Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2025-02-20DOI: 10.1021/acs.bioconjchem.4c00540
Maria Nerantzaki, Claire Husser, Isaure Sergent, Laurence Charles, Jean-François Lutz, Michael Ryckelynck
{"title":"Chemical Synthesis and Poly(ethylene glycol)-Like Conjugation of the Mango-II Fluorogenic RNA Aptamer.","authors":"Maria Nerantzaki, Claire Husser, Isaure Sergent, Laurence Charles, Jean-François Lutz, Michael Ryckelynck","doi":"10.1021/acs.bioconjchem.4c00540","DOIUrl":"10.1021/acs.bioconjchem.4c00540","url":null,"abstract":"<p><p>A reliable method for the efficient chemical synthesis and poly(ethylene glycol) PEG-like modification of fluorogenic RNA aptamers is reported. The 43-mer version of Mango-II RNA (MangoII-v1), which binds tightly and specifically to the green fluorophore TO1-Biotin (TO1-B), was synthesized by automated phosphoramidite chemistry using 2'-<i>O</i>-[(triisopropylsilyl)oxy]methyl] (2'-<i>O</i>-TOM)-protected ribonucleosides. Solid-phase phosphoramidite chemistry was also used as a single tool to prepare MangoII-v1 modified with a PEG-like oligophosphate synthetic segment (MangoII-v1-<b>P</b>). After cleavage from the resin, deprotection, and purification, the capacity to activate the fluorescence of TO1-B and the degradation behavior of the chemically synthesized RNAs MangoII-v1 and MangoII-v1-<b>P</b>, were deeply investigated in comparison with those of the enzymatically synthesized 48 nucleotides long RNA MangoII. Interestingly, the chemically synthesized MangoII-v1 RNA aptamer demonstrated great activity toward its target, compared to the enzymatically synthesized analogue. Moreover, it was found to be highly stable, retaining its structural integrity and bioactivity, even after seven days of incubation in 20% fetal bovine serum. MangoII-v1-<b>P</b> also showed a high affinity for TO1-B and excellent degradation resistance.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"449-456"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143466422","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2025-02-20DOI: 10.1021/acs.bioconjchem.5c00041
Jing Wang, Chengxue He, Rui Guo, Li Wen, Jinping Tao, Huimao Zhang, HaiFeng Huang, Hua Zhu, Zhi Yang, Xianteng Yang
{"title":"[<sup>177</sup>Lu]Lu-XYIMSR-01: A Novel CAIX-Targeted Radiotherapeutic for Enhanced Treatment of Malignant Glioma.","authors":"Jing Wang, Chengxue He, Rui Guo, Li Wen, Jinping Tao, Huimao Zhang, HaiFeng Huang, Hua Zhu, Zhi Yang, Xianteng Yang","doi":"10.1021/acs.bioconjchem.5c00041","DOIUrl":"10.1021/acs.bioconjchem.5c00041","url":null,"abstract":"<p><p>Malignant glioma highly expresses carbonic anhydrase IX (CAIX). This study aimed to develop [<sup>177</sup>Lu]Lu-XYIMSR-01, a small-molecule therapeutic agent CAIX, to assess its potential for treating malignant glioma. [<sup>177</sup>Lu]Lu-XYIMSR-01 was synthesized by radiolabeling DOTA-XYIMSR-01 with <sup>177</sup>Lu. In vitro assays were conducted to evaluate the affinity for U87MG tumor cells. The probe was injected via the tail vein into subcutaneous and orthotopic U87MG models for micro-SPECT/CT imaging. The survival rates of tumor-bearing mice were assessed after [<sup>177</sup>Lu]Lu-XYIMSR-01 injection by intratumoral in orthotopic models, including untreated controls and those treated with Temozolomide or combination therapy. After purification, the radiochemical yield of [<sup>177</sup>Lu]Lu-XYIMSR-01 was 86.47 ± 2.42%, with a radiochemical purity (RCP) of 99%. Its cell uptake in U87MG cells was 3.70 ± 0.57 ‰ AD/10<sup>5</sup> cells, significantly higher than that in HCT116 cells (0.68 ± 0.16 ‰ AD/10<sup>5</sup> cells, <i>P</i> = 0.001). In the biodistribution study, [<sup>177</sup>Lu]Lu-XYIMSR-01 uptake in U87MG tumors was 6.19 ± 1.37%ID/g, with a tumor/muscle ratio of 20.14 ± 3.24. In the orthotopic glioma model, local injection combined with Temozolomide significantly improved survival and inhibited tumor growth. The results indicate that [<sup>177</sup>Lu]Lu-XYIMSR-01 is a promising therapeutic molecular probe for targeting CAIX, and its combination with Temozolomide significantly enhances treatment outcomes for malignant glioma.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"588-596"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143466677","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2025-02-24DOI: 10.1021/acs.bioconjchem.4c00559
Marc García-Trujillo, Jesús Lavado-García, Arnau Boix-Besora, Francesc Gòdia, Laura Cervera
{"title":"Gag HIV-1 Virus-like Particles and Extracellular Vesicles Functionalization with Spike Epitopes of SARS-CoV-2 Using a Copper-Free Click Chemistry Approach.","authors":"Marc García-Trujillo, Jesús Lavado-García, Arnau Boix-Besora, Francesc Gòdia, Laura Cervera","doi":"10.1021/acs.bioconjchem.4c00559","DOIUrl":"10.1021/acs.bioconjchem.4c00559","url":null,"abstract":"<p><p>Enveloped nanoparticles such as extracellular vesicles (EVs) and virus-like particles (VLPs) have emerged as promising nanocarriers capable of transporting bioactive molecules for drug delivery and vaccination. Optimized functionalization methodologies are required to increase the functionalization levels of these nanoparticles, enhancing their performance. Here, a bioorthogonal copper-free strain-promoted azide-alkyne cycloaddition (SPAAC) reaction has been optimized to functionalize human immunodeficiency virus type 1 (HIV-1) Gag-based VLPs and EVs. The optimization process has been carried out through reaction kinetics and design of experiments (DoE) using Cy5 as a reporter molecule. The functionalization of both VLPs and EVs has been studied using super-resolution fluorescence microscopy (SRFM), revealing remarkable differences between Gag-VLPs and coproduced EVs. EVs produced by mock transfection and cell growth have been functionalized achieving a mean of 3618.63 ± 48.91 and 6498.75 ± 352.71 Cy5 molecules covalently linked per particle (Cy5<sub>cov</sub>/particle), respectively. Different nanoparticles have been functionalized with two linear B-cell epitopes from the Spike protein of SARS-CoV-2, S<sub>315-338</sub> TSNFRVQPTESIVRFPNITNLCPF and S<sub>648-663</sub> GCLIGAEHVNNSYECD, and analyzed by an immunoassay with sera from COVID-19 patients. The obtained results validate the selected B-cell epitopes and highlight the potential of the optimized functionalization approach for the development of nanoparticle-based vaccines.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"486-499"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143490303","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"FeOOH-Assisted Formation of Hybrid Polymer Nanospindles for Efficient Iron Delivery and Ferroptosis Tumor Therapy.","authors":"Heng Liu, Lu Wang, Hao Jin, Kepeng Tao, Xuanqi Zhu, Mengsi Zhang, Yuchuan Hou, Shuwei Liu, Hao Zhang","doi":"10.1021/acs.bioconjchem.4c00546","DOIUrl":"10.1021/acs.bioconjchem.4c00546","url":null,"abstract":"<p><p>Exogenous iron delivery using iron-containing nanomaterials is an alternative strategy for enhancing the efficacy in ferroptosis tumor therapy but limited by the problems of low iron content, low tumor enrichment, low cellular uptake, and uncontrolled release of iron ions. To solve the problems, an FeOOH-assisted approach is demonstrated to produce iron hybrid polymer nanospindles (IHPNSs) for efficient iron delivery and ferroptosis tumor therapy. The IHPNSs are prepared through the cohydrolysis of FeCl<sub>3</sub>·6H<sub>2</sub>O with aniline, pyrrole, or amino-pyrrole. On the one hand, the hydrolysis of Fe<sup>3+</sup> generates FeOOH particles, which further act as the templates to form fusiform architectures. On the other hand, Fe<sup>3+</sup> triggers the oxidative polymerization of aniline, pyrrole, or amino-pyrrole. The as-prepared polymers are capable of coordinating with excessive Fe<sup>3+</sup> and locate on the FeOOH templates, thus producing Fe<sup>3+</sup>/polymer composite-coated FeOOH nanospindles. Systematic studies indicate that the one-dimension-like morphology facilitates tumor enrichment and cellular uptake of IHPNSs. Besides the high iron content of IHPNSs, the controlled release of Fe<sup>3+</sup> stimulated by the overexpressed glutathione (GSH) in the tumor microenvironment is achieved. The released Fe<sup>3+</sup> is further transformed to Fe<sup>2+</sup> by scavenging GSH, which leads to excessive accumulation of reactive oxygen species and lipid peroxides and finally induces ferroptosis of tumor cells. As a proof of concept, the IHPNSs show good efficacy in the treatment of a rat model of bladder tumors in situ.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"464-475"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143565615","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Taeyeol Youn, Ganghee Kim, Parameswaran Hariharan, Xianglan Li, Waqar Ahmed, Bernadette Byrne, Xiangyu Liu, Lan Guan, Pil Seok Chae
{"title":"Improved Pendant-Bearing Glucose-Neopentyl Glycols for Membrane Protein Stability.","authors":"Taeyeol Youn, Ganghee Kim, Parameswaran Hariharan, Xianglan Li, Waqar Ahmed, Bernadette Byrne, Xiangyu Liu, Lan Guan, Pil Seok Chae","doi":"10.1021/acs.bioconjchem.4c00556","DOIUrl":"https://doi.org/10.1021/acs.bioconjchem.4c00556","url":null,"abstract":"<p><p>Membrane proteins are biologically and pharmaceutically significant, and determining their 3D structures requires a membrane-mimetic system to maintain protein stability. Detergent micelles are widely used as membrane mimetics; however, their dynamic structures often lead to the denaturation and aggregation of encapsulated membrane proteins. To address the limitations of classical detergents in stabilizing membrane proteins, we previously reported a class of glucose-neopentyl glycols (GNGs) and their pendant-bearing versions (P-GNGs), several of which proved more effective than DDM in stabilizing membrane proteins. In this study, we synthesized additional GNG derivatives by varying the lengths of the pendant (P-GNGs), and by introducing hemifluorinated pendants to the GNG scaffold (fluorinated pendant-bearing GNGs or FP-GNGs). The synthetic flexibility of the GNG chemical architecture allowed us to create a diverse range of derivatives, essential for the effective optimization of detergent properties. When tested with two model membrane proteins (a transporter and a G-protein coupled receptor (GPCR)), most of the new (F)P-GNGs demonstrated superior stabilization of these membrane proteins compared to DDM, the original GNG (OGNG)), and a previously developed P-GNG (i.e., GNG-3,14). Notably, several P-GNGs synthesized in this study were as effective as or even better than lauryl maltose neopentyl glycol (LMNG) in stabilizing a human GPCR, beta2 adrenergic receptor (β2AR). Enhanced protein stability was particularly observed for the P-GNGs with a butyl (C4) or pentyl (C5) pendant, indicating that these pendant sizes are optimal for membrane protein stability. The volumes of these pendants appear to minimize the empty spaces in the micelle interiors, thereby enhancing detergent-detergent interactions in micelles complexed with the membrane proteins. Additionally, we identified one FP-GNG that was more efficient at extracting the transporter and more effective at stabilizing the GPCR than DDM. Thus, the current study demonstrates that both chain length and number of fluorine atoms in the pendants of the P-GNGs were crucial determinants for membrane protein stability. We not only developed a few (F)P-GNGs that are significantly more effective than maltoside detergents (LMNG/DDM) for protein extraction and stability but we also provided an effective strategy for detergent design through the utilization of partially fluorinated pendants of varying length.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":""},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143655463","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2025-02-25DOI: 10.1021/acs.bioconjchem.5c00028
Amy E Laturski, Maria T Dulay, Jillian L Perry, Joseph M DeSimone
{"title":"Transfection via RNA-Based Nanoparticles: Comparing Encapsulation vs Adsorption Approaches of RNA Incorporation.","authors":"Amy E Laturski, Maria T Dulay, Jillian L Perry, Joseph M DeSimone","doi":"10.1021/acs.bioconjchem.5c00028","DOIUrl":"10.1021/acs.bioconjchem.5c00028","url":null,"abstract":"<p><p>Historically, RNA delivery via nanoparticles has primarily relied on encapsulation, as demonstrated by lipid nanoparticles in SARS-CoV-2 vaccines. Concerns about RNA degradation on nanoparticle surfaces initially limited the exploration of adsorption-based approaches. However, recent advancements have renewed interest in adsorption as a viable alternative. This Viewpoint explores the approaches of RNA incorporation in nanoparticles, comparing encapsulation, adsorption, and the combination of encapsulation and adsorption, and presents a framework to guide the selection of the most suitable strategy based on general characteristics.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"367-376"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143497498","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2025-02-26DOI: 10.1021/acs.bioconjchem.5c00019
Jiale Si, Cheng Li, Xin Chen, Qinghao Zhou, Yueming Xue, Yuanyuan Ji, Yansong Dong, Zhishen Ge
{"title":"A Near-Infrared Fluorescent Macromolecular Dye for Precise Identification of Glioblastoma Boundaries.","authors":"Jiale Si, Cheng Li, Xin Chen, Qinghao Zhou, Yueming Xue, Yuanyuan Ji, Yansong Dong, Zhishen Ge","doi":"10.1021/acs.bioconjchem.5c00019","DOIUrl":"10.1021/acs.bioconjchem.5c00019","url":null,"abstract":"<p><p>Glioblastoma (GBM) is a highly invasive tumor with poorly defined boundaries, often leaving residual tissue after surgery, which contributes to the recurrence and poor prognosis. A critical challenge in GBM treatment is the precise identification of tumor boundaries during surgery to achieve a safe and complete resection. In this study, we present a novel near-infrared fluorescent agent, IR-PEG-cRGD, that is designed to accurately delineate GBM boundaries for surgical navigation of tumor resection. IR-PEG-cRGD is successfully prepared from the cyanine dye IR-820, which is conjugated to poly(ethylene glycol) (PEG) to prolong circulation time and enhance tumor accumulation. Additionally, a glioma-targeting peptide (cRGD, cyclo(Arg-Gly-Asp-d-Phe-Cys)) is conjugated to PEG to selectively target GBM. IR-PEG-cRGD demonstrates effective targeting and enrichment in subcutaneous human-derived GBM mice models, enabling specific distinguishing of the GBM margin from the surrounding parenchyma with a high signal-to-background ratio (SBR) of 4.79. Moreover, IR-PEG-cRGD can pass across the blood-brain barrier (BBB) efficiently. These findings indicate that IR-PEG-cRGD can serve as a valuable tool for the precise intraoperative delineation of GBM boundaries, aiding in safe and complete tumor resection.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"578-587"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143497485","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Lipid Nanocarriers as Precision Delivery Systems for Brain Tumors.","authors":"Roshan Keshari, Mahima Dewani, Navneet Kaur, Girijesh Kumar Patel, Sumit Kumar Singh, Pranjal Chandra, Rajendra Prasad, Rohit Srivastava","doi":"10.1021/acs.bioconjchem.5c00007","DOIUrl":"10.1021/acs.bioconjchem.5c00007","url":null,"abstract":"<p><p>Brain tumors, particularly glioblastomas, represent the most complicated cancers to treat and manage due to their highly invasive nature and the protective barriers of the brain, including the blood-brain barrier (BBB). The efficacy of currently available treatments, viz., radiotherapy, chemotherapy, and immunotherapy, are frequently limited by major side effects, drug resistance, and restricted drug penetration into the brain. Lipid nanoparticles (LNPs) have emerged as a promising and targeted delivery system for brain tumors. Lipid nanocarriers have gained tremendous attention for brain tumor therapeutics due to multiple drug encapsulation abilities, controlled release, better biocompatibility, and ability to cross the BBB. Herein, a detailed analysis of the design, mechanisms, and therapeutic benefits of LNPs in brain tumor treatment is discussed. Moreover, we also discuss the safety issues and clinical developments of LNPs and their current and future challenges. Further, we also focused on the clinical transformation of LNPs in brain tumor therapy by eliminating side effects and engineering the LNPs to overcome the related biological barriers, which provide personalized, affordable, and low-risk treatment options.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"347-366"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143404895","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2025-03-10DOI: 10.1021/acs.bioconjchem.4c00561
Sonia Boga, David Bouzada, Roi Lopez-Blanco, Axel Sarmiento, Iria Salvadó, David Alvar Gil, José Brea, María Isabel Loza, Natalia Barreiro-Piñeiro, José Martínez-Costas, Silvia Mena, Gonzalo Guirado, Alice Santoro, Peter Faller, M Eugenio Vázquez, Miguel Vázquez López
{"title":"Copper(II) Cyclopeptides with High ROS-Mediated Cytotoxicity.","authors":"Sonia Boga, David Bouzada, Roi Lopez-Blanco, Axel Sarmiento, Iria Salvadó, David Alvar Gil, José Brea, María Isabel Loza, Natalia Barreiro-Piñeiro, José Martínez-Costas, Silvia Mena, Gonzalo Guirado, Alice Santoro, Peter Faller, M Eugenio Vázquez, Miguel Vázquez López","doi":"10.1021/acs.bioconjchem.4c00561","DOIUrl":"10.1021/acs.bioconjchem.4c00561","url":null,"abstract":"<p><p>Cu(II) coordination complexes are emerging as promising anticancer agents due to their ability to induce oxidative stress through reactive oxygen species (ROS) generation. In this study, we synthesized and characterized two novel Cu(II) metallopeptide systems, <b>1</b>/Cu(II) and <b>2</b>/Cu(II), derived from the oligocationic bipyridyl cyclopeptides <b>1</b> and <b>2,</b> and designed to enhance the transport of Cu(II) into cells and increase ROS levels. Spectroscopic and electrochemical analyses confirmed the formation of stable metallopeptide species in aqueous media. Inductively coupled plasma mass spectrometry (ICP-MS) studies demonstrated that both metallopeptides significantly increase intracellular Cu(II) accumulation in NCI/ADR-RES cancer cells, highlighting their role as efficient Cu(II) transporters. Additionally, ROS generation assays revealed that <b>1</b>/Cu(II) induces a substantial increase in intracellular ROS levels, supporting the hypothesis of oxidative stress-induced cytotoxicity. Cell-viability assays further confirmed that both <b>1</b>/Cu(II) and <b>2</b>/Cu(II) exhibit strong anticancer activity in a number of cancer cell lines, with IC<sub>50</sub> values significantly lower than those of their free cyclopeptide counterparts or Cu(II) alone, showing an order of activity higher than that of cisplatin. Finally, molecular modeling studies provided further insights into the structural stability and coordination environment of Cu(II) within the metallopeptide complexes. These findings suggest that these Cu(II) cyclometallopeptide systems hold potential as novel metal-based therapeutic agents, leveraging Cu(II) transport and ROS increase as key strategies for cancer treatment.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"500-509"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143583932","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bioconjugate ChemistryPub Date : 2025-03-19Epub Date: 2024-12-31DOI: 10.1021/acs.bioconjchem.4c00483
Seungyoon Kang, Gyung A Kim, Myo Naing Win, Yeongcheol Ki, Hohjai Lee, Min Su Han
{"title":"Fluorescence-Based Simple and Practical Assay Method for DNA Damage Analysis in DNA-Encoded Library Synthesis.","authors":"Seungyoon Kang, Gyung A Kim, Myo Naing Win, Yeongcheol Ki, Hohjai Lee, Min Su Han","doi":"10.1021/acs.bioconjchem.4c00483","DOIUrl":"10.1021/acs.bioconjchem.4c00483","url":null,"abstract":"<p><p>The dsDNA-selective fluorescent-dye-based DNA damage assay was developed for DNA-encoded library (DEL) synthesis. For the various DEL synthesis conditions, the assay was validated through cross-checking with high-performance liquid chromatography (HPLC) analysis, and the fact was confirmed that the usage of a specific ratio of organic solvent can critically induce DNA damage. Also, the applicability of the assay was confirmed through the screening of the DNA-damaging condition of the on-DNA amide coupling reaction and Pd-catalyzed on-DNA <i>N</i>-arylation reaction.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"395-400"},"PeriodicalIF":4.0,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142908733","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}