Anti-cancer agents in medicinal chemistry最新文献

{"title":"Oxygen Free Radicals and Cancer: Protective Role of Endogenous Antioxidants and Natural Compounds.","authors":"Zainab Irfan, Sayed Mohammad Firdous, Sumon Giri, Anam Hashmi","doi":"10.2174/0118715206459486260128064009","DOIUrl":"https://doi.org/10.2174/0118715206459486260128064009","url":null,"abstract":"<p><strong>Introduction: </strong>Reactive oxygen species (ROS) are highly reactive oxygen-derived molecules that function as both potent inducers of cellular damage and essential signalling mediators. In a physiological setting, normal ROS levels control vital functions like immune responses, cell division, and proliferation. However, oxidative stress, which is a major factor in the onset and spread of cancer, is caused by a disturbance in redox equilibrium.</p><p><strong>Methods: </strong>The published literature on ROS, antioxidant defense mechanisms, redox-sensitive signalling pathways, and the anticancer potential of natural substances was summarised and critically assessed in this review. A systematic analysis of peer-reviewed research on molecular mechanisms, signalling cascades, and therapeutic implications was conducted.</p><p><strong>Results: </strong>DNA damage, lipid peroxidation, and protein oxidation are caused by excessive ROS production or impaired antioxidant defenses, which encourage genomic instability and oncogenic transformation. Increased ROS levels impact apoptosis, proliferation, and tumour growth by activating several redox-sensitive pathways such as NF-κB, PI3K/Akt, and MAPK. Both enzymatic and non-enzymatic antioxidants shield cells from oxidative damage, but they can also act as pro-oxidants in certain situations. By altering reactive oxygen levels, suppressing oncogenic signalling, and promoting apoptosis, natural compounds like curcumin, resveratrol, lycopene, and marine-derived metabolites show promising anticancer activity.</p><p><strong>Discussion: </strong>The intricacy of redox control in cancer is highlighted by the dualistic involvement of ROS as tumour promoters and suppressors. Opportunities for redox-based therapeutic interventions are presented by cancer cells, related oxidative stress, and increased reliance on antioxidant systems.</p><p><strong>Conclusion: </strong>A precise understanding of ROS-driven mechanisms can help design targeted redox-based strategies for effective cancer prevention and treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621386","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":"Decoding Sarcoma Drug Resistance: From Molecular Mechanisms to Precision Interventions.","authors":"Guizhen Lyu, Dongbing Li","doi":"10.2174/0118715206435280260122110804","DOIUrl":"https://doi.org/10.2174/0118715206435280260122110804","url":null,"abstract":"<p><strong>Introduction: </strong>This study aims to systematically synthesize current knowledge on the molecular and microenvironmental mechanisms driving sarcoma drug resistance, and to evaluate emerging precision strategies for overcoming these obstacles.</p><p><strong>Methods: </strong>We conducted a comprehensive literature review (PubMed, Web of Science, Embase; inception- 31 July 2025) using MeSH and free-text terms relating to sarcoma, drug resistance, biomarkers, and precision medicine. Inclusion criteria were peer-reviewed original or review studies in human or pre-clinical sarcoma models reporting resistance mechanisms or counter-strategies. Data were qualitatively categorized by resistance pathways (efflux pumps, DNA repair, apoptosis inhibition, secondary mutations, and immune evasion) and linked to therapeutic countermeasures.</p><p><strong>Results: </strong>ABC transporter over-expression (especially P-gp) and heightened DNA repair via homologous recombination were recurrent chemo-resistance drivers. Targeted-therapy failure was dominated by secondary KIT/PDGFRA or NTRK mutations, bypass signaling (PI3K/AKT ↔ RAS/MAPK), and epithelial- mesenchymal transition. Immune escape occurred through antigen loss, MHC-I down-regulation, adenosine- rich immunosuppressive microenvironments, and T-cell exhaustion (PD-1/CTLA-4 up-regulation). Epigenetic dysregulation (EZH2, HDAC, DNMT) further fostered stem-like survival. Liquid-biopsy ctDNA enabled real-time resistance monitoring. Next-generation TKIs, dual-pathway inhibitors, epigenetic drugs, and rationally designed chemo-immuno combinations showed synergistic activity in pre-clinical and early clinical studies.</p><p><strong>Discussion: </strong>Integrating multi-omics profiling, liquid biopsies, and patient-derived organoids into adaptive trial designs can individualize therapy sequences and delay resistance. Limitations include heterogeneous sarcoma biology, limited clinical validation, and economic barriers to the implementation of precision.</p><p><strong>Conclusion: </strong>Resistance to drugs in sarcoma is multifactorial and changeable. Nevertheless, fusing mechanistic knowledge with biomarker - guided combination/sequential therapies offers a clear way to improve patient situations.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621380","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":"Glycyrrhetinic Acid in Cancer Therapy: Mechanistic Insights, Therapeutic Potential, and Future Directions.","authors":"Nilufar Yoqubova, Shokhid Gulyamov, Doniyorbek Abdulla-Zoda, Khurshid Tursunov, Avez Sharipov, Kamal Rizaev, Xuebo Hu","doi":"10.2174/0118715206440313260127193145","DOIUrl":"https://doi.org/10.2174/0118715206440313260127193145","url":null,"abstract":"<p><p>Cancer presents a significant and growing global health challenge in the 21st century, marked by a rising number of new diagnoses and cancer-related deaths reported annually. Glycyrrhetinic Acid (GA), a triterpenoid compound derived from the licorice plant, Glycyrrhiza glabra, G. inflata, and G. uralensis, has a long-standing history of use in traditional healing practices. In this comprehensive review, the evolving research on GA's pharmacological properties published between 2015 and 2024, with a specific focus on its potential as a cancer therapy, is critically analyzed. In preclinical studies, GA showed anti-tumor effects and modulated several cellular pathways involved in cancer growth. Despite this promising anti-tumor activity, GA's clinical use is still being evaluated because of poor solubility and low bioavailability. A clear understanding of GA's complex pharmacokinetics is necessary to optimize its clinical application. This work explores how GA may act against cancer, including its capacity to enhance chemotherapeutic treatments and its interactions in the tumor microenvironment. In addition, this paper critically reviews GA's therapeutic potential across different cancer types and discusses new formulation approaches, pointing to key directions for future clinical and translational studies. This review summarizes the existing evidence on GA and discusses its potential use as a treatment in oncology. Further research is needed to assess GA's effectiveness and safety in clinical studies. Such investigations can help translate laboratory results into practical use in clinical settings.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621405","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":"MVs and MVs-Crocin as Novel Therapeutic Agents for Lung Cancer, Apoptosis, and Gene Regulation.","authors":"Hosein Keshavaerz, Bita Zand, Leila Sadat Nilchiani, Raheleh Halabian, Farideh Heshmati","doi":"10.2174/0118715206444442260125215301","DOIUrl":"https://doi.org/10.2174/0118715206444442260125215301","url":null,"abstract":"<p><strong>Introduction: </strong>Lung cancer is one of the most common malignancies worldwide. Stem cells and their secretions have recently attracted attention as potential therapeutic agents due to their anti-cancer properties. This study investigated the effects of mesenchymal stem cell-derived microvesicles (MVs) and Crocinpreconditioned MVs (MVs-Crocin) on lung cancer cells (A549) compared with normal cells (HEK293).</p><p><strong>Materials and methods: </strong>Mesenchymal stem cells were preconditioned with Crocin, and microvesicles were subsequently isolated. The appropriate therapeutic concentrations of MVs and MVs-Crocin were determined using the MTT assay. A549 and HEK293 cells were treated with the optimized doses. Apoptosis was assessed by flow cytometry, and the expression of apoptotic genes was analyzed through real-time PCR.</p><p><strong>Results: </strong>MTT assay results identified 40 μg/ml for MVs and 50 μg/ml for MVs-Crocin as optimal therapeutic concentrations. Treatment with MVs and MVs-Crocin significantly reduced the survival of A549 cells, while apoptosis assays and gene expression analysis confirmed enhanced apoptotic activity in treated cancer cells.</p><p><strong>Discussion: </strong>Both MVs and MVs-Crocin demonstrated potent anti-cancer effects by reducing lung cancer cell survival and inducing apoptosis. Preconditioning with Crocin appeared to further strengthen the therapeutic efficacy of MVs. Importantly, these effects were more pronounced in cancer cells compared to normal cells, indicating selective anti-cancer potential.</p><p><strong>Conclusion: </strong>MVs and MVs-Crocin promote apoptosis in lung cancer cells and may serve as promising candidates for the development of novel therapeutic strategies against lung cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621458","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":"Ginkgolide A Suppresses Osteosarcoma Proliferation and Activates the Apoptotic Pathway by Targeting the KAT2A-H3K18la Lactylation Axis.","authors":"Chunfeng Fu, Jiaqin Wu, Shuwan Hou, Minfu Liu, Shunshun Wang, Qianqian Du, Huiming Yu, Sixiang Wang, Fan Feng, Kang Xu, Chunli Wang, Muhammad Farrukh Nisar","doi":"10.2174/0118715206443791260209074742","DOIUrl":"https://doi.org/10.2174/0118715206443791260209074742","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;Osteosarcoma (OS) is a highly aggressive primary bone malignancy characterized by profound metabolic reprogramming and limited therapeutic options. Although histone lactylation has recently emerged as a metabolic-epigenetic mechanism linking glycolysis to gene regulation, its functional relevance and therapeutic tractability in OS remain largely unexplored. Here, we identify the natural diterpene lactone Ginkgolide A (GA) as a potent suppressor of OS progression through targeted disruption of lactate-driven histone lactylation.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Human Osteosarcoma (OS) MG63 and U2OS cell lines were given GA to find cell viability loss, migration, and apoptosis, which were examined using CCK-8 assay, wound-healing assay, Annexin V/PI flow cytometry, TUNEL staining, qRT-PCR, and immunoblotting. Gas Chromatography Mass Spectrometry (GC-MS) metabolomics was employed to profile the metabolic changes induced by GA, with a focus on the glycolytic pathway. In-depth ligation patterns and regulatory mechanisms of histone were studied herein through sitespecific immunoblotting, Chromatin Immunoprecipitation (ChIP)-qPCR, immunofluorescence, and Molecular Docking (MD) tools. Later on, the antitumor potential of GA was further examined using a nude mouse xenograft model.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;GA significantly checked OS cell proliferation and migration by modulating apoptosis, with halfmaximal inhibitory concentrations of 10.83 μM (MG63 cells) and 12.88 μM (U2OS cells). GA boosts mitochondrial apoptosis, indicated by enhanced BAX and caspase-3/-9 levels while repressing the expression level of BCL-2. Integrated metabolomic profiling indicated a marked decline of intracellular lactate and acetate levels, which establishes a metabolic basis for downstream epigenetic remodeling by GA. GA showed a site-specific epigenetic regulation by targeted suppression of histone H3 lysine-18 lactylation (H3K18la) with no effect on non-target lactylation sites. GA may downregulate expression of lactyltransferase KAT2A, alter H3K18laassociated promoter occupancy of apoptosis-linked genes, and induce pro-apoptotic transcriptional activity. In the xenograft in vivo model, GA modulated apoptosis to significantly inhibit tumor growth and expression of Ki67.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Discussion: &lt;/strong&gt;Findings reported in the present study confirmed that GA directly interacts with KAT2A, inhibits lactylation by disrupting the binding of KAT2A with H3K18, thereby regulating OS cell proliferation.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;GA markedly inhibits proliferation, migration, and induces apoptosis in OS cells primarily by regulating the glycolytic pathway, i.e., reduction in lactate levels, subsequent targeting of KAT2A, downregulation of H3K18 lactylation, and ultimate transcriptional regulation of apoptosis. It is hereby recognized that GA mediates metabolic inhibition by selective epigenetic reprogramming of the KAT2A-H3K18 lactyla","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621417","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":"Chitosan-Gold Nanogel Loaded with Doxorubicin: An Enhanced Delivery System for NSCLC Lung Cancer.","authors":"Elham Aminirad, Tala Haghnazari Esfahlan, Ali Rajabi, Marziyeh Fathi, Ali Saber, Mohammad Ali Hosseinpour Feizi, Reza Safaralizadeh","doi":"10.2174/0118715206437499260128114402","DOIUrl":"https://doi.org/10.2174/0118715206437499260128114402","url":null,"abstract":"<p><strong>Introduction: </strong>Lung Cancer (LC) is the leading cause of cancer deaths globally. Long non-coding RNAs (lncRNAs) have emerged as important regulators in lung cancer, playing key roles in tumor development and metastasis. Recent advances in nanoparticle-based drug delivery systems and lncRNA research offer promising strategies to enhance treatment efficacy and reduce adverse effects.</p><p><strong>Methods: </strong>CS/AuNPs were synthesized via chloroauric acid reduction in chitosan solution, and DOX was incorporated using TPP crosslinking to form CS/AuNP-DOX. The nanoparticles were characterized by FT-IR spectroscopy, particle size, and zeta potential analysis. The in vitro effects of CS/AuNP-DOX on cytotoxicity (IC50), apoptosis, cell cycle, and lncRNA expression were evaluated.</p><p><strong>Results: </strong>CS/AuNP-DOX demonstrated enhanced anticancer activity compared to free DOX, with reduced IC₂⁽ (1.36 μM vs. 1.9 μM), increased apoptosis (57% vs. 37%), and greater G2/M phase cell cycle arrest. Importantly, CS/AuNP-DOX induced only limited apoptotic and cell-cycle effects in normal cells (HFFF2). Additionally, treatment with CS/AuNP-DOX significantly downregulated the expression of HIF1A-AS1 and DLGAP1-AS2.</p><p><strong>Discussion: </strong>The enhanced therapeutic efficacy and reduced toxicity observed in this study suggest that CS/AuNP-DOX may overcome limitations of conventional chemotherapy by improving drug bioavailability.</p><p><strong>Conclusions: </strong>These findings highlight the potential of integrating nanoparticle-based drug delivery with lncRNA-targeted therapies to improve lung cancer treatment. However, further in vivo studies are required to confirm these results.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621367","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":"A Preliminary Study on Photodynamic Therapy for Central Tracheobronchial Malignant Tumours.","authors":"Beilei Gong, Yongyan Zhang, Ting Wang, Qian Zhang, Yuanbing Shen, Wei Li","doi":"10.2174/0118715206411779251202224306","DOIUrl":"https://doi.org/10.2174/0118715206411779251202224306","url":null,"abstract":"<p><strong>Introduction: </strong>Photodynamic therapy (PDT) holds considerable potential in inoperable central tracheobronchial malignant tumours. However, evidence is scarce from Chinese populations. This preliminary study was conducted to monitor the therapeutic efficacy and assess the safety of PDT for central tracheobronchial malignant tumours in a Chinese population.</p><p><strong>Methods: </strong>This study involved nine patients with central tracheobronchial malignant tumours who underwent PDT. The primary endpoints of the study were clinical efficacy and safety, while secondary endpoints included the one-year overall survival (OS), two-year OS, and recurrence-free survival (RFS).</p><p><strong>Results: </strong>Nine patients with a follow-up period exceeding two years, six patients exhibited sustained clinical stability for one year. After PDT, there was a significant improvement in both the clinical symptoms and the quality of life of the patients (t = 5.57, P<0.0001). The one-year OS reached 88.9%, while the two-year OS was 77.8%. Among the included patients, two patients with adenoid cystic carcinoma had not yet reached the average RFS, with a mean RFS of 15.9±10.5 months (ranging from 2.1 to 35.0 months). Adverse effects were limited, with two patients experiencing grade 1 photosensitivity reactions, one patient developing localized bronchial scarring. Importantly, no serious treatment-related complications were observed.</p><p><strong>Discussion: </strong>This study demonstrates that PDT is associated with a favorable safety profile and significant therapeutic benefits, particularly when combined with multimodal comprehensive treatment strategies. While the small sample size and single-center design limit the generalizability of our findings, the data presented here provide important insights into the application of PDT for central airway malignancies in China. Future research should aim to include a larger, more diverse patient population to further validate the efficacy of PDT and explore its potential as a new treatment option for patients.</p><p><strong>Conclusions: </strong>This preliminary study establishes that PDT represents a viable and effective approach for the management of central tracheobronchial malignant tumours. PDT yields favourable survival outcomes while being associated with mild and well-tolerated complications. Overall, this study highlights the significant clinical value of PDT.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621430","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":"Decoding the Anticancer Potential of Natural N-Heterocycles: Molecular Frameworks, Bioactivity, and Mechanistic Advances.","authors":"Honey Saini, Anuradha Mehra, Amit Mittal","doi":"10.2174/0118715206435258260119060605","DOIUrl":"https://doi.org/10.2174/0118715206435258260119060605","url":null,"abstract":"<p><p>Cancer is the leading cause of death and morbidity worldwide. Numerous scientists are trying to develop new anticancer medications that are more potent and less hazardous. This review, in contrast to previous reviews, focuses on the latest research findings from 2020-2025 on N-heterocyclic moieties as natural anticancer agents. This review provides a contemporary evaluation that integrates recent mechanistic discoveries, emerging nanotechnology-based delivery approaches, and translational progress relevant to natural Nheterocyclic anticancer agents. The literature was collected from online sources such as PubMed, Science Direct, Embase, and Google Scholar by searching with keywords like research paper on Natural N-heterocyclic products having anticancer activity, etc. The findings suggest that combining naturally obtained N-heterocyclic compounds with nanotechnology can provide us with a low-toxic anticancer drug in the future. The process of combining natural products containing N-Heterocyclic moieties with nanotechnology can be a game-changer for the development of anticancer medications. Still, there is a lot of research to be done in this area, which can change the viewpoint of the world regarding the treatment of cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147621391","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":"Targeting XBP1 in Cancer: A Review of Therapeutic Approaches and Strategies.","authors":"Abdolah Mousavi Salehi, Ali Khavanin, Shirin Azizidoost, Maryam Cheraghzadeh, Maryam Khombi Shooshtari, Maryam Farzaneh, Mahrokh Abouali Gale Dari","doi":"10.2174/0118715206401777251126092808","DOIUrl":"https://doi.org/10.2174/0118715206401777251126092808","url":null,"abstract":"<p><p>X-box binding protein 1 (XBP1) is an essential unfolded protein response (UPR) transcription factor that has important roles in cancer biology. Malignant XBP1 signaling promotes tumor survival, drug resistance, and immune evasion and thus represents a potential therapeutic target and biomarker. A structured literature search was conducted using PubMed, Embase, Springer, Elsevier, ISI Web of Knowledge, and Google Scholar. The studies that had investigated the expression, role, and therapeutic targeting of XBP1 in various cancers were identified and critically assessed. XBP1 overexpression is associated with aggressive phenotypes, metastasis, and drug resistance to chemotherapy, radiotherapy, and endocrine therapy in many cancers, including breast, colorectal, lung, ovarian, liver, prostate, and hematopoietic cancers. Aside from intrinsic tumor activities, XBP1 also modulates the tumor microenvironment by suppressing dendritic cell function, promoting T-cell exhaustion, and reprogramming. Preclinical data support that inhibiting the IRE1α-XBP1 pathway restores treatment sensitivity and shows synergy with immunotherapy. XBP1 is a molecular interface for ER stress adaptation, oncogenic progression, and immune modulation. The fact that XBP1 is both a prognostic biomarker and a therapeutic target underscores the translational potential of XBP1-targeted therapy to improve the outcome of cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147462565","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":"Medicinal Chemistry of Natural Anti-Skin Cancer Agents: An Evidence-Based Literature Review.","authors":"Mirna Al-Hasan, Abdullah Al Lawati, Maather Al Shuhaibi, Jumana Al Subeihi, Taif Al Hinai, Qusay Al Badi, Hanan Al Lawati, Srinivasa Rao Sirasanagandla, Srijit Das","doi":"10.2174/0118715206383549251208065934","DOIUrl":"https://doi.org/10.2174/0118715206383549251208065934","url":null,"abstract":"<p><p>Globally, the incidence and prevalence of skin cancer have increased. Skin cancers involve an abnormal growth of cells. Skin cancers are classified into melanoma and nonmelanoma skin cancer (NMSC), and NMSC is further classified as squamous cell carcinoma (SCC) and basal cell carcinoma (BCC). In the present narrative review, we searched databases, such as PubMed, Scopus, and Google Scholar, to retrieve the relevant articles. The ideal selection of therapeutic options depends on the anatomical location, genetic composition, different tumor stages, the individual's age, and general health conditions. Various chemotherapeutic options are available for effective treatment, but there are various side effects of the drugs. Natural products (NPs) may be used as supplements. NPs can potentiate apoptosis, decrease cell growth, and prevent metastasis. They are also safe and effective. The present review summarizes the use of natural products, such as Aloe vera, eggplant, frankincense, milk thistle, turmeric, black raspberry, mistletoe, burdock root, Dong Quai, black salve, astragalus, Solanum sodomaeum, Calendula officinalis, Melaleuca alternifolia, Hypericum perforatum, Withania somnifera, Polypodium leucotomos, Rosmarinus officinalis, Alpinia galangal, hypericin, tea, coffee, genistein, grape seed, and silymarin. Larger clinical trials are needed to explore the safety profile of various natural products that have proven effective against skin cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147462562","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}