and Meta-Analysis.","authors":"Shimeng Li, Lu Qiao, Boyao Sun, Jiaru Huang","doi":"10.2174/0118715206431798260121080228","DOIUrl":"https://doi.org/10.2174/0118715206431798260121080228","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Mitochondrial ATP synthase F1 subunit beta (ATP5B) is involved in the catalytic process of oxidative phosphorylation (OXPHOS). However, the prognostic value of ATP5B remains conflicting. Therefore, a systematic meta-analysis is needed to assess the prognostic value of ATP5B in solid tumors.</p><p><strong>Methods: </strong>A search for articles in multiple databases, including PubMed, Web of Science, China National Knowledge Infrastructure (CNKI), and Wanfang Data, was carried out for records up to June 1st, 2025. The analysis of the association between ATP5B expression levels and overall survival (OS) was conducted by calculating pooled hazard ratios (HRs) and 95% confidence intervals (CIs). Heterogeneity was measured via the I² statistic and Cochran's Q test. Subgroup analyses were performed to determine heterogeneity in ethnicity, cancer type, treatment regimen, data extraction method, sample size, and test target. Sensitivity and publication bias analyses were also performed.</p><p><strong>Results: </strong>This meta-analysis included 12 studies (15 cohorts) with 2,344 patients. The results showed that high ATP5B expression was significantly associated with poor OS (HR = 1.95, 95%CI: 1.29-2.94). In subgroup analyses, reduced heterogeneity between studies was observed in the melanoma subgroup (I² = 44%), in studies based on mRNA expression (I² = 0%), and in studies with large sample sizes (I² = 0%). No significant bias was detected in the publication bias analysis.</p><p><strong>Discussion: </strong>This first meta-analysis confirms the potential of ATP5B as a prognostic biomarker in solid tumors. High ATP5B expression is associated with poor prognosis, supporting its role as a pan-cancer indicator. More high-quality studies with large samples and standardized detection protocols are needed to further clarify the prognostic value of ATP5B, so that it may become a widely used biomarker in clinical practice.</p><p><strong>Conclusion: </strong>High ATP5B expression may independently predict inferior survival outcomes in patients with solid tumors.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607711","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}

{"title":"Natural Products for Overcoming EGFR-TKI Resistance in NSCLC: A Narrative Review.","authors":"Zhenzhen Guo, Yufei Ma, Changjiang Guo, Tingting Liu, Yue Yang, Mingyue Zhu, Fei Cao, Xiaohong Kang","doi":"10.2174/0118715206424271260109095114","DOIUrl":"https://doi.org/10.2174/0118715206424271260109095114","url":null,"abstract":"<p><strong>Introduction: </strong>Epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) has transformed the treatment of non-small cell lung cancer (NSCLC), yet acquired resistance remains a major challenge to its clinical efficacy. This review summarizes current advances in overcoming EGFR-TKI resistance with natural products and further discusses the emerging role of targeted protein degradation (TPD) as a complementary strategy to enhance the selective and irreversible clearance of resistant proteins.</p><p><strong>Methods: </strong>We conducted a comprehensive literature review using the PubMed database with the keywords \"natural products\", \"drug resistance\", \"EGFR-TKI\", \"targeted protein degradation\", and \"non-small cell lung cancer\".</p><p><strong>Results: </strong>Cumulative evidence indicates that a variety of natural products can reverse or mitigate EGFR-TKI resistance in NSCLC via multitarget modulation. These compounds have been shown to influence EGFR mutations, inhibit aberrant signaling pathways such as Phosphatidylinositol 3-Kinase (PI3K)/ Protein kinase B (PI3K/AKT), block histologic and phenotypic transformation, and reduce drug efflux. Moreover, natural product- based TPD approaches have shown initial promise in their potential to degrade resistance-associated targets and may enhance TKI sensitivity, hinting at possible therapeutic advantages.</p><p><strong>Discussion: </strong>The reviewed evidence collectively supports the versatility of natural products in counteracting EGFR-TKI resistance. Integration with TPD strategies appears synergistic and may help address the limitations of single-agent therapy.</p><p><strong>Conclusion: </strong>Natural products, particularly when combined with TPD approaches, represent a promising strategy for overcoming EGFR-TKI resistance in NSCLC and may contribute to the development of more effective targeted therapies.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147589432","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}

{"title":"Sulfonamides as Aromatase Inhibitors: Nimesulide Analogues, N-cyclic- and Aryl-Sulfonamides.","authors":"Cristina Maccallini, Alessandra Ammazzalorso, Barbara De Filippis, Marialuigia Fantacuzzi, Letizia Giampietro, Rosa Amoroso","doi":"10.2174/0118715206416396251122063142","DOIUrl":"https://doi.org/10.2174/0118715206416396251122063142","url":null,"abstract":"<p><p>Aromatase catalyzes the final and rate-limiting step in the biosynthesis of estrogens. Inhibitors of this key enzyme are used to treat hormone receptor-positive early, locally advanced, and metastatic breast cancers and are classified by structure into steroidal and nonsteroidal classes. Non-steroidal inhibitors, in particular, bind non-covalently to the heme moiety of aromatase and prevent the binding of the substrate androstenedione by saturating the binding site. Several aromatase inhibitors have been developed to date, most of which share a common pharmacophore: (i) one or two aromatic rings that contribute to hydrophobic interactions, (ii) a triazole or imidazole that coordinates with the heme iron of aromatase, and (iii) hydrophobic groups that help the molecule fit into the lipophilic binding pocket of aromatase. In recent years, several studies have focused on developing aromatase inhibitors containing a sulfonamide group, which can form significant interactions with aromatase due to its ability to participate in hydrogen bonding. This review aims to describe the most significant structure-activity relationships of nonsteroidal aromatase inhibitors containing a sulfonamide moiety, focusing on (i) biological results related to enzyme inhibition and (ii) interactions with active-site residues of aromatase identified through molecular modeling. Based on their core scaffold, the molecules are classified into (i) analogues of nimesulide, (ii) N-cyclic sulfonamides, and (iii) aryl-sulfonamides.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607714","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}

{"title":"Oleuropein and Colorectal Cancer Chemoprevention: Recent Advances into Cellular and Molecular Mechanisms.","authors":"Gaetano Leto","doi":"10.2174/0118715206437468260218075425","DOIUrl":"https://doi.org/10.2174/0118715206437468260218075425","url":null,"abstract":"<p><p>A growing number of epidemiological studies provide strong evidence regarding the significant association between Olive Oil (OO) consumption and reduced risk of colorectal cancer (CRC). The chemopreventive effects of OO on CRC growth and progression appear likely to be related to the presence, among various components, of \"minor bioactive compounds\", such as flavonoids, phenolic acids, alcohols, lignans, and secoiridoids, as these molecules have been shown to be endowed with antioxidant, anti-inflammatory, immunomodulatory, and anticancer properties. In particular, Oleuropein (Ole), the major glycosylated secoiridoid found in olive leaves and fruits of the olive tree (Olea europea L.), has attracted growing interest as this molecule exhibits a remarkable anticancer activity. The antitumor activity of Ole appears to rely on targeting multiple signalling pathways underlying cancer cell growth and progression. These observations further indicate a possible therapeutic role of this molecule in the prevention and treatment of human tumors. On the basis of these observations, a growing number of preclinical in vitro and in vivo investigations have been undertaken to unravel the specific mechanisms underlying the antitumor activity of Ole and to assess its potential therapeutic effectiveness in the prevention and treatment of CRC. The results from these studies underpin the potential clinical role of Ole in the prevention and treatment of CRC and may pave the path for more effective and less toxic therapeutic approaches to the prevention and clinical treatment of this tumor and other human neoplasms. This review provides further insight into the molecular mechanisms through which Ole may counteract the growth and progression of CRC and examines the results from emerging studies that underpin the potential clinical role of this molecule in the prevention and treatment of this neoplastic disease.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607669","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}

{"title":"Prognostic Value of Lactate Metabolism-Related Gene Signatures in Cancer Cells.","authors":"Reza Mosaddeghi-Heris, Seyyed Sina Hejazian, Hanie Karimi, Faezeh Ghanbari Sevari, Hamed Rahmani Youshanlouei, Seyed Reza Taha, Mahdieh Shariat Zadeh, Khadijeh Abbasi, Andarz Fazlollahpour Naghibi, Kimia Bagheri, Maryam Farzaneh","doi":"10.2174/0118715206437346260216055104","DOIUrl":"https://doi.org/10.2174/0118715206437346260216055104","url":null,"abstract":"<p><strong>Introduction: </strong>Predicting prognosis in cancer is complex. While traditional staging methods are useful, they do not fully account for the unique biology of each tumor. There is a growing need for biomarkers that capture this biological nuance, which is where molecular signatures like those involved in lactate metabolism (LMRGs) come into play.</p><p><strong>Methods: </strong>We conducted a structured narrative review of existing studies to investigate the link between LMRGs and patient survival. Our analysis spanned a wide array of cancers, from common types like breast and lung cancer to rarer forms such as sarcomas and gliomas, employing relevant keywords associated with lactate metabolism, gene signatures, and cancer prognosis.</p><p><strong>Results: </strong>Our synthesis of the data suggests a consistent trend: higher activity of lactate metabolism genes may be associated with more aggressive disease. Across many different cancers, this signature was reliably associated with worse outcomes for patients, including shorter survival times.</p><p><strong>Discussion: </strong>These findings suggest that LMRGs could be a valuable tool for dividing patients into more precise risk groups, potentially leading to more personalized treatment plans. However, moving this from research to the clinic will require overcoming hurdles like standardizing tests and proving its value in clinical trials.</p><p><strong>Conclusion: </strong>In summary, lactate metabolism genes may hold promise as a broadly applicable warning sign for aggressive cancer. Tapping into this metabolic 'switch' could ultimately help doctors better predict outcomes and tailor treatments for their patients.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607679","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}

{"title":"Phytochemical Insights and Anticancer Potential of Solanum americanum Mill: A Multi-Omics Perspective.","authors":"Pawan Kumar Goswami, Sonakshi Antal, Ranjeet Kumar, Priya Dhiman","doi":"10.2174/0118715206438008260212054456","DOIUrl":"10.2174/0118715206438008260212054456","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;Solanum americanum Mill is a medicinal plant, which is used in the traditional systems of medicine in Ayurveda, African, Pacific Islander, and Native American for treating fever, liver disorders, inflammation, infections, and cancer. Notwithstanding its widespread traditional use and claims, rigorous scientific investigation of its phytochemical constitution and biological activities, including its anticancer potential, is lacking and scattered. In this review, the authors investigate the phytochemical constituents, pharmacological activities, and anticancer mechanisms of S. americanum, particularly focusing on the role of cutting-edge analytical approaches and multi-omics strategies in clarifying its therapeutic activities.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;A thorough literature review of scientific databases was conducted to gather information on the traditional use of the plant, bioactive compounds, and pharmacological studies. Mechanistic studies on apoptosis, oxidative stress, and cell cycle arrest were conducted. High throughput HPTLC, HPLC, LC-MS, GC-MS, and NMR, as well as the Fire-blanket approach of genomics-transcriptomics-proteomics, and the integration of metabolomics data were used to strengthen molecular insights. ` Results: The plant species harbours different phytoconstituents, including steroidal glycoalkaloids such as solamargine and solasonine, flavonoids such as quercetin and kaempferol, and phenolic acids such as chlorogenic acid, which exhibit antioxidant, anti-inflammatory, antimicrobial, and anticancer activities. The anticancer effects are achieved through apoptosis, ROS production, and the Blockade of PI3K/Akt/mTOR and NF-κB pathways. Omics-profiling shows alterations in gene/protein expression and pathways that support the selective cytotoxicity, as well as the potential therapeutic utility of targeting it in cancer cells.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Discussion: &lt;/strong&gt;The results also reflect the multitargeting potential of S. americanum as a therapeutic agent by virtue of its capacity to modulate several signaling pathways associated with cancer. The integration of omics technologies not only facilitates our insight into the molecular mechanisms of UA but also has the potential to support biomarker identification and target-based drug design. Nevertheless, additional preclinical and clinical trials would be required to validate efficacy, bioavailability, and safety. The authors highlight that standardization, pharmacokinetic assessment, and formulation optimization are crucial steps for the successful binging of S. americanum from bench to bedside.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;Solanum americanum Mill. has significant potential as a multi-targeted, plant-derived therapeutic agent in oncology. It is complemented by contemporary omics approaches to provide accurate phytochemical characterization and mechanistic rectification, thereby advocating its progression in personalized medicine and drug ","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607633","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}

{"title":"Research Progress on Desmoid Tumors: New Perspectives from Molecular Mechanisms to Clinical Management.","authors":"Guizhen Lyu, Yuxin Zhang, Dongbing Li","doi":"10.2174/0118715206431105260213034234","DOIUrl":"https://doi.org/10.2174/0118715206431105260213034234","url":null,"abstract":"<p><p>Desmoid Tumors (DT) are rare fibromatoses that are locally invasive. These are described as being monoclonal, and they tend to recur. Their clinical features are also different, and the prognoses of these tumors are not predictable. The recent achievements made in molecular genetics and the encouragement of multidisciplinary treatment modes have made a tremendous contribution to the diagnosis, treatment strategies, and qualityof-life measures of patients with DT. This is a narrative review that summarizes clinical, molecular pathology, conventional, and new areas of treatment, prognosis, and the current research on quality of life assessment tools in DT. It specifically highlights the uses and opportunities of targeted therapies, such as the secretase inhibitor nirogacestat (DeFi trial, NCT03785964) and tyrosine kinase inhibitors, such as sorafenib, reporting substantial disease progression, and critically reviews the role of surgery, in the context of high recurrence rates of marginpositive or even margin-negative resection. The study indicates the significance of personalized treatment that varies treatment options with proper risk-benefit analysis of each patient. This review also explains that the heterogeneous nature of DT and the absence of a standard-of-care predetermine the necessity of such an individual approach. Future areas of research that would offer a more powerful scientific foundation for individual guidance are also mentioned.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607703","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}

{"title":"Anthracycline Drugs: An Update on Chemistry, Structure-Activity Relationship, Mechanism of Action, Cardiotoxicity, Physicochemical and Pharmacokinetic Properties.","authors":"Yaser Pashaei, Necla Kulabaş, Sevil Şenkardeş","doi":"10.2174/0118715206429934251224112953","DOIUrl":"https://doi.org/10.2174/0118715206429934251224112953","url":null,"abstract":"<p><strong>Objective: </strong>This review aims to examine the literature on FDA-approved anthracyclines, focusing on their physicochemical and pharmacokinetic properties, and to analyze relevant studies for insights into chemistry, structure-activity relationships (SAR), mechanisms of action, and cardiotoxicity, to guide safer clinical use and future drug development.</p><p><strong>Methods: </strong>A systematic literature search was conducted across PubMed, Scopus, Web of Science, ScienceDirect, and Google Scholar up to June 2025. Eligible articles included experimental, clinical, and review data on anthracyclines.</p><p><strong>Results: </strong>Anthracyclines act primarily through DNA intercalation, topoisomerase II poisoning, generation of reactive oxygen species, and histone eviction. Key SAR determinants include the aglycone core (C-13, C- 14, and C-4 substituents) and the daunosamine sugar; metabolic conversion to C-13 secondary alcohols and disturbed iron handling are major drivers of chronic cardiotoxicity. Clinically, safe administration relies on cumulative dose limits and cardiac monitoring, while liposomal formulations are validated strategies to reduce toxicity without compromising antitumor efficacy.</p><p><strong>Discussion: </strong>Integrating SAR, physicochemical, and pharmacokinetic insights provides a framework for rationally modifying scaffolds and optimizing delivery systems to expand the therapeutic window. Advances in understanding cardiotoxicity mechanisms support the development of cardioprotective agents, chemical modifications, and clinically validated strategies such as liposomal formulations, while emerging green nanomaterials, combined with nanocarrier-based co-encapsulation strategies, represent a promising, sustainable, and biocompatible approach. This review emphasizes clinically relevant dosing regimens, pharmacokinetic parameters, and cardiotoxicity thresholds, enabling consistent comparisons of FDA-approved anthracyclines.</p><p><strong>Conclusion: </strong>This review clarifies key determinants of anthracycline efficacy and toxicity and recommends actionable strategies, including SAR-guided analogues and validated delivery systems, to advance safer therapies.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147607620","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}

{"title":"Marine-Derived Anticancer Compounds and their Clinical Status.","authors":"Dharmendra Kumar, Kajal Goyal, Pramod Kumar Sharma","doi":"10.2174/0118715206450961260106111347","DOIUrl":"https://doi.org/10.2174/0118715206450961260106111347","url":null,"abstract":"<p><strong>Introduction: </strong>Marine ecosystems provide an abundant reservoir of structurally diverse natural compounds that exhibit distinctive pharmacological activities. In recent decades, many bioactive molecules isolated from marine sources have been recognized as promising anticancer candidates. These agents act through multiple mechanisms, such as suppressing tumor cell proliferation, triggering programmed cell death, and influencing the tumor microenvironment. This review aims to provide a highlight of recent advances (2020-2025) in the discovery, preclinical evaluation, and clinical development of marine-derived compounds for cancer therapy, with emphasis on their structural diversity, biological activity, and clinical trial status.</p><p><strong>Methods: </strong>Relevant literature was systematically searched in PubMed, ScienceDirect, Google Scholar, Scopus, SpringerLink, and https://clinicaltrials.gov/. using keywords \"marine natural products,\" \"anticancer activity,\" \"clinical trials,\" and \"FDA-approved marine drugs.\" Only studies published between 2020 and 2025 were included, and data on cell line activity were extracted.</p><p><strong>Results: </strong>Several promising marine-derived compounds, including alkaloids, peptides, polyketides, and depsipeptides, have shown potent anticancer activity in in-vivo cell line models such as renieramycin M, salinosporamide A, bryostatins, halichondrin B, etc., while many of these compounds have achieved FDA approval, such as trabectedin, eribulin, plitidepsin, and lurbinectedin. While many other marine compounds are currently in clinical trials, they are expected to demonstrate therapeutic effects.</p><p><strong>Discussion: </strong>Marine-derived compounds show significant anticancer potential due to their novel chemical structure and diverse mechanisms of action. Recent research studies have highlighted the efficacy of targeting tumor growth and minimizing the risk of resistance. Future research needs to conduct more clinical trials to support the results and to enable large-scale production of marine-derived compounds.</p><p><strong>Conclusion: </strong>Marine sources offer a wide variety of compounds, and modifying them provides researchers with new opportunities for drug development. Many marine-derived compounds have already shown strong pharmacological effects, with some even proven in clinical use. New studies suggest that marine compounds could also play an important role in anticancer drug delivery systems, making them a promising option for future treatments.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147508832","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}

{"title":"Amlodipine Targeting SPINK1 Attenuates Lung Cancer Cell Growth and Proliferation Through Glycolytic Metabolism.","authors":"Guojun Yue, Lingyun Yue, Yan Chen, Heng Yang, Xi Chen, Yaqian Zhao, Shiyun Xing, Gang Shen, Lei Zhou, Yu Zhang, Yiju Bai","doi":"10.2174/0118715206386163251202104251","DOIUrl":"https://doi.org/10.2174/0118715206386163251202104251","url":null,"abstract":"<p><strong>Introduction: </strong>A trypsin inhibitor, the serine peptidase inhibitor, Kazal type 1 (SPINK1), a secreted protein, has been identified in recent years as contributing to the advancement of specific cancer types. Lung cancer is a common class of malignant tumors. However, the role of SPINK1 in lung cancer is unknown. This study aimed to investigate the profound mechanism of SPINK1 in lung cancer.</p><p><strong>Methods: </strong>In this study, we used bioinformatics methods to select lung cancer samples for single-cell sequencing analysis, including CNV analysis, GSVA analysis, mimetic timing analysis, and intercellular communication, to identify potential molecular targets and pathways. We selected A549 cells and SPC-A1 cells to evaluate the role of SPINK1 in tumorigenesis in vitro.</p><p><strong>Results: </strong>The study indicated that SPINK1 expression was significantly elevated in tumor tissue compared with normal tissue, and higher levels correlated with poorer patient prognosis. Moreover, when SPINK1 was overexpressed, both BEAS-2B and SPC-A1 cells formed dense cell clusters, and SPINK1 overexpression significantly promoted the formation of cell clones.</p><p><strong>Discussion: </strong>Amlodipine (AML) treatment decreases mRNA and protein expression of CDK1, BCL-2, CyclinE1, and CCND1 in A549 and SPC-A1 cells by targeting SPINK1, which regulates glycolytic metabolism.</p><p><strong>Conclusion: </strong>The present study suggests that SPINK1 may modulate glycolytic metabolism in lung cancer cells, inhibiting their growth and proliferation, and potentially providing therapeutic insights.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621425","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}