Biomedicine & Pharmacotherapy最新文献

筛选
英文 中文
Retraction notice to "Moschus exerted protective activity against H2O2-induced cell injury in PC12 cells through regulating Nrf-2/ARE signaling pathways" [Biomedicine & Pharmacotherapy 159 (2023) 114290] 撤回“Moschus通过调节Nrf-2/ARE信号通路对h2o2诱导的PC12细胞损伤具有保护作用”[生物医药与药物治疗]159(2023)114290]。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-10 DOI: 10.1016/j.biopha.2026.119201
Danni Xie , Ting Deng , Zhenwei Zhai , Tao Qin , Caiyou Song , Ying Xu , Tao Sun
{"title":"Retraction notice to \"Moschus exerted protective activity against H2O2-induced cell injury in PC12 cells through regulating Nrf-2/ARE signaling pathways\" [Biomedicine & Pharmacotherapy 159 (2023) 114290]","authors":"Danni Xie , Ting Deng , Zhenwei Zhai , Tao Qin , Caiyou Song , Ying Xu , Tao Sun","doi":"10.1016/j.biopha.2026.119201","DOIUrl":"10.1016/j.biopha.2026.119201","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119201"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147438446","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
Retraction notice to “Pinostrobin ameliorates lipopolysaccharide (LPS)-induced inflammation and endotoxemia by inhibiting LPS binding to the TLR4/MD2 complex” [Biomed. Pharmacother. 156 (2022) 113874] “Pinostrobin通过抑制脂多糖(LPS)与TLR4/MD2复合物的结合,改善脂多糖(LPS)诱导的炎症和内毒素血症”的撤回通知[Biomed]。药理学杂志,2006(5):349 - 349。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-10 DOI: 10.1016/j.biopha.2026.119108
Athapaththu Mudiyanselage Gihan Kavinda Athapaththu , Kyeong Tae Lee , Mirissa Hewage Dumindu Kavinda , Seunghun Lee , Sanghyuck Kang , Mi-Hwa Lee , Chang-Hee Kang , Yung Hyun Choi , Gi-Young Kim
{"title":"Retraction notice to “Pinostrobin ameliorates lipopolysaccharide (LPS)-induced inflammation and endotoxemia by inhibiting LPS binding to the TLR4/MD2 complex” [Biomed. Pharmacother. 156 (2022) 113874]","authors":"Athapaththu Mudiyanselage Gihan Kavinda Athapaththu , Kyeong Tae Lee , Mirissa Hewage Dumindu Kavinda , Seunghun Lee , Sanghyuck Kang , Mi-Hwa Lee , Chang-Hee Kang , Yung Hyun Choi , Gi-Young Kim","doi":"10.1016/j.biopha.2026.119108","DOIUrl":"10.1016/j.biopha.2026.119108","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119108"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147438487","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
A rise in double-strand breaks sensitizes tumors to oxidative metabolism inhibitors 双链断裂的增加使肿瘤对氧化代谢抑制剂敏感
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-10 DOI: 10.1016/j.biopha.2026.119184
Ferran Medina-Jover , Agnès Figueras , Núria Gendrau-Sanclemente , Emilio Racionero-Andrés , Meritxell Sociats-Font , Álvaro Lahiguera , Pau Guillén , María Tormo-Fabios , Roderic Espín , Miguel Ángel Pardo-Cea , Andrés Mendez-Lucas , Edurne Berra , Josep Maria Piulats , Álvaro Aytés , Alberto Villanueva , Adrià Bernat-Peguera , Margarita Romeo , Miquel Angel Pujana , José Carlos Perales , Francesc Viñals
{"title":"A rise in double-strand breaks sensitizes tumors to oxidative metabolism inhibitors","authors":"Ferran Medina-Jover ,&nbsp;Agnès Figueras ,&nbsp;Núria Gendrau-Sanclemente ,&nbsp;Emilio Racionero-Andrés ,&nbsp;Meritxell Sociats-Font ,&nbsp;Álvaro Lahiguera ,&nbsp;Pau Guillén ,&nbsp;María Tormo-Fabios ,&nbsp;Roderic Espín ,&nbsp;Miguel Ángel Pardo-Cea ,&nbsp;Andrés Mendez-Lucas ,&nbsp;Edurne Berra ,&nbsp;Josep Maria Piulats ,&nbsp;Álvaro Aytés ,&nbsp;Alberto Villanueva ,&nbsp;Adrià Bernat-Peguera ,&nbsp;Margarita Romeo ,&nbsp;Miquel Angel Pujana ,&nbsp;José Carlos Perales ,&nbsp;Francesc Viñals","doi":"10.1016/j.biopha.2026.119184","DOIUrl":"10.1016/j.biopha.2026.119184","url":null,"abstract":"<div><div>Double-strand breaks (DSBs) accumulate in tumoral DNA due to deficiencies in homologous recombination (HR) repair, such as mutations in BRCA genes, or following antitumoral treatments. In the present study, we show that DSB accumulation, irrespective of origin, triggers an adaptive shift toward oxidative metabolism. We demonstrate that DSBs downregulate the glycolytic transcription factor HIF-1α. This downregulation reduces PDHK1 expression, thereby activating the pyruvate dehydrogenase complex, a key mitochondrial gatekeeper of cellular metabolism. We establish that the induction of oxidative metabolism represents a therapeutically actionable vulnerability across diverse cancer types, independent of HR proficiency. Targeting this metabolic switch in combination with DSB-inducing chemotherapies synergizes <em>in vivo</em>, resulting in significantly reduced tumor growth. Collectively, our findings reveal a critical feedback loop linking DSBs to cancer cell metabolism that constrains metabolic plasticity and creates a compelling therapeutic opportunity for rational combination strategies.</div></div>","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119184"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147387826","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
Corrigendum to “Protective effect of sargahydroquinoic acid against Aβ25–35-evoked damage via PI3K/Akt mediated Nrf2 antioxidant defense system” [Biomed. Pharmacother., vol. 144, (2021), 112271] “通过PI3K/Akt介导的Nrf2抗氧化防御系统对a - β25-35诱发的损伤的保护作用”[Biomed.]的更正。Pharmacother。, vol. 144,(2021), 112271]。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-05 DOI: 10.1016/j.biopha.2026.119146
Jeong-Hyun Yoon , Kumju Youn , Mira Jun
{"title":"Corrigendum to “Protective effect of sargahydroquinoic acid against Aβ25–35-evoked damage via PI3K/Akt mediated Nrf2 antioxidant defense system” [Biomed. Pharmacother., vol. 144, (2021), 112271]","authors":"Jeong-Hyun Yoon ,&nbsp;Kumju Youn ,&nbsp;Mira Jun","doi":"10.1016/j.biopha.2026.119146","DOIUrl":"10.1016/j.biopha.2026.119146","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119146"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147370852","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
Corrigendum to “Chronic citalopram effects on the brain neurochemical profile and perfusion in a rat model of depression detected by the NMR techniques – Spectroscopy and perfusion” [Biomed. Pharmacother. 181 (2024) 117656] “慢性西酞普兰对大鼠抑郁症模型的脑神经化学特征和灌注的影响,通过核磁共振技术检测-光谱学和灌注”[生物医学杂志]。药理学杂志,181(2024):117656。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-02-27 DOI: 10.1016/j.biopha.2026.119170
Iveta Harastova-Pavlova , Eva Drazanova , Lucie Kratka , Petra Amchova , Maria Hrickova , Ondrej Macicek , Jiri Vitous , Radovan Jirik , Jana Ruda-Kucerova
{"title":"Corrigendum to “Chronic citalopram effects on the brain neurochemical profile and perfusion in a rat model of depression detected by the NMR techniques – Spectroscopy and perfusion” [Biomed. Pharmacother. 181 (2024) 117656]","authors":"Iveta Harastova-Pavlova ,&nbsp;Eva Drazanova ,&nbsp;Lucie Kratka ,&nbsp;Petra Amchova ,&nbsp;Maria Hrickova ,&nbsp;Ondrej Macicek ,&nbsp;Jiri Vitous ,&nbsp;Radovan Jirik ,&nbsp;Jana Ruda-Kucerova","doi":"10.1016/j.biopha.2026.119170","DOIUrl":"10.1016/j.biopha.2026.119170","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119170"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147319238","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
Retraction notice to: "Current status and future therapeutic perspectives of glioblastoma multiforme (GBM) therapy: A review" [ Biomedicine & Pharmacotherapy 92 (2017) 681-689] 对“多形性胶质母细胞瘤(GBM)治疗的现状及未来治疗前景综述”的撤回通知[生物医学与药物治疗92(2017)681-689]。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-02-26 DOI: 10.1016/j.biopha.2026.119164
Komal Anjum , Bibi Ibtesam Shagufta , Syed Qamar Abbas , Seema Patel , Ishrat Khan , Sayed Asmat Ali Shah , Najeeb Akhter , Syed Shams ul Hassan
{"title":"Retraction notice to: \"Current status and future therapeutic perspectives of glioblastoma multiforme (GBM) therapy: A review\" [ Biomedicine & Pharmacotherapy 92 (2017) 681-689]","authors":"Komal Anjum ,&nbsp;Bibi Ibtesam Shagufta ,&nbsp;Syed Qamar Abbas ,&nbsp;Seema Patel ,&nbsp;Ishrat Khan ,&nbsp;Sayed Asmat Ali Shah ,&nbsp;Najeeb Akhter ,&nbsp;Syed Shams ul Hassan","doi":"10.1016/j.biopha.2026.119164","DOIUrl":"10.1016/j.biopha.2026.119164","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119164"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147313468","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
Retraction notice to "Acute myocardial infarction therapy using calycosin and tanshinone co-loaded mitochondria targeted lipid-polymer hybrid nano-system: Preparation, characterization, and anti myocardial infarction activity assessment" [Biomed. Pharmacother. 155 (2022) 113650] “用毛蕊异黄酮和丹参酮共载线粒体靶向脂质-聚合物混合纳米系统治疗急性心肌梗死:制备、表征和抗心肌梗死活性评估”撤回通知[生物医学杂志]。药理学杂志,2015(5):349 - 349。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-16 DOI: 10.1016/j.biopha.2026.119224
Jieke Yan , Jing Guo , Yuzhen Wang , Xiaowei Xing , Xuguang Zhang , Guanghao Zhang , Zhaoqiang Dong
{"title":"Retraction notice to \"Acute myocardial infarction therapy using calycosin and tanshinone co-loaded mitochondria targeted lipid-polymer hybrid nano-system: Preparation, characterization, and anti myocardial infarction activity assessment\" [Biomed. Pharmacother. 155 (2022) 113650]","authors":"Jieke Yan ,&nbsp;Jing Guo ,&nbsp;Yuzhen Wang ,&nbsp;Xiaowei Xing ,&nbsp;Xuguang Zhang ,&nbsp;Guanghao Zhang ,&nbsp;Zhaoqiang Dong","doi":"10.1016/j.biopha.2026.119224","DOIUrl":"10.1016/j.biopha.2026.119224","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119224"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147476488","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
Retraction notice to “Investigation of prunetrin induced G2/M cell cycle arrest and apoptosis via Akt/mTOR/MAPK pathways in hepatocellular carcinoma cells” [Biomed. Pharmacother. 174 (2024) 116483] 《prunetrin通过Akt/mTOR/MAPK通路诱导肝癌细胞G2/M细胞周期阻滞和凋亡的研究》撤回通知[Biomed. 2011]。药理学杂志。174(2024)116483。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-16 DOI: 10.1016/j.biopha.2026.119203
Abuyaseer Abusaliya , Pritam Bhagwan Bhosale , Hun Hwan Kim , Min Yeong Park , Se Hyo Jeong , Sijoon Lee , Gon Sup Kim
{"title":"Retraction notice to “Investigation of prunetrin induced G2/M cell cycle arrest and apoptosis via Akt/mTOR/MAPK pathways in hepatocellular carcinoma cells” [Biomed. Pharmacother. 174 (2024) 116483]","authors":"Abuyaseer Abusaliya ,&nbsp;Pritam Bhagwan Bhosale ,&nbsp;Hun Hwan Kim ,&nbsp;Min Yeong Park ,&nbsp;Se Hyo Jeong ,&nbsp;Sijoon Lee ,&nbsp;Gon Sup Kim","doi":"10.1016/j.biopha.2026.119203","DOIUrl":"10.1016/j.biopha.2026.119203","url":null,"abstract":"","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119203"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147476497","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
Ceftriaxone administration reduces vascular calcification associated with experimental models of chronic kidney disease 头孢曲松给药减少与慢性肾病实验模型相关的血管钙化。
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-05 DOI: 10.1016/j.biopha.2026.119131
Teresa Obrero Sojo , Ma José Jiménez Moral , Fátima Guerrero Pavón , Ma Encarnación Rodríguez Ortiz , Ana Isabel Torralbo , Karen Valdés Díaz , Raquel Ma García Sáez , Antonio Domínguez Rivas , Daniel Jurado Montoya , Fernando Leiva-Cepas , Ma Victoria Pendón Ruiz de Mier , Cristian Rodelo Haad , Griet Glorieux , Mariano Rodríguez , Sagrario Soriano Cabrera , Juan Rafael Muñoz Castañeda
{"title":"Ceftriaxone administration reduces vascular calcification associated with experimental models of chronic kidney disease","authors":"Teresa Obrero Sojo ,&nbsp;Ma José Jiménez Moral ,&nbsp;Fátima Guerrero Pavón ,&nbsp;Ma Encarnación Rodríguez Ortiz ,&nbsp;Ana Isabel Torralbo ,&nbsp;Karen Valdés Díaz ,&nbsp;Raquel Ma García Sáez ,&nbsp;Antonio Domínguez Rivas ,&nbsp;Daniel Jurado Montoya ,&nbsp;Fernando Leiva-Cepas ,&nbsp;Ma Victoria Pendón Ruiz de Mier ,&nbsp;Cristian Rodelo Haad ,&nbsp;Griet Glorieux ,&nbsp;Mariano Rodríguez ,&nbsp;Sagrario Soriano Cabrera ,&nbsp;Juan Rafael Muñoz Castañeda","doi":"10.1016/j.biopha.2026.119131","DOIUrl":"10.1016/j.biopha.2026.119131","url":null,"abstract":"<div><div>Gut microbiota dysbiosis has been implicated in systemic inflammation, potentially exacerbating chronic kidney disease (CKD) and vascular calcification (VC). The effects of gut microbiota depletion on VC using antibiotics remain largely unknown. We investigated the role of microbiota depletion in chronic and acute experimental models of CKD and VC in Wistar rats. The chronic CKD model consisted of 5/6 nephrectomy (Nx), a moderate-phosphate diet (0.9 %), and intraperitoneal injections of calcitriol (25 ng/kg i.p every 48 h) for 30 days. For the following 15 days, dietary phosphate was increased to 1.2 %, and calcitriol at 40 ng/kg i.p every 48 h. In the acute VC model, a high-phosphate diet (1.2 %) and calcitriol (60 ng/kg every 48 h) were administered for 14 days after the Nx. In both models, half of the animals received oral ceftriaxone (ATB, 400 mg/kg/day) for seven days prior to Nx. Parameters related to mineral metabolism, kidney function, bone histomorphometry and mineralization, VC, calcification-related signaling pathways, uremic toxins, and fecal microbiota composition and functional inference were analysed. Antibiotic-treated rats showed significantly lower serum phosphate levels, reduced uremic toxins, and decreased VC with no effects on bone turnover. Colidextribacter and Escherichia-Shigella were positively correlated with serum phosphate levels. Interestingly, Ceftriaxone treatment reduced the abundance of such genera. Additionally, the abundance of Colidextribacter also correlated with calcium content in the thoracic aorta. In conclusion, microbiota depletion by ceftriaxone reduced hyperphosphatemia and VC in experimental CKD and VC models. These findings support the potential of targeting the gut microbiota as a novel strategy to mitigate mineral metabolism disturbances and VC in CKD.</div></div>","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119131"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147373766","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
Synthesis and characterization of new P2X7 receptor antagonists as antitumor agents 新型P2X7受体拮抗剂的合成与表征
IF 7.5 2区 医学
Biomedicine & Pharmacotherapy Pub Date : 2026-04-01 Epub Date: 2026-03-11 DOI: 10.1016/j.biopha.2026.119185
Marianna Grignolo , Andrea Spinaci , Ludovica Ricci , Anna Pegoraro , Luigia Ruo , Catia Lambertucci , Daniele Vitone , Marcello Leopoldo , Enza Lacivita , Federica Fortuna , Michela Buccioni , Beatrice Francucci , Gabriella Marucci , Diego Dal Ben , Rosaria Volpini , Elena Adinolfi
{"title":"Synthesis and characterization of new P2X7 receptor antagonists as antitumor agents","authors":"Marianna Grignolo ,&nbsp;Andrea Spinaci ,&nbsp;Ludovica Ricci ,&nbsp;Anna Pegoraro ,&nbsp;Luigia Ruo ,&nbsp;Catia Lambertucci ,&nbsp;Daniele Vitone ,&nbsp;Marcello Leopoldo ,&nbsp;Enza Lacivita ,&nbsp;Federica Fortuna ,&nbsp;Michela Buccioni ,&nbsp;Beatrice Francucci ,&nbsp;Gabriella Marucci ,&nbsp;Diego Dal Ben ,&nbsp;Rosaria Volpini ,&nbsp;Elena Adinolfi","doi":"10.1016/j.biopha.2026.119185","DOIUrl":"10.1016/j.biopha.2026.119185","url":null,"abstract":"<div><div>Extracellular ATP is a key component of the tumor microenvironment, where it promotes cancer progression by activating the P2X7 receptor (P2X7R). Prolonged receptor stimulation triggers the release of pro-tumorigenic extracellular vesicles and soluble factors, including IL-1β, VEGF, and TGFβ. Here, we report the design and characterization of novel triazole- and benzamide-based negative allosteric modulators of P2X7R. Among these, compounds <strong>5</strong> and <strong>9</strong> showed nanomolar affinity for the human receptor (<em>K</em><sub>i</sub> = 80 nM and 3.17 nM, respectively) and effectively inhibited calcium influx (IC<sub>50</sub> 370 nM and 47 nM, respectively). Molecular docking supported distinct binding modes for the two scaffolds, aligning them with known allosteric inhibitors through interactions with Lys297, Asp92, and hydrophobic subpockets. Compounds <strong>5</strong> and <strong>9</strong> displayed favorable metabolic stability in mouse liver microsomes and efficiently blocked P2X7R-dependent signaling in melanoma, glioblastoma, and colon carcinoma cells. Treatment with both compounds significantly reduced tumor cell proliferation, invasiveness, and extracellular vesicle release, with efficacy comparable to or greater than that of the reference antagonist A740003. In vivo, both molecules suppressed melanoma growth in syngeneic mice and modulated cytokine levels in the TME by increasing IFN-γ while reducing VEGF, IL-1β, and TGF-β. These findings identify compounds <strong>5</strong> and <strong>9</strong> as potent, selective, and metabolically stable P2X7R antagonists with translational potential as anticancer agents targeting both tumor growth and extracellular vesicle-mediated communication.</div></div>","PeriodicalId":8966,"journal":{"name":"Biomedicine & Pharmacotherapy","volume":"197 ","pages":"Article 119185"},"PeriodicalIF":7.5,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147387417","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
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书