Bioorganic Chemistry最新文献_第3页

Beyond peptides: Unveiling the design strategies, structure activity correlations and protein-ligand interactions of small molecule inhibitors against PD-1/PD-L1.

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-06 DOI: 10.1016/j.bioorg.2024.108036

Pujan Sasmal, P Prabitha, B R Prashantha Kumar, B R Swetha, Sajeev Kumar Babasahib, Nulgumnalli Manjunathaiah Raghavendra

{"title":"Beyond peptides: Unveiling the design strategies, structure activity correlations and protein-ligand interactions of small molecule inhibitors against PD-1/PD-L1.","authors":"Pujan Sasmal, P Prabitha, B R Prashantha Kumar, B R Swetha, Sajeev Kumar Babasahib, Nulgumnalli Manjunathaiah Raghavendra","doi":"10.1016/j.bioorg.2024.108036","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108036","url":null,"abstract":"The landscape of cancer treatment has been transformed by the emergence of immunotherapy, especially through the use of antibodies that target the PD-1/PD-L1 pathway. Recently, there has been a notable increase in interest surrounding immune checkpoint inhibitors for cancer therapy. While antibody-based approaches have drawbacks like high costs and prolonged activity, the approval of monoclonal antibodies such as pembrolizumab and nivolumab has paved the way for a range of alternative therapies, including peptides, peptidomimetics, and small-molecule inhibitors. These smaller molecules, which target the PD-1/PD-L1 interaction, are seen as potential substitutes or supplements to monoclonal antibodies. Our focus in this article is primarily on exploring small molecules designed for PD-1/PD-L1 checkpoint pathway modulation in cancer immunotherapy, along with highlighting current advances in their structural and preclinical/clinical development. The pursuit of therapeutics based on small-molecule inhibitors of the PD-1/PD-L1 axis offers a promising yet intricate avenue for advancing cancer treatment.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108036"},"PeriodicalIF":4.5,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142851750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Damsin and neoambrosin: Two sesquiterpene lactones with affinity and different activity for PPAR and TRPA1 receptors. Damsin 和 neoambrosin：对 PPAR 和 TRPA1 受体具有亲和力和不同活性的两种倍半萜内酯。

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-06 DOI: 10.1016/j.bioorg.2024.108032

Shymaa I A Abdel-Dayem, Asmaa M Otify, Fabio Arturo Iannotti, Fatema R Saber, Aniello Schiano Moriello, Simone Giovannuzzi, Łukasz Świątek, Alessandro Bonardi, Paola Gratteri, Krystyna Skalicka-Woźniak, Claudiu T Supuran

{"title":"Damsin and neoambrosin: Two sesquiterpene lactones with affinity and different activity for PPAR and TRPA1 receptors.","authors":"Shymaa I A Abdel-Dayem, Asmaa M Otify, Fabio Arturo Iannotti, Fatema R Saber, Aniello Schiano Moriello, Simone Giovannuzzi, Łukasz Świątek, Alessandro Bonardi, Paola Gratteri, Krystyna Skalicka-Woźniak, Claudiu T Supuran","doi":"10.1016/j.bioorg.2024.108032","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108032","url":null,"abstract":"Ambrosia maritima L. (family Asteraceae) is an annual herb widely distributed throughout the Mediterranean region and Africa. The herb is employed in folk medicine for the treatment of many ailments. Herein, we report a comprehensive investigation of the diverse biological potential of two sesquiterpene lactones, damsin and neoambrosin, isolated from Ambrosia maritima. 1D and 2D NMR and HR-ESI-MS/MS were employed to characterize the chemical structures of both compounds. In order to identify biological targets of both compounds we investigated their potential affinity for peroxisome proliferator-activated receptors (PPARs) and transient receptor potential (TRP) channels, which are pleiotropic classes of receptors implicated in essential functions of the body. This was investigated using a luciferase assay and a calcium fluorometric assay. A carbonic anhydrase inhibition assay was also performed using stopped flow CO2 hydrase spectrophotometric assay. Our analysis revealed that unlike damsin, neoambrosin showed a selective partial agonist effect on PPARγ receptors and TRPA1 channels. Its binding mode was investigated through in silico analysis. Both compounds showed no affinity for the tested carbonic anhydrases. Overall, our study details the chemical properties of neoambrosin and damsin and highlights neoambrosin as novel, cost-effective partial agonist of PPARɣ and TRPA1 receptors despite additional in vivo studies are needed to elucidate its biological and pharmacological properties.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108032"},"PeriodicalIF":4.5,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142821539","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Design, synthesis, and biological evaluation of novel 3-naphthylthiophene derivatives as potent SIRT2 inhibitors for the treatment of myocardial fibrosis. 新型 3-萘基噻吩衍生物作为强效 SIRT2 抑制剂用于治疗心肌纤维化的设计、合成和生物学评价。

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-06 DOI: 10.1016/j.bioorg.2024.108033

Zhuo Zhang, Chao Ma, Xiong Gao, Chuncheng Wang, Yanchun Li, Chen Yang, Enlong Ma, Maosheng Cheng

{"title":"Design, synthesis, and biological evaluation of novel 3-naphthylthiophene derivatives as potent SIRT2 inhibitors for the treatment of myocardial fibrosis.","authors":"Zhuo Zhang, Chao Ma, Xiong Gao, Chuncheng Wang, Yanchun Li, Chen Yang, Enlong Ma, Maosheng Cheng","doi":"10.1016/j.bioorg.2024.108033","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108033","url":null,"abstract":"SIRT2 (sirtuin2) is a NAD+-dependent deacetylase implicated in fibrosis and inflammation of the liver, kidney, and heart. In this study, we designed and synthesized a series of 3-naphthylthiophene derivatives and evaluated their inhibitory activity against the SIRT2 enzyme. Among them, Z18 demonstrated outstanding SIRT2 inhibitory activity and selectivity. It significantly inhibited both the proliferation of cardiac fibroblasts (CFs) and the activity and expression of SIRT2 in CFs. Moreover, compound Z18 effectively suppressed TGF-β1-induced increases in α-SMA and CoL-1A1 protein expression, as well as hydroxyproline levels. Pharmacological mechanism tests demonstrated that Z18 inhibited SIRT2, thereby suppressing the TGF-β1-induced autocrine production of TGF-β1 and the phosphorylation of Smad2/3 in CFs. In MTT assays, Z18 exhibited a significant inhibitory effect on the proliferation of CFs induced by TGF-β1. In vivo, Z18 effectively ameliorated TAC- and ISO-induced declines in cardiac function, histopathological morphological changes, and collagen deposition. It also inhibited SIRT2 activity and reduced the expression of α-SMA and p-Smad2/3. In hepatorenal toxicity assays, Z18 exhibited an excellent safety profile. These results support the further development of the selective SIRT2 inhibitor Z18 as a potential lead compound for the treatment of myocardial fibrosis.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108033"},"PeriodicalIF":4.5,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142821540","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Epidermal growth factor receptor mutations in breast Cancer: Therapeutic challenges and way forward. 乳腺癌中的表皮生长因子受体突变：治疗挑战与前进之路。

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-06 DOI: 10.1016/j.bioorg.2024.108037

Swathi R Shetty, Trisha Kar, Amitava Das

{"title":"Epidermal growth factor receptor mutations in breast Cancer: Therapeutic challenges and way forward.","authors":"Swathi R Shetty, Trisha Kar, Amitava Das","doi":"10.1016/j.bioorg.2024.108037","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108037","url":null,"abstract":"Epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase (RTK) that is upregulated in aggressive triple-negative breast cancer (TNBC). Ligands such as EGF, TGF-α, epigen, and amphiregulin activate the auto-phosphorylation activity of tyrosine residues on EGFR, which regulates the growth, proliferation, adhesion, migration, and survival of cancer cells. Our prior studies depicted that inhibition of EGFR modulates the chemosensitivity in breast cancer stem cells and, thus, serves as a potent therapeutic target in breast cancer. Small-molecule tyrosine kinase inhibitors (TKIs) and monoclonal antibodies (mAbs) specifically targeting EGFR have been clinically approved for breast cancer treatment. However, intrinsic and acquired resistance generated due to EGFR mutations limits the applications of designed EGFR-TKIs in breast cancer patients. This review highlights the therapeutic approaches, and the challenges encountered in targeting EGFR-specific mutations. It suggests the need to develop more advanced higher-generation inhibitors for use in combinatorial therapy along with chemo-or-immune therapeutics in clinics as a breast cancer treatment strategy against relapse of the disease.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108037"},"PeriodicalIF":4.5,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142821542","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Novel dual-channel ratiometric fluorescence probe for SO₂ detection in food and bioimaging applications based on FRET mechanism. 基于 FRET 机制用于食品和生物成像应用中二氧化硫检测的新型双通道比率荧光探针。

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-06 DOI: 10.1016/j.bioorg.2024.108034

Shufei Li, Huiquan Xiao, Jiaxin Hong, Xinyu Xia, Luying Duan, Wuying Yang, Xiaoli Yin, Yunhua Zeng, Yanping Hong

{"title":"Novel dual-channel ratiometric fluorescence probe for SO2 detection in food and bioimaging applications based on FRET mechanism.","authors":"Shufei Li, Huiquan Xiao, Jiaxin Hong, Xinyu Xia, Luying Duan, Wuying Yang, Xiaoli Yin, Yunhua Zeng, Yanping Hong","doi":"10.1016/j.bioorg.2024.108034","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108034","url":null,"abstract":"SO2 is commonly used to ensure the safety of food, but englobing of excessive SO2 poses serious risks to human health. Additionally, as fourth gaseous signaling molecule, it plays a critical role in various physiological processes. Therefore, monitoring the concentration of SO2 in food and cells is crucial for correlative research and disease diagnosis. Herein, two ratiometric fluorescence probes (EHDA and EHDB) have been synthesized for detecting sulfite based on fluorescence resonance energy transfer (FRET). Undoubtedly, EHDA as the preferable probe due to its superior discernibility to SO32- than that of EHDB. Moreover, EHDA featured rapid response, high sensitivity, excellent selectivity, and low cytotoxicity in physiological pH. Besides, EHDA could be expanded to establish convenient smartphone SO2 sensing platform through innovatively loading EHDA on polyvinylidene fluoride membrane. Fortunately, EHDA has been utilized for determining SO32- in food samples and imaging the fluctuation of sulfite in living cells and zebrafish.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108034"},"PeriodicalIF":4.5,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142821543","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Coccinic acid exhibits anti-tumor efficacy against NSCLC harboring EGFR L858R/T790M mutation via the EGFR/STAT3 pathway.

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-06 DOI: 10.1016/j.bioorg.2024.108038

Peiyuan Sun, Shuanggou Zhang, Yana Qu, Xuanyou Li, Guirui Chen, Xuanjun Wang, Jun Sheng, Jing Wang

{"title":"Coccinic acid exhibits anti-tumor efficacy against NSCLC harboring EGFR L858R/T790M mutation via the EGFR/STAT3 pathway.","authors":"Peiyuan Sun, Shuanggou Zhang, Yana Qu, Xuanyou Li, Guirui Chen, Xuanjun Wang, Jun Sheng, Jing Wang","doi":"10.1016/j.bioorg.2024.108038","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108038","url":null,"abstract":"Epidermal growth factor receptor (EGFR) is a starring target for the treatment of non-small cell lung cancer (NSCLC). EGFR tyrosine kinase inhibitors (EGFR-TKIs) have been used to treat NSCLC patients with EGFR-activating mutations. However, most patients invariably develop resistance to these agents due to the occurrence of novel mutations at the EGFR kinase domain. There is an urgent need to develop more effective therapy strategies to provide more selection for patients with NSCLC. Coccinic acid was reported to exerts potential anti-tumor effects, but its mechanism has not been elucidated and warrants investigation. In this study, coccinic acid was shown to inhibit cell proliferation on cells harboring L858R/T790M mutant EGFR by suppressing p-EGFR and p-STAT3. It was also shown that coccinic acid promoted cell cycle distribution and showed a potent apoptosis-inducing efficacy. Further results in vivo assays demonstrated that coccinic acid reduced tumor growth of NCI-H1975 xenograft in nude mice via the EGFR/STAT3 signaling. Moreover, these effects are involving in the binding of coccinic acid to the EGFR extracellular domain. In conclusion, our finding demonstrated that coccinic acid may be utilized as a potential novel candidate for NSCLC with EGFR L858R/T790M mutation.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108038"},"PeriodicalIF":4.5,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142794109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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 novel tetrazole-based pyruvate kinase M2 inhibitors targeting U87MG glioblastoma cells.

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-05 DOI: 10.1016/j.bioorg.2024.108029

Moumita Ghosh Chowdhury, Saumya Kapoor, Venkatesh Muthukumar, Deep Rohan Chatterjee, Amit Shard

{"title":"Development of novel tetrazole-based pyruvate kinase M2 inhibitors targeting U87MG glioblastoma cells.","authors":"Moumita Ghosh Chowdhury, Saumya Kapoor, Venkatesh Muthukumar, Deep Rohan Chatterjee, Amit Shard","doi":"10.1016/j.bioorg.2024.108029","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108029","url":null,"abstract":"Glioblastoma (GB), the most aggressive and life-threatening primary brain tumor in adults, poses significant therapeutic challenges. Tumor pyruvate kinase M2 (PKM2) has been implicated in the proliferation and survival of glioma cells. In this study, we designed and synthesized a series of 23 novel tetrazole-based derivatives. The compounds were thoroughly characterized using 1H, 13C, 19F NMR, along with HRMS analysis. Among them, 1-(imidazo[1,2-a]pyrimidin-3-yl)-2-(5-(naphthalen-2-yl)-2H-tetrazol-2-yl)ethan-1-one (9b) exhibited potent and selective antiproliferative activity against U87MG glioma cells, with minimal effects on bEnd (brain endothelial cell line) non-glioma cells. It emerged as a potent PKM2 inhibitor, with an IC50 of 0.307 µM. Apoptosis assays and cell cycle analysis revealed that compound 9b induced early apoptosis and caused G1 phase arrest. A significant decrease in pyruvate concentration further suggested PKM2 inhibition. In silico studies confirmed the binding affinity to the PKM2 inhibitory site, and RT-PCR data demonstrated its inhibitory activity against PKM2. Additionally, it reduced lactate levels, indicating its potential impact on cellular metabolism. Collectively, these findings suggest that the most potent compound holds promise as a therapeutic candidate against GB.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108029"},"PeriodicalIF":4.5,"publicationDate":"2024-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142851778","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

Novel aryl (dithioglycosyl)methane derivatives as anti-proliferative agents.

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-05 DOI: 10.1016/j.bioorg.2024.108030

Abhijit Rana, Satyajit Halder, Rittika Chakraborty, Utsab Debnath, Kuladip Jana, Anup Kumar Misra

引用次数: 0

Design, synthesis, biological evaluations and in silico studies of (Z)-2-(2,4-dioxothiazolidin-5-ylidene)methyl)-2-ethoxyphenyl-alkyl/arylsulfonates as potential α-glucosidase inhibitors.

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-04 DOI: 10.1016/j.bioorg.2024.108027

Lalita Dahiya, Jatin Jangra, Sunil Kumar, Rajiv Kumar, Rajnish Kumar, Sandip V Pawar, Ashok Kumar Yadav

{"title":"Design, synthesis, biological evaluations and in silico studies of (Z)-2-(2,4-dioxothiazolidin-5-ylidene)methyl)-2-ethoxyphenyl-alkyl/arylsulfonates as potential α-glucosidase inhibitors.","authors":"Lalita Dahiya, Jatin Jangra, Sunil Kumar, Rajiv Kumar, Rajnish Kumar, Sandip V Pawar, Ashok Kumar Yadav","doi":"10.1016/j.bioorg.2024.108027","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108027","url":null,"abstract":"Diabetes mellitus is considered one of the major worldwide health emergencies of the twenty-first century. This work described development, synthesis, and characterization of new (Z)-2-(2,4-dioxothiazolidin-5-ylidene)methyl)-2-ethoxyphenyl-alkyl/aryl-sulfonates. Compounds 7j and 7m were shown to be the most potent among the newly developed (Z)-2-(2,4-dioxothiazolidin-5-ylidene)methyl)-2-ethoxyphenyl-alkyl/aryl-sulfonates after in vitro testing for α-glucosidase inhibitory activity. Following that, an in-vivo disaccharide loading test was performed on these compounds. From the cytotoxicity studies, the most potent substance (7m) was also founded non-toxic. To investigate the binding mechanism and important interactions of α-glucosidase's amino acid residues, docking analyses were completed and binding affinities of the synthesised compounds were observed from -7.1 to 9.6 kcal/mol. To determine the binding stability of the α-glucosidase protein with chemicals 7j and 7m, molecular dynamic simulations were employed. In silico research and prediction studies for absorption, distribution, metabolism, and excretion (ADME) were used to identify the \"druggable\" pharmacokinetic profiles. In this instance, we developed unique (Z)-2-(2,4-dioxothiazolidin-5-ylidene)methyl)-2-ethoxyphenyl-alkyl/aryl-sulfonates as α-glucosidase inhibitors.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108027"},"PeriodicalIF":4.5,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142805577","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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

An overview of phenylsulfonylfuroxan-based nitric oxide donors for cancer treatment.

IF 4.5 2区医学

Bioorganic Chemistry Pub Date : 2024-12-04 DOI: 10.1016/j.bioorg.2024.108020

Chao Gao, Xingyu Li, Tong Liu, Wanning Wang, Jianhui Wu

{"title":"An overview of phenylsulfonylfuroxan-based nitric oxide donors for cancer treatment.","authors":"Chao Gao, Xingyu Li, Tong Liu, Wanning Wang, Jianhui Wu","doi":"10.1016/j.bioorg.2024.108020","DOIUrl":"https://doi.org/10.1016/j.bioorg.2024.108020","url":null,"abstract":"Nitric oxide (NO) is a gaseous molecule integral to numerous physiological processes, including tumor modulation, cardiovascular regulation, and systemic physiological functions. Its dual role in promoting and inhibiting tumor growth makes it a focal point of contemporary oncological research. Phenylsulfonylfuroxan, a classical NO donor, has been shown to significantly elevate NO levels, thereby inducing apoptosis and inhibiting proliferation and metastasis in tumor cells. It enhances the efficacy of chemotherapy, radiotherapy, and immunotherapy, reverses multidrug resistance (MDR), and impedes tumor progression. Notably, phenylsulfonylfuroxan have the ability to trigger ferroptosis in cancer cells by binding covalently to inhibit glutathione peroxidase 4 (GPX4). Recent developments in phenylsulfonylfuroxan-based therapies have positioned them as crucial in the advancement of cancer treatment modalities. This review elucidates the mechanism by which phenylsulfonylfuroxan releases NO and summarizes the significant advancements over the past 16 years in the research and development of phenylsulfonylfuroxan conjugates with various anticancer agents for targeted cancer therapy.","PeriodicalId":257,"journal":{"name":"Bioorganic Chemistry","volume":"154 ","pages":"108020"},"PeriodicalIF":4.5,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142805774","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"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