Bioconjugate Chemistry最新文献

{"title":"","authors":"","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/bcv036i007_1959891","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631027","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"","authors":"Qi Cao, Xiao Wu, Juan Tan, Hanying Xu, Ying Zhang, Yang Hu, Yuxi Chen, Shiyong Zhang and Tian Tang*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acs.bioconjchem.5c00256","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"","authors":"Shuang-Shuang Long*, Xi-Feng Zou, Wen-Xi Zhang, Ke Zeng, Qing-Long Qiao*, Xu-Dong Jiang* and Ying-Wu Lin*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acs.bioconjchem.5c00092","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631036","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"","authors":"Liam Connah, Danijela Bataveljić, Aleksandra M. Bondžić, Lucía Cabrera Fernández De Henestrosa, Andrej Korenić, Bojan P. Bondžić, Pavle Andjus and Goran Angelovski*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acs.bioconjchem.5c00005","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631034","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and Application of Conjugatable Small Molecule Toll-Like Receptor 4 Ligands.","authors":"Yutaro Mahara, Issa Fukuda, Ryuho Tanaka, Shin-Ya Oyama, Hiroyuki Shinchi, Yasuo Suda, Nikunj M Shukla, Michael Chan, Tomoko Hayashi, Howard B Cottam, Dennis A Carson, Masahiro Wakao","doi":"10.1021/acs.bioconjchem.5c00076","DOIUrl":"10.1021/acs.bioconjchem.5c00076","url":null,"abstract":"<p><p>We identified structurally distinct pyrimido[5,4-<i>b</i>]indole derivatives as toll-like receptor 4 (TLR4) ligands. Previous structure-activity relationship studies revealed that C8-aryl derivatives in pyrimido[5,4-<i>b</i>]indole, especially phenyl and 2-naphthyl compounds, are more potent in the activation of TLR4 signaling. Molecular modeling of these compounds indicated that C8-aryl groups are important for the interaction of the TLR4/myeloid differentiation factor-2 (MD-2) complex. Additionally, the modeling suggested that the N5 position in pyrimido[5,4-<i>b</i>]indole could be used as a further modification site to develop various drug conjugates. In this study, we examined whether the N5 position in pyrimido[5,4-<i>b</i>]indole can be used for conjugation without losing potency. Since tetraethylene glycol (TEG) derivatives at the N5 position were predicted to bind to TLR4/MD-2 complex using in silico molecular docking analysis, the compounds with the TEG group at the N5 position were synthesized and evaluated for immunostimulatory activity by human TLR4 reporter cell assay. As a result of fine-tuning of the C8 substitution groups, we found that TLR4 ligand (TLR4L) <b>10</b> with a 3-thienylethynyl group at the C8 position maintained TLR4 potency and demonstrated agonistic activity in primary murine bone marrow dendritic cells (mBMDC) and human TLR4 reporter HEK-Blue cells. TLR4L <b>10</b> was conjugated to sugar-immobilized gold nanoparticles (SGNPs) by introducing thioctic acid as a spacer into the TEG moiety. The obtained TLR4L-SGNPs <b>17</b> were taken up and showed agonistic activity in mBMDC. Thus, our designed TLR4L <b>10</b> and TLR4L-SGNP <b>17</b> are new candidates as immunomodulators for novel class adjuvant systems.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"1409-1420"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144323842","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":"Multicheckpoint Cellular Targeting of siRNAs Using Antibody-Directed Lipid-Polymer Hybrid Nanoparticles.","authors":"Ritam Das, Jewel Medeiros, Jithu Krishna, Sriya Munugoti, Ranit Dutta, Anirudh Devarajan, Arpan Ghosh, S Thayumanavan","doi":"10.1021/acs.bioconjchem.5c00205","DOIUrl":"10.1021/acs.bioconjchem.5c00205","url":null,"abstract":"<p><p>Despite advancements in tissue-specific gene therapy, current technologies struggle to target organs beyond the liver, spleen, and lungs. Passive approaches such as selective organ targeting (SORT) lipids show potential but require time-intensive optimization. Active targeting, exemplified by antibody-drug conjugates (ADCs), offers a modular and effective alternative. Building on this, we developed antibody-functionalized hybrid lipid-polymer nanoparticles for siRNA delivery, targeting cancer-overexpressed receptors such as EGFR and TROP2, prevalent in aggressive cancers like triple-negative breast cancer (TNBC). In addition, to enhance therapeutic safety and efficacy, we integrated multi-siRNA delivery into a multicheckpoint targeting strategy, minimizing reliance on single antigens and reducing off-target risks. Using TNBC cells as a model, this platform demonstrates potential for developing a robust and safe therapeutic approach. In this article, we present our findings that lay the foundation for developing a multicheckpoint strategy to enhance target selectivity in nanomedicine.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"1527-1540"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144558422","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":"","authors":"G. G. Simpson,&nbsp;J. M. Quintana,&nbsp;J. E. Carrothers,&nbsp;F. Jiang,&nbsp;S. A. Walker,&nbsp;C. Cho,&nbsp;R. Weissleder,&nbsp;M. A. Miller and T. S. C. Ng*,&nbsp;","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acs.bioconjchem.5c00139","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631026","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"","authors":"Junya Michibata,&nbsp;Yoshimasa Kawaguchi,&nbsp;Yusei Furuyama,&nbsp;Yoshihiro Sasaki,&nbsp;Kazunari Akiyoshi and Shiroh Futaki*,&nbsp;","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acs.bioconjchem.5c00176","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631038","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preclinical Evaluation of an Integrin α_vβ₆-Targeted Photodynamic Therapy.","authors":"Hua Zhang, Tanushree Ganguly, Rebecca Harris, Ryan A Davis, Sven H Hausner, Luciana Kovacs, Julie L Sutcliffe","doi":"10.1021/acs.bioconjchem.5c00202","DOIUrl":"10.1021/acs.bioconjchem.5c00202","url":null,"abstract":"<p><p>Photodynamic therapy (PDT) is a minimally invasive treatment in which an external light source activates an injected photosensitizer (PS) to generate reactive oxygen species, causing localized cell death. Although the first PDT received FDA approval in 1995, clinical adoption has been limited, in part due to the limited tumor selectivity of PSs. The goal of this study was to develop a PS with improved tumor selectivity by incorporating a targeting peptide that selectively binds to the integrin α_vβ₆. The integrin α_vβ₆ is an epithelial-specific cell-surface receptor that is overexpressed in several cancer types, with expression level often linked to poor overall survival. The integrin α_vβ₆ targeting peptide (ABM-5G) was conjugated onto a water-soluble PS (IRDye700DX, IR700) in solution phase, and the resulting PS-α_vβ₆-targeted-peptide conjugate (IR700-ABM-5G, <b>1</b>) demonstrated excellent photochemical and photophysical properties, including high extinction coefficient and singlet oxygen productivity similar to the nontargeted PS (free IR700). <i>In vitro,</i> <b>1</b> showed α_vβ₆-selective binding to and internalization into DX3puroβ6 (α_vβ₆+) cells vs DX3puro (α_vβ₆-) cells, and α_vβ₆-selective phototoxicity with EC₅₀s of 1.6 nM for DX3puroβ6 cells and ≥ 250 nM for DX3puro cells. In mice bearing paired DX3puroβ6 (α_vβ₆+) and DX3puro (α_vβ₆-) tumor xenografts, the fluorescence intensity of <b>1</b> in DX3puroβ6 (α_vβ₆+) tumors was 2.5- to 7-fold higher than that of the other tissues (including DX3puro (α_vβ₆-) tumors, <i>p</i> < 0.0001), except for the kidneys and stomach. A single treatment of <b>1</b> (1.4 nmol per mouse) combined with near-infrared light exposure significantly suppressed the growth of DX3puroβ6 (α_vβ₆+) tumors (198 ± 112 mm³ vs 714 ± 251 mm³ for saline control, <i>p</i> < 0.0001, on day 37 post treatment). In summary, PDT treatment with <b>1</b> demonstrated α_vβ₆-selective therapeutic efficacy both <i>in vitro</i> and <i>in vivo</i> and is a promising targeted therapy for the treatment of a range of α_vβ₆-expressing cancers.</p>","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"1516-1526"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12272554/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144281678","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"","authors":"Andrew S. Browne,&nbsp;Jieqiong Fang,&nbsp;Amany Elsharkawy,&nbsp;Tianwei Jia,&nbsp;Evan Reboli,&nbsp;Ying Luo,&nbsp;Xiaolin Sheng,&nbsp;Mukesh Kumar* and Suri S. Iyer*,&nbsp;","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":"36 7","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":4.0,"publicationDate":"2025-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acs.bioconjchem.5c00153","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144631030","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}