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The novel strategy to overcome the drug-resistant lung cancer: Dual targeting delivery of PROTAC to inhibit cancer-associated fibroblasts and lung cancer cells 克服耐药肺癌的新策略:双靶向递送PROTAC以抑制癌症相关成纤维细胞和肺癌细胞
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2026-01-01 Epub Date: 2025-10-17 DOI: 10.1016/j.drup.2025.101316
Lingmin Zhang , Linlong He , Yinshan Lin , Juyan Wei , Shiqi Tang , Xueping Lei , Xufeng Lin , Dazhi Zhou , Liwu Fu , Yuehua Li , Juyun He , Lu Liang , Xi-Yong Yu
Current pharmacotherapy on the fatal lung cancer is often limited by the development of drug resistance, which significantly contributes to treatment failure. The drug resistance in cancer is associated with tumor microenvironment (TME), particularly with cancer-associated fibroblasts (CAFs). However, the present approaches show little progress in the eliminating lung cancer cells and reversing the TME synergistically. The emergence of nanomedicine offers promising strategies to overcome this challenge. In this study, we developed a proteolysis-targeting chimeras (PROTAC)-based nanodrug, designed to eliminate both lung cancer cells and CAFs, thereby amplifying the therapeutic effects. This nanodrug was constructed by loading dBET6 with US Food and Drug Administration (FDA) approved polymer Poly(lactic-co-glycolic acid) (PLGA), and further camouflaged with the hybrid membranes derived from platelet and lung cancer cells (PLMPD). PLMPD demonstrated excellent dual-targeting capabilities to both lung cancer cells and CAFs, leading to significant apoptosis in both cell types in vitro. We also found that PLMPD could inhibited the growth of Osimertinib-resistant cells. In vivo studies revealed that PLMPD enhanced tumor targeting, effectively inhibited tumor growth, and reversed the tumor-promoting TME in the lung cancer xenograft models. These findings underscore the potential of PLMPD as a promising PROTAC-based nanodrug for lung cancer therapy, offering a new avenue for overcoming drug resistance and improving treatment outcomes.
目前对致命肺癌的药物治疗往往受到耐药性的限制,这是导致治疗失败的重要原因。肿瘤耐药与肿瘤微环境(tumor microenvironment, TME)有关,特别是与癌症相关成纤维细胞(cancer-associated fibroblasts, CAFs)有关。然而,目前的方法在消除肺癌细胞和协同逆转TME方面进展甚微。纳米医学的出现为克服这一挑战提供了有希望的策略。在这项研究中,我们开发了一种基于蛋白水解靶向嵌合体(PROTAC)的纳米药物,旨在消除肺癌细胞和CAFs,从而扩大治疗效果。该纳米药物由美国食品和药物管理局(FDA)批准的聚合物聚乳酸-羟基乙酸(PLGA)负载dBET6构建,并进一步用来自血小板和肺癌细胞的杂交膜(PLMPD)进行伪装。在体外实验中,PLMPD对肺癌细胞和caf均表现出出色的双靶向能力,导致两种细胞类型的显著凋亡。我们还发现PLMPD可以抑制奥西替尼耐药细胞的生长。体内研究显示,PLMPD在肺癌异种移植模型中增强肿瘤靶向性,有效抑制肿瘤生长,逆转促瘤TME。这些发现强调了PLMPD作为一种有前景的基于protac的肺癌治疗纳米药物的潜力,为克服耐药性和改善治疗结果提供了新的途径。
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引用次数: 0
Integration of blaOXA-48 into a Col156 plasmid drove a carbapenem-resistant Escherichia coli ST131 outbreak in New Zealand: Global genomic evidence for the gene’s multilayered dissemination 将blaOXA-48整合到Col156质粒中,导致了新西兰耐碳青霉烯类大肠杆菌ST131的爆发:该基因多层次传播的全球基因组证据
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2026-01-01 Epub Date: 2025-11-19 DOI: 10.1016/j.drup.2025.101327
Rhys T. White , Craig N. Thornley , Max Bloomfield , Kristin Dyet , Juliet Elvy , Hermes Perez , Allan Hardaker , Michael Harrington , Simon Jackson , Matthew Kelly , Loushy Mangalasseril , Annette Nesdale , Xiaoyun Ren , Jenny Szeto , Claire Underwood , David Winter , Rosemary Woodhouse , Zuyu Yang

Aims

To investigate the genetic diversity in OXA-48-producing Escherichia coli ST131 in a New Zealand community outbreak, and to characterize the mobile genetic elements carrying blaOXA-48, with emphasis on the gene’s global dissemination.

Methods

Forty outbreak isolates underwent short-read sequencing; 36 also underwent long-read sequencing. Bayesian phylogenetics reconstructed the emergence and spread of the outbreak. A pangenome graph of 543 Col156 plasmids and 806 global blaOXA-48-positive contigs were analyzed to assess structural diversity, mobility, and global distribution.

Results

The outbreak clone likely emerged circa 2017, following a single introduction into New Zealand after acquiring blaOXA-48 on a 7872 bp Col156 plasmid. It shares ancestry (circa 2009) with Southeast Asian E. coli ST131 genomes. Long-read sequencing and pangenome graph analyses identified a single IS1-mediated transposition of blaOXA-48 into a Col156 plasmid backbone, observed across species and continents. Globally, blaOXA-48 is present in diverse plasmid contexts and insertion sequence arrangements and is widely distributed among Enterobacterales.

Conclusions

This is the first high-resolution genomic reconstruction of a community-associated blaOXA-48 outbreak, identifying a compact Col156 plasmid as a key vector driving carbapenem resistance. Our findings demonstrate the value of complete genome assemblies and pangenome graph analyses in resolving the structural and evolutionary dynamics of antimicrobial resistance.
目的研究新西兰社区暴发中产生oxa -48的大肠杆菌ST131的遗传多样性,并表征携带blaOXA-48的移动遗传元件,重点研究该基因的全球传播。方法对40株暴发分离株进行短读测序;36个也进行了长读测序。贝叶斯系统发育重建了疫情的出现和传播。分析了543个Col156质粒和806个全球blaoxa -48阳性contigs的全基因组图,以评估结构多样性、流动性和全球分布。结果爆发克隆可能在2017年左右出现,在7872 bp Col156质粒上获得blaOXA-48后,被引入新西兰。它与东南亚大肠杆菌ST131基因组共享祖先(大约2009年)。长读测序和全基因组图分析发现,在不同物种和大洲中都观察到is1介导的blaOXA-48转位到Col156质粒主干。在全球范围内,blaOXA-48存在于不同的质粒背景和插入序列安排中,广泛分布于肠杆菌中。这是社区相关blaOXA-48暴发的第一个高分辨率基因组重建,确定了紧凑的Col156质粒是驱动碳青霉烯类耐药性的关键载体。我们的研究结果证明了全基因组组装和泛基因组图谱分析在解决抗菌素耐药性的结构和进化动力学方面的价值。
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引用次数: 0
The role of tumor microenvironment and signaling pathways in regulating breast cancer stem cells: Implications for therapy resistance and tumor recurrence 肿瘤微环境和信号通路在调节乳腺癌干细胞中的作用:对治疗抵抗和肿瘤复发的影响
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2026-01-01 Epub Date: 2025-10-13 DOI: 10.1016/j.drup.2025.101315
Hongbo Zhang , Yue Sun , Rui Liu , Hayam Hamdy , Zhi Shi , Dewei Jiang , Jianwei Sun
Breast cancer stem cells (BCSCs) are recognized as a critical subpopulation involved in cancer recurrence and metastasis, as they are capable of self-renewal and differentiate into various cell types. BCSCs play significant roles in tumor progression, being regulated by key signaling pathways such as Notch, PI3K/AKT/mTOR, and Hedgehog, and their interactions with the tumor microenvironment, which affect tumor growth and resistance to therapeutics. This review focuses on the surface markers of BCSCs, their roles in recurrence and metastasis, and the key signaling pathways. It also discusses the recent progress in understanding how BCSCs contribute to drug resistance and explores potential therapeutic strategies targeting these cells and their microenvironment to improve clinical outcomes and prevent relapse.
乳腺癌干细胞(BCSCs)被认为是参与癌症复发和转移的关键亚群,因为它们能够自我更新并分化成各种细胞类型。BCSCs在肿瘤进展中发挥重要作用,受Notch、PI3K/AKT/mTOR和Hedgehog等关键信号通路调控,并与肿瘤微环境相互作用,影响肿瘤生长和对治疗药物的耐药性。本文就bscs的表面标记物及其在复发转移中的作用、关键信号通路进行综述。它还讨论了了解BCSCs如何促进耐药的最新进展,并探讨了针对这些细胞及其微环境的潜在治疗策略,以改善临床结果和预防复发。
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引用次数: 0
Gamma-synuclein drives bevacizumab resistance in colorectal cancer via VEGFR2 activation and angiogenesis γ -突触核蛋白通过VEGFR2激活和血管生成驱动结直肠癌的贝伐单抗耐药
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2026-01-01 Epub Date: 2025-09-09 DOI: 10.1016/j.drup.2025.101299
Caiyun Liu , Lin Meng , Lixin Wang , Bin Dong , Like Qu , Chuanke Zhao , Chengchao Shou

Background

Resistance to Bevacizumab (Bev) remains a major obstacle in colorectal cancer (CRC) treatment. Gamma-synuclein (SNCG), overexpressed in tumor vasculature and cancer cells, is investigated here for its role in Bev resistance and therapeutic potential.

Methods

Using isogenic CRC models with SNCG overexpression or knockout, we assessed SNCG's impact on Bev response in vitro and in vivo. The therapeutic efficacy of combining Bev with an anti-SNCG monoclonal antibody (42#) was evaluated in Bev-resistant models. Mechanistic studies, including ELISA, Western blot, surface plasmon resonance (SPR), and molecular docking, explored interactions between SNCG, VEGF, and VEGFR2.

Results

SNCG overexpression reduced Bev sensitivity by impairing the inhibition of migration, invasion, and spheroid formation, whereas SNCG knockout enhanced therapeutic response. Molecular docking revealed that SNCG binds VEGFR2 at an allosteric site, forming a stable ternary complex (SNCG-VEGF-VEGFR2) with enhanced hydrogen bonding, which sustained VEGFR2 phosphorylation and angiogenesis. In vivo, SNCG-overexpressing tumors showed reduced responsiveness to Bev (42.8 % inhibition vs. 64.3 % in controls, p < 0.05), while SNCG-deficient tumors exhibited a 3.2-fold increase in sensitivity. Combining Bev with 42# synergistically suppressed tumor growth (0.70 ± 0.36 g vs. 1.55 ± 0.41 g, p = 0.003), reduced metastatic burden (0.29 ± 0.23 g vs. 0.97 ± 0.42 g, p = 0.006), and extended median survival (86.8 vs. 69.8 days, p = 0.033) in Bev-resistant models.

Conclusions

SNCG drives Bev resistance in CRC by forming a ternary complex with VEGF and VEGFR2, enhancing VEGFR2 signaling and angiogenesis. Dual targeting of VEGF and SNCG represents a promising therapeutic strategy to overcome Bev resistance, with the potential to improve outcomes in CRC patients.
贝伐单抗(Bevacizumab, Bev)耐药仍然是结直肠癌(CRC)治疗的主要障碍。在肿瘤血管和癌细胞中过度表达的γ -突触核蛋白(SNCG)在Bev耐药和治疗潜力中的作用进行了研究。方法采用SNCG过表达或敲除的等基因CRC模型,在体外和体内评估SNCG对Bev反应的影响。在Bev耐药模型中评估Bev联合抗sncg单克隆抗体(42#)的治疗效果。机制研究包括ELISA、Western blot、表面等离子体共振(SPR)和分子对接等,探讨了SNCG、VEGF和VEGFR2之间的相互作用。结果SNCG过表达降低了Bev的敏感性,损害了对迁移、侵袭和球体形成的抑制,而SNCG敲除增强了治疗反应。分子对接发现,SNCG在变构位点与VEGFR2结合,形成稳定的三元配合物(SNCG- vegf -VEGFR2),氢键增强,维持VEGFR2磷酸化和血管生成。在体内,sncg过表达的肿瘤对Bev的反应性降低(对照组抑制率为42.8 %,对照组为64.3 %,p <; 0.05),而sncg缺陷肿瘤的敏感性增加了3.2倍。贝福结合42 #协同抑制肿瘤生长( 0.70±0.36  g和1.55 ±0.41  g p = 0.003),降低转移负担( 0.29±0.23  g和0.97 ±0.42  g p = 0.006),和延长平均存活(86.8 vs 69.8天,p = 0.033)在Bev-resistant模型。结论sncg通过与VEGF和VEGFR2形成三元复合物,增强VEGFR2信号传导和血管生成,从而驱动结直肠癌的Bev耐药。VEGF和SNCG的双重靶向治疗是克服Bev耐药的一种有希望的治疗策略,有可能改善结直肠癌患者的预后。
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引用次数: 0
Peptide nanonet trapping suppresses bacterial motility and delays antibiotic resistance emergence 肽纳米捕获抑制细菌运动和延迟抗生素耐药性的出现
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2026-01-01 Epub Date: 2025-10-29 DOI: 10.1016/j.drup.2025.101320
Jian Xu , Nhan Dai Thien Tram , Peiyan Yu, Dhanya Mahalakshmi Murali, Wei Meng Chen, Samantha Jinglin Yang , Pui Lai Rachel Ee

Aims

In the presence of antibiotics, motile bacteria can navigate chemical gradients for adaptation and survival. Antimicrobial peptides (AMPs) have been widely explored as adjuvant to improve the activity potency of antibiotics, but mainly through the disruption of bacterial membranes. In this work, we investigated the impact of nanonet trapping using fibrillating peptides, a mechanistically unique sub-group of AMPs, on motility recovery of bacteria and their capacity to develop antibiotic resistance.

Methods

The ability of fibrillating AMPs to potentiate activity and delay resistance of antibiotics from diverse classes was evaluated against clinical isolates of Gram-negative pathogens. Using soft agar assay and live-tracking microscopy, shifts in the motility of the bacteria population subjected to different treatments were evaluated. To further elucidate the mechanism of action, the expression of major flagella-encoding genes was quantified and hypomotile bacteria strains were studied.

Results

At sub-inhibitory concentrations, fibrillating peptides not only displayed synergistic interactions, but also significantly delayed the emergence of resistance to antibiotics such as rifampicin for at least 18 days. The peptide-antibiotic synergy profiles were lost after prolonged treatment with antibiotic monotherapy but preserved when co-administered with fibrillating peptides throughout the serial passage. The nanonet-forming peptides were shown to serve as a motility filter where the bacteria population gradually shifted towards homogeneous hypomotility associated with inferior survivability.

Conclusions

This work showcases the potential of AMPs as low-concentration adjuvants for extending the clinical lifespan of current antibiotics and highlights bacterial motility as an underexplored target for antibiotic development.
目的在抗生素的存在下,活动细菌可以通过化学梯度来适应和生存。抗菌肽(Antimicrobial peptides, AMPs)作为提高抗生素活性效力的佐剂已被广泛研究,但主要是通过破坏细菌膜。在这项工作中,我们研究了利用纤颤肽(amp的一个独特的亚群)捕获纳米网络对细菌运动恢复及其产生抗生素耐药性的能力的影响。方法以临床分离的革兰氏阴性病原菌为对照,评价纤颤amp增强不同种类抗生素的活性和延迟耐药性的能力。使用软琼脂实验和实时跟踪显微镜,在不同的处理下,细菌群体的运动能力的变化进行了评估。为了进一步阐明其作用机制,我们对主要鞭毛编码基因的表达进行了量化,并对低动菌菌株进行了研究。结果在亚抑制浓度下,纤颤肽不仅表现出协同作用,而且显著延缓了利福平等抗生素耐药的出现至少18天。在长时间的抗生素单药治疗后,肽-抗生素协同作用谱丢失,但在整个序列通道中与纤颤肽共同施用时保留。纳米形成肽被证明可以作为一种运动过滤器,在那里细菌群体逐渐转向均匀的低运动,与低生存能力相关。结论:本研究显示了抗菌肽作为低浓度佐剂的潜力,可以延长当前抗生素的临床使用寿命,并强调了细菌运动是抗生素开发中一个未被充分开发的靶点。
{"title":"Peptide nanonet trapping suppresses bacterial motility and delays antibiotic resistance emergence","authors":"Jian Xu ,&nbsp;Nhan Dai Thien Tram ,&nbsp;Peiyan Yu,&nbsp;Dhanya Mahalakshmi Murali,&nbsp;Wei Meng Chen,&nbsp;Samantha Jinglin Yang ,&nbsp;Pui Lai Rachel Ee","doi":"10.1016/j.drup.2025.101320","DOIUrl":"10.1016/j.drup.2025.101320","url":null,"abstract":"<div><h3>Aims</h3><div>In the presence of antibiotics, motile bacteria can navigate chemical gradients for adaptation and survival. Antimicrobial peptides (AMPs) have been widely explored as adjuvant to improve the activity potency of antibiotics, but mainly through the disruption of bacterial membranes. In this work, we investigated the impact of nanonet trapping using fibrillating peptides, a mechanistically unique sub-group of AMPs, on motility recovery of bacteria and their capacity to develop antibiotic resistance.</div></div><div><h3>Methods</h3><div>The ability of fibrillating AMPs to potentiate activity and delay resistance of antibiotics from diverse classes was evaluated against clinical isolates of Gram-negative pathogens. Using soft agar assay and live-tracking microscopy, shifts in the motility of the bacteria population subjected to different treatments were evaluated. To further elucidate the mechanism of action, the expression of major flagella-encoding genes was quantified and hypomotile bacteria strains were studied.</div></div><div><h3>Results</h3><div>At sub-inhibitory concentrations, fibrillating peptides not only displayed synergistic interactions, but also significantly delayed the emergence of resistance to antibiotics such as rifampicin for at least 18 days. The peptide-antibiotic synergy profiles were lost after prolonged treatment with antibiotic monotherapy but preserved when co-administered with fibrillating peptides throughout the serial passage. The nanonet-forming peptides were shown to serve as a motility filter where the bacteria population gradually shifted towards homogeneous hypomotility associated with inferior survivability.</div></div><div><h3>Conclusions</h3><div>This work showcases the potential of AMPs as low-concentration adjuvants for extending the clinical lifespan of current antibiotics and highlights bacterial motility as an underexplored target for antibiotic development.</div></div>","PeriodicalId":51022,"journal":{"name":"Drug Resistance Updates","volume":"84 ","pages":"Article 101320"},"PeriodicalIF":21.7,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145382791","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"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
Overcoming delivery challenges of antimicrobial peptides for clinical translation: From nanocarriers to molecular modifications 克服临床翻译抗菌肽的递送挑战:从纳米载体到分子修饰
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2025-11-01 Epub Date: 2025-08-05 DOI: 10.1016/j.drup.2025.101289
Nan Gao, Jiaqi Sun, Xiang Li, Yuting Yao, Yujie Hu, Jiani Zhao, Anshan Shan, Jiajun Wang
Antimicrobial peptides (AMPs) have emerged as a promising solution to combat multidrug-resistant (MDR) bacteria. Their unique mechanisms of action reduce the likelihood of resistance development. However, despite their potential, AMPs in clinical trials face significant challenges, including proteolytic degradation and short half-lives during systemic or oral administration. To address these limitations and enhance AMP stability and therapeutic efficacy, several key strategies have been explored. In this review, we summarize recent advances in AMP design, covering: 1) the delivery and formulation of AMPs, including metal-based, polymer-based, and lipid-based delivery systems, as well as the self-assembled nanotechnology of AMPs; 2) the internal modification of AMPs, including stereochemical modification, structural cyclization modification, and terminal modification. This review provides critical insights into AMP optimization, guides the development of future drug candidates, and highlights the interdisciplinary approaches required to accelerate clinical translation.
抗菌肽(AMPs)已成为对抗多药耐药(MDR)细菌的一种有前途的解决方案。它们独特的作用机制降低了产生耐药性的可能性。然而,尽管AMPs具有潜力,但在临床试验中面临着重大挑战,包括在全身或口服给药过程中蛋白水解降解和半衰期短。为了解决这些限制并提高AMP的稳定性和治疗效果,研究人员探索了几个关键策略。本文综述了AMP设计的最新进展,包括:1)AMP的递送和配方,包括金属基、聚合物基和脂质基递送系统,以及AMP的自组装纳米技术;2) AMPs的内部修饰,包括立体化学修饰、结构环化修饰和末端修饰。这篇综述为AMP优化提供了重要的见解,指导了未来候选药物的开发,并强调了加速临床转化所需的跨学科方法。
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引用次数: 0
Targeting DNA damage response pathways in tumor drug resistance: Mechanisms, clinical implications, and future directions 肿瘤耐药中的靶向DNA损伤反应途径:机制、临床意义和未来方向
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2025-11-01 Epub Date: 2025-08-05 DOI: 10.1016/j.drup.2025.101287
Hengzhou Zhu , Yuanyang Tian , Haoyan Chen , Yiyang Qian , Jiahui Li , Dong Niu , Wenyue Zhao , Yulin Wu , Xian Zhang , Tao Tang , Hu Li , Yan-Fang Xian , Dongdong Sun , Chunhui Jin
Targeting DNA damage response (DDR) pathways has become a promising strategy for overcoming tumor drug resistance, particularly in cancers with DNA repair defects. DDR pathways, including homologous recombination (HR), non-homologous end joining (NHEJ), base excision repair (BER), and mismatch repair (MMR), are essential for maintaining genomic stability. However, resistance to DDR-targeted therapies, such as PARP inhibitors, often arises due to tumor adaptation through various mechanisms. These include HR pathway restoration, mutations in DDR proteins, altered drug metabolism, and the activation of compensatory repair pathways. This review provides a comprehensive analysis of the molecular mechanisms underlying DDR resistance in tumors and explores the clinical implications of these mechanisms in the context of ongoing therapeutic strategies. We also discuss emerging approaches to overcome DDR resistance, including the development of novel DDR inhibitors, combination therapies, and precision medicine approaches based on biomarkers. Furthermore, we highlight future research directions, focusing on the use of advanced technologies, such as CRISPR screening, single-cell sequencing, and artificial intelligence, to uncover new targets and therapeutic strategies to combat DDR-related drug resistance.
靶向DNA损伤反应(DDR)途径已成为克服肿瘤耐药的一种有前景的策略,特别是在DNA修复缺陷的癌症中。DDR通路,包括同源重组(HR)、非同源末端连接(NHEJ)、碱基切除修复(BER)和错配修复(MMR),对维持基因组稳定性至关重要。然而,对ddr靶向治疗的耐药,如PARP抑制剂,往往是由于肿瘤通过各种机制的适应而产生的。这些包括HR通路恢复、DDR蛋白突变、药物代谢改变和代偿修复通路的激活。这篇综述全面分析了肿瘤中DDR耐药的分子机制,并探讨了这些机制在正在进行的治疗策略中的临床意义。我们还讨论了克服DDR耐药的新方法,包括新型DDR抑制剂的开发、联合疗法和基于生物标志物的精准医学方法。此外,我们强调了未来的研究方向,重点是利用先进技术,如CRISPR筛选、单细胞测序和人工智能,发现新的靶点和治疗策略,以对抗ddr相关的耐药。
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引用次数: 0
Targeted therapy in acute myeloid leukemia: Resistance and overcoming strategy 急性髓系白血病的靶向治疗:耐药性和克服策略
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2025-11-01 Epub Date: 2025-07-31 DOI: 10.1016/j.drup.2025.101286
Feifeng Song , Sisi Lin , Tong Xu , Chang Yang , Bold Sharavyn , Hua Naranmandura , Yiwen Zhang , Ping Huang
Acute myeloid leukemia (AML) is an aggressive hematological malignancy characterized by uncontrolled proliferation of immature myeloid blasts, leading to hematopoietic suppression and bone marrow failure. Advances in understanding the pathogenesis of AML have fueled the development of precision medicine approaches, with notable successes in targeting specific mutant proteins (e.g., FLT3, IDH1, IDH2), apoptotic regulators (e.g., BCL-2, MCL1), and cell-surface antigens (e.g., CD33, CD123, CD47). These targeted inhibitors exhibit moderate antileukemic activity as monotherapies and their clinical responses are often limited due to the emergence of drug resistance and disease relapse. Nevertheless, synergistic effects have been observed when these agents are combined with conventional chemotherapy or oncogenic pathway inhibitors. This review analyzes the current limitations of targeted therapies and explores multifaceted resistance drivers, encompassing on-target mutations, compensatory signaling pathway activation, drug-efflux mechanisms mediated by metabolic enzymes or transporters, intrinsic adaptive changes, and interactions with the tumor microenvironment. Corresponding therapeutic counterstrategies are also examined, such as mutation-specific molecular targeting, combinatorial suppression of alternative pathways, disruption of intrinsic adaptive responses, and immunotherapeutic approaches. These evolving interventions aim to overcome specific resistance mechanisms and reduce relapse rates. Future research integrating these strategies holds significant promise for addressing persistent challenges in AML management, ultimately advancing treatment paradigms and patient survival.
急性髓细胞白血病(AML)是一种侵袭性血液系统恶性肿瘤,其特征是未成熟髓细胞不受控制的增殖,导致造血抑制和骨髓衰竭。了解AML发病机制的进展推动了精准医学方法的发展,在靶向特定突变蛋白(如FLT3、IDH1、IDH2)、凋亡调节因子(如BCL-2、MCL1)和细胞表面抗原(如CD33、CD123、CD47)方面取得了显著成功。这些靶向抑制剂作为单一疗法表现出中等的抗白血病活性,由于出现耐药性和疾病复发,它们的临床反应往往受到限制。然而,当这些药物与常规化疗或致癌途径抑制剂联合使用时,已观察到协同效应。本文分析了目前靶向治疗的局限性,并探讨了多方面的耐药驱动因素,包括靶突变、代偿信号通路激活、代谢酶或转运体介导的药物外排机制、内在适应性变化以及与肿瘤微环境的相互作用。相应的治疗对策也进行了研究,如突变特异性分子靶向、替代途径的组合抑制、内在适应性反应的破坏和免疫治疗方法。这些不断发展的干预措施旨在克服特定的耐药机制并降低复发率。整合这些策略的未来研究对于解决AML管理中持续存在的挑战具有重要的前景,最终推进治疗范式和患者生存率。
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引用次数: 0
Targeting CLK1/SRSF7 axis-dependent alternative splicing sensitizes pancreatic ductal adenocarcinoma to chemotherapy and immunotherapy 靶向CLK1/SRSF7轴依赖性替代剪接使胰腺导管腺癌对化疗和免疫治疗增敏
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2025-11-01 Epub Date: 2025-08-16 DOI: 10.1016/j.drup.2025.101292
Chun Zhang , Yinhao Chen , Shuncang Zhu , Zuwei Wang , Hongyi Lin , Jinpeng Lu , Haoxiang Zhang , Yueyi Weng , Xiaoxiao Huang , Ge Li , Yongding Wu , Zhiyuan Li , Jianfei Hu , Chengke Xie , Jianlin Lai , Yifeng Tian , Chengyu Liao , Shi Chen

Aim

The persistently high mortality rate of pancreatic ductal adenocarcinoma (PDAC) is largely attributed to the acquired resistance to chemotherapy, particularly gemcitabine. This study aims to elucidate the underlying molecular mechanisms of gemcitabine resistance in PDAC, uncover additional pro-tumorigenic factors contributing to drug resistance, and develop more effective and safer targeted therapeutic strategies against this phenomenon.

Methods

Circular RNA (circRNA) sequencing was employed to identify differentially expressed circRNAs between chemo-sensitive and resistant tumors. Liquid Chromatography-Mass Spectrometry (LC-MS) was utilized to uncover the RNA-binding proteins (RBPs) associated with circular RNA of alpha-1, 3-glucosyltransferase 8 (cALG8). Molecular biology techniques were applied to explore the biological functions and regulatory mechanisms of cALG8 in the context of gemcitabine resistance in PDAC. Single-cell sequencing was performed to reveal changes in the composition of tumor immune microenvironment of pancreatic cancer. Patient-Derived Organoid (PDO) and Patient-Derived Xenograft (PDX) were employed to further validate the molecular mechanisms. Finally, antisense oligonucleotides (ASOs) targeting cALG8 were developed for in vivo use, and their translational therapeutic potential was evaluated in mouse models.

Results

This study identified that cALG8, which is associated with alternative splicing, is highly expressed in gemcitabine-resistant PDAC cells. cALG8 regulates the alternative splicing complex, thereby promoting chemoresistance and immunosuppression in PDAC. Mechanistically, high level of cALG8 functions as a protein scaffold through its 34–85 nt and 109–160 nt regions, creating spatial conditions for CDC-like kinase 1 (CLK1) to phosphorylate serine/arginine-rich splicing factor 7 (SRSF7) at site 231S. This process facilitates the formation of the SRSF7-dependent ataxia-telangiectasia mutated (ATM) kinase variant, ATM203, enhancing the translational efficiency of ATM, and consequently promoting DNA damage repair and immune microenvironment remodeling in PDAC cells to counteract the effects of chemotherapeutic drugs. A cALG8-targeting ASO that disrupts the CLK1-SRSF7 interaction, when combined with gemcitabine and anti-programmed cell death protein (PD)-1 antibody, significantly reduced tumor burden in PDX model, validating its therapeutic translational value.

Conclusion

We demonstrated that the cALG8/CLK1/SRSF7 axis promotes ATM expression by enhancing the splicing of ATM203, thereby facilitating gemcitabine resistance and formation of an immunosuppressive microenvironment in PDAC. This insight aids in the development of drugs targeting chemotherapy resistance induced by DNA damage repair mechanisms in PDAC.
目的胰腺导管腺癌(pancreatic ductal adenocarcinoma, PDAC)的高死亡率主要是由于获得性耐药,尤其是对吉西他滨的耐药。本研究旨在阐明PDAC中吉西他滨耐药的潜在分子机制,揭示导致耐药的其他致瘤因子,并针对这一现象制定更有效、更安全的靶向治疗策略。方法采用环状RNA (circRNA)测序技术鉴定化疗敏感和耐药肿瘤之间表达差异的环状RNA。利用液相色谱-质谱法(LC-MS)揭示了α - 1,3 -葡萄糖基转移酶8 (cALG8)环状RNA相关的RNA结合蛋白(rbp)。应用分子生物学技术探讨cALG8在PDAC耐吉西他滨情况下的生物学功能及调控机制。单细胞测序揭示胰腺癌肿瘤免疫微环境组成的变化。采用患者源性类器官(PDO)和患者源性异种移植(PDX)进一步验证分子机制。最后,开发了靶向cALG8的反义寡核苷酸(ASOs)用于体内应用,并在小鼠模型中评估了它们的转化治疗潜力。结果本研究发现与选择性剪接相关的cALG8在耐吉西他滨PDAC细胞中高表达。cALG8调节选择性剪接复合体,从而促进PDAC的化疗耐药和免疫抑制。从机制上讲,高水平的cALG8通过其34-85 nt和109-160 nt区域作为蛋白质支架,为CLK1在231S位点磷酸化富含丝氨酸/精氨酸的剪接因子7 (SRSF7)创造了空间条件。这一过程促进了srsf7依赖性ataxa -毛细血管扩张突变(ATM)激酶变体ATM203的形成,提高ATM的翻译效率,从而促进PDAC细胞DNA损伤修复和免疫微环境重塑,以抵消化疗药物的作用。当与吉西他滨和抗程序性细胞死亡蛋白(PD)-1抗体联合使用时,一种破坏CLK1-SRSF7相互作用的calg8靶向ASO显著降低了PDX模型中的肿瘤负荷,验证了其治疗转化价值。结论cALG8/CLK1/SRSF7轴通过增强ATM203的剪接促进ATM的表达,从而促进了PDAC的吉西他滨耐药和免疫抑制微环境的形成。这一见解有助于开发针对PDAC中DNA损伤修复机制诱导的化疗耐药的药物。
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引用次数: 0
Emerging role of sialylation in cancer therapy resistance: Mechanisms and therapeutic implications 唾液化在癌症治疗耐药中的新作用:机制和治疗意义
IF 21.7 1区 医学 Q1 PHARMACOLOGY & PHARMACY Pub Date : 2025-11-01 Epub Date: 2025-07-29 DOI: 10.1016/j.drup.2025.101285
Rebecca E. Farrell , Kell A. Stelzer , Guo-Jun Liu , Danielle Skropeta
Resistance to existing cancer therapies is a major factor contributing to cancer's persistence as a global health challenge. Abnormal sialylation patterns, commonly due to changes in the expression of sialyltransferases (STs) is a well-established property of tumour cells. There is a growing body of evidence to demonstrate that sialylation is involved in resistance to chemotherapy, targeted therapy, radiotherapy and immunotherapy through a variety of mechanisms that are still being unveiled. In this review, we summarise the reported correlations between aberrant sialylation and cancer therapy resistance, the underlying mechanisms discovered thus far, and progress made in targeting sialylation to enhance responsiveness to cancer treatment.
对现有癌症疗法的耐药性是导致癌症作为全球健康挑战持续存在的一个主要因素。异常唾液化模式,通常是由于唾液转移酶(STs)表达的改变,是肿瘤细胞的一个公认的特性。越来越多的证据表明,唾液酰化参与了对化疗、靶向治疗、放疗和免疫治疗的耐药性,其机制尚不清楚。在这篇综述中,我们总结了异常唾液化与癌症治疗耐药性之间的相关性,迄今为止发现的潜在机制,以及靶向唾液化以增强癌症治疗反应性的进展。
{"title":"Emerging role of sialylation in cancer therapy resistance: Mechanisms and therapeutic implications","authors":"Rebecca E. Farrell ,&nbsp;Kell A. Stelzer ,&nbsp;Guo-Jun Liu ,&nbsp;Danielle Skropeta","doi":"10.1016/j.drup.2025.101285","DOIUrl":"10.1016/j.drup.2025.101285","url":null,"abstract":"<div><div>Resistance to existing cancer therapies is a major factor contributing to cancer's persistence as a global health challenge. Abnormal sialylation patterns, commonly due to changes in the expression of sialyltransferases (STs) is a well-established property of tumour cells. There is a growing body of evidence to demonstrate that sialylation is involved in resistance to chemotherapy, targeted therapy, radiotherapy and immunotherapy through a variety of mechanisms that are still being unveiled. In this review, we summarise the reported correlations between aberrant sialylation and cancer therapy resistance, the underlying mechanisms discovered thus far, and progress made in targeting sialylation to enhance responsiveness to cancer treatment.</div></div>","PeriodicalId":51022,"journal":{"name":"Drug Resistance Updates","volume":"83 ","pages":"Article 101285"},"PeriodicalIF":21.7,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144781258","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"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
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Drug Resistance Updates
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