JACS Au Pub Date : 2024-08-09 DOI: 10.1021/jacsau.4c00492

Chuan-Ming Dai, Jiaping Xu, Xin Xu, Cong Wang, Tao You, Wei Li, Jiwen Jian

引用次数: 0

An Enzymatic Oxidation Cascade Converts δ-Thiolactone Anthracene to Anthraquinone in the Biosynthesis of Anthraquinone-Fused Enediynes 在蒽醌-融合烯二炔的生物合成过程中，δ-硫内酯蒽向蒽醌的酶促氧化级联转化

JACS Au Pub Date : 2024-08-09 DOI: 10.1021/jacsau.4c00279

Guang-Lei Ma, Wanqiu Liu, Huawei Huang, Xin-Fu Yan, Wei Shen, Surawit Visitsatthawong, Kridsadakorn Prakinee, Hoa Tran, Xiaohui Fan, Yong‐Gui Gao, P. Chaiyen, Jian Li, Zhao-Xun Liang

引用次数: 0

An Aptamer Glue Enables Hyperefficient Targeted Membrane Protein Degradation 一种能实现高效定向膜蛋白降解的 Aptamer 胶水

JACS Au Pub Date : 2024-08-08 DOI: 10.1021/jacsau.4c00260

Guo-Rong Zhang, Chi Zhang, Ting Fu, Weihong Tan, Xueqiang Wang

引用次数: 0

Challenges and Future Perspectives in Photocatalysis: Conclusions from an Interdisciplinary Workshop 光催化技术的挑战与未来展望：跨学科研讨会的结论

JACS Au Pub Date : 2024-08-08 DOI: 10.1021/jacsau.4c00527

Sebastian B. Beil, Sylvestre Bonnet, Carla Casadevall, R. Detz, Fabian Eisenreich, Starla D. Glover, Christoph Kerzig, Line Næsborg, Sonja Pullen, Golo Storch, Ning Wei, Cathleen Zeymer

引用次数: 0

Structure-Based Design of CBP/EP300 Degraders: When Cooperativity Overcomes Affinity 基于结构设计的 CBP/EP300 降解剂：当合作性战胜亲和性时

JACS Au Pub Date : 2024-08-08 DOI: 10.1021/jacsau.4c00292

Iván Cheng-Sánchez, Katherine A. Gosselé, Leonardo Palaferri, E. Laul, Gionata Riccabella, R. K. Bedi, Yaozong Li, Anna Müller, Ivan Corbeski, A. Caflisch, Cristina Nevado

引用次数: 0

Engineering Central Substitutions in Heptamethine Dyes for Improved Fluorophore Performance 在七甲基染料中进行中心取代工程以提高发荧光体的性能

JACS Au Pub Date : 2024-08-07 DOI: 10.1021/jacsau.4c00343

Lei Guo, Meek Yang, Bin Dong, Seth Lewman, Alex Van Horn, Shang Jia

{"title":"Engineering Central Substitutions in Heptamethine Dyes for Improved Fluorophore Performance","authors":"Lei Guo, Meek Yang, Bin Dong, Seth Lewman, Alex Van Horn, Shang Jia","doi":"10.1021/jacsau.4c00343","DOIUrl":"https://doi.org/10.1021/jacsau.4c00343","url":null,"abstract":"As a major family of red-shifted fluorophores that operate beyond visible light, polymethine dyes are pivotal in light-based biological techniques. However, methods for tuning this kind of fluorophores by structural modification remain restricted to bottom-up synthesis and modification using coupling or nucleophilic substitutions. In this study, we introduce a two-step, late-stage functionalization process for heptamethine dyes. This process enables the substitution of the central chlorine atom in the commonly used 4′-chloro heptamethine scaffold with various aryl groups using aryllithium reagents. This method borrows the building block and designs from the xanthene dye community and offers a mild and convenient way for the diversification of heptamethine fluorophores. Notably, this efficient conversion allows for the synthesis of heptamethine-X, the heptamethine scaffold with two ortho-substituents on the 4′-aryl modification, which brings enhanced stability and reduced aggregation to the fluorophore. We showcase the utility of this method by a facile synthesis of a fluorogenic, membrane-localizing fluorophore that outperforms its commercial counterparts with a significantly higher brightness and contrast. Overall, this method establishes the synthetic similarities between polymethine and xanthene fluorophores and provides a versatile and feasible toolbox for future optimizing heptamethine fluorophores for their biological applications.","PeriodicalId":14799,"journal":{"name":"JACS Au","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141946204","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Temperature Effects and Activation Barriers in Aqueous Proton-Uptake Reactions 水质质子吸收反应中的温度效应和活化障碍

JACS Au Pub Date : 2024-08-06 DOI: 10.1021/jacsau.4c00326

Balázs Antalicz, Huib J. Bakker

引用次数: 0

Transition-Metal-Free C-Diarylations to Reach All-Carbon Quaternary Centers 通过无过渡金属 C-二芳基化达到全碳季态中心

JACS Au Pub Date : 2024-08-05 DOI: 10.1021/jacsau.4c00500

Shobhan Mondal, Benjamin Gunschera, Berit Olofsson

引用次数: 0

One-Pot Synthesis of Terminal Alkynes from Alkenes 以烯为原料单锅合成端基炔烃

JACS Au Pub Date : 2024-08-05 DOI: 10.1021/jacsau.4c00599

Cristina Bilanin, Amravati S. Singh, Lluis Martínez-Belenguer, Antonio Leyva-Pérez

引用次数: 0

18F-Fluorination of Nitroimidazolyl-Containing Sultone: A Direct Access to a Highly Hydrophilic Radiotracer for High-Performance Positron Emission Tomography Imaging of Hypoxia 18F-氟化含硝基咪唑的苏丹酮：直接获取高亲水性放射性示踪剂，用于缺氧的高性能正电子发射断层扫描成像

JACS Au Pub Date : 2024-08-02 DOI: 10.1021/jacsau.4c00546

Clémence Maingueneau, Anne-Elodie Lafargue, Stéphane Guillouet, Fabien Fillesoye, Thanh T. Cao Pham, Bénédicte F. Jordan, Cécile Perrio

{"title":"18F-Fluorination of Nitroimidazolyl-Containing Sultone: A Direct Access to a Highly Hydrophilic Radiotracer for High-Performance Positron Emission Tomography Imaging of Hypoxia","authors":"Clémence Maingueneau, Anne-Elodie Lafargue, Stéphane Guillouet, Fabien Fillesoye, Thanh T. Cao Pham, Bénédicte F. Jordan, Cécile Perrio","doi":"10.1021/jacsau.4c00546","DOIUrl":"https://doi.org/10.1021/jacsau.4c00546","url":null,"abstract":"Hypoxia, characterized by nonphysiological levels of oxygen tension, is a key phenomenon common to the majority of malignant tumors with poor prognosis. Many efforts have been made to develop hypoxia imaging for diagnosis, staging, and monitoring of diseases, as well as for evaluating therapies. PET Imaging using 18F-fluoronitroimidazoles (i.e., [18F]FMISO as a lead radiotracer) has demonstrated potential for clinical investigations, but the poor contrast and prolonged acquisition times (>2.5 h) strongly limit its accuracy and routine developments. Here, we report an original [18F]fluoronitroimidazole bearing a sulfo group ([18F]FLUSONIM) that displays highly hydrophilic properties and rapid clearance, providing high-performance hypoxia specific PET imaging. We describe the synthesis and radiosynthesis of [18F]FLUSONIM, its in vivo preclinical evaluation by PET imaging in healthy rats and a rhabdomyosarcoma rat model, as well as its radiometabolization and histological studies. [18F]FLUSONIM was prepared in a single step by high yielding radiofluorination of a sultone precursor, highlighting the advantages of this new radiolabeling approach not yet explored for radiopharmaceutical development. PET imaging experiments were conducted by systematically comparing [18F]FLUSONIM to [18F]FMISO as a reference. The overall results unequivocally demonstrate that the developed radiopharmaceutical meets the criteria of an ideal candidate for hypoxia PET imaging─rapid and efficient radiosynthesis, total stability, exclusive urinary elimination, high specificity for hypoxic regions, unprecedented tumor/background ratios, short acquisition delays (<60 min), and promising potential for further preclinical and clinical applications.","PeriodicalId":14799,"journal":{"name":"JACS Au","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-08-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141881701","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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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