Chemistry - A European Journal最新文献_第2页

Negative cooperativity in the UHRF1 TTD-PHD dual domain masks the contributions of cation-π interactions between trimethyllysine and the TTD aromatic cage. UHRF1 TTD- phd双结构域的负协同性掩盖了三甲基赖氨酸与TTD芳香笼间阳离子-π相互作用的贡献。

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202500848

Christopher R Travis, Jake R Wilkinson, Ryan G Dumais, Hanne C Henriksen, Joseph W Treacy, Noah K Schomburg, K N Houk, Marcey L Waters

{"title":"Negative cooperativity in the UHRF1 TTD-PHD dual domain masks the contributions of cation-π interactions between trimethyllysine and the TTD aromatic cage.","authors":"Christopher R Travis, Jake R Wilkinson, Ryan G Dumais, Hanne C Henriksen, Joseph W Treacy, Noah K Schomburg, K N Houk, Marcey L Waters","doi":"10.1002/chem.202500848","DOIUrl":"https://doi.org/10.1002/chem.202500848","url":null,"abstract":"UHRF1 is a promising epigenetic target in oncology, but inhibitor development has proven challenging due to the interplay between its tandem Tudor domain (TTD) and plant homeodomain (PHD). The TTD binds trimethyllysine (Kme3) at position 9 while the PHD binds Arg at position 2 on histone 3. Herein, we report how the PHD influences TTD recognition of the histone 3 tail containing Kme3 (H3K9me3) versus its neutral isostere, tert-butyl norleucine (tBuNle). Our findings show that the dual domain binds both peptides equally, supporting tBuNle's potential for inhibitor development. However, unexpectedly, the binding mechanism of H3K9me3 differs between the single and dual domains. In the TTD alone, Kme3 is bound in the aromatic cage via electrostatically tunable cation-π interactions, but in the dual domain, Kme3 binding is independent of electrostatics in the aromatic cage-an unprecedented observation. Computational studies suggest cation-π interactions should contribute in both cases. The contrasting experimental and computational results point to an unusual example of negative chelate cooperativity: interactions between the histone and PHD mask the mechanism of TTD recognition of K9me3. This work underscores the complexity of histone PTM readout in multi-domain proteins and demonstrates the first example of a masked cation-π interaction.","PeriodicalId":144,"journal":{"name":"Chemistry - A European Journal","volume":" ","pages":"e202500848"},"PeriodicalIF":3.9,"publicationDate":"2025-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810288","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}

引用次数: 0

Spatial Confinement of Pd Nanoclusters in Pyrene-Based Covalent Organic Frameworks for Boosting Photocatalytic CO2 Reduction. 芘基共价有机骨架中钯纳米团簇的空间限制促进光催化CO2还原。

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202500766

Yuling Lin, Xiaofang Lai, Guiting Huang, Jianhui Luo, Qiaoshan Chen, Guocheng Huang, Jinhong Bi

{"title":"Spatial Confinement of Pd Nanoclusters in Pyrene-Based Covalent Organic Frameworks for Boosting Photocatalytic CO2 Reduction.","authors":"Yuling Lin, Xiaofang Lai, Guiting Huang, Jianhui Luo, Qiaoshan Chen, Guocheng Huang, Jinhong Bi","doi":"10.1002/chem.202500766","DOIUrl":"https://doi.org/10.1002/chem.202500766","url":null,"abstract":"Photocatalytic CO2 reduction offers a promising strategy to mitigate the greenhouse effect, yet it remains a challenging process due to the high energy barrier associated with the high stability of CO2. In this study, we synthesized Py-bTDC, a pyrene-based covalent organic framework (COF) enriched with nitrogen and sulfur atoms, and anchored palladium nanoclusters (Pd NCs) onto its structure to enhance CO2 reduction efficiency. The confined Pd NCs amplify the built-in electric field (IEF), enabling efficient photogenerated carrier migration and suppressing electron-hole recombination. Simultaneously, Pd NCs serve as catalytic active sites, optimizing CO2 adsorption and activation. Density functional theory (DFT) calculations reveal that Pd reduces the energy barrier for forming the critical intermediate (*COOH), thereby accelerating CO production. Under visible-light irradiation in a gas-solid system using water as a proton donor, the Pd3/Py-bTDC composite achieved a CO evolution rate of 17.75 μmol·h-1·g-1 with 86.0% selectivity. This study advances the design of COF-based photocatalysts by synergistically modulating IEF and the engineering active sites for efficient CO2 reduction.","PeriodicalId":144,"journal":{"name":"Chemistry - A European Journal","volume":" ","pages":"e202500766"},"PeriodicalIF":3.9,"publicationDate":"2025-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810324","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}

引用次数: 0

Cover Feature: Technetium and Rhenium Auto-reduction, Polymerization and Lability towards Group VII Polyoxometalate Chemistry (Chem. Eur. J. 21/2025) 封面特征：锝和铼的自动还原，聚合和对第七族多金属氧酸盐化学的不稳定性。欧元。j . 21/2025)

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202582104

Jenna Bustos, Dr. Mohammad Shohel, Dr. Ana Guilherme Buzanich, Dr. Lev Zakharov, Jordi Buils, Mireia Segado-Centellas, Dr. Carles Bo, Dr. May Nyman

引用次数: 0

Design and Evaluation of Bivalent K-Ras Inhibitors that Target the CAAX Binding Site and the Acidic Surface of Farnesyltransferase and Geranylgeranyltransferase I. 靶向法尼基转移酶和香叶基转移酶酸性表面和CAAX结合位点的二价K-Ras抑制剂的设计与评价

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202500306

Junko Ohkanda, Naomi Horiuchi, Rania Omer, Fumitoshi Sugino, Naomi Ogino, Yoshihisa Inoue, Kazi Aslamuzzaman, Takeyuki Suzuki, Said Sebti

{"title":"Design and Evaluation of Bivalent K-Ras Inhibitors that Target the CAAX Binding Site and the Acidic Surface of Farnesyltransferase and Geranylgeranyltransferase I.","authors":"Junko Ohkanda, Naomi Horiuchi, Rania Omer, Fumitoshi Sugino, Naomi Ogino, Yoshihisa Inoue, Kazi Aslamuzzaman, Takeyuki Suzuki, Said Sebti","doi":"10.1002/chem.202500306","DOIUrl":"https://doi.org/10.1002/chem.202500306","url":null,"abstract":"Mutant K-Ras drives cancer through its membrane localization, which requires post-translational modification by farnesyltransferase (FTase). FTase attaches farnesyl to the K-Ras C-terminal CVIM tetrapeptide, enabling membrane binding. However, K-Ras can also undergo compensatory geranylgeranylation by geranylgeranyltransferase I (GGTase I), making FTase inhibition alone ineffective. Dual inhibition of FTase and GGTase I is necessary to fully block K-Ras localization and its cancer activity. We developed bivalent inhibitors targeting both FTase and GGTase I by binding to the CVIM site and an adjacent acidic surface. A non-thiol CVIM peptidomimetic based on a piperidine scaffold showed potent FTase inhibition (Ki = 2.1 nM) with less effect on GGTase I (Ki = 210 nM). Adding cationic modules to this compound produced dual inhibitors with enhanced potency (Ki = 2-5 nM), significantly improving upon previous agents. These bivalent inhibitors effectively reduced mutant K-Ras cancer cell viability and inhibited K-Ras farnesylation and geranylgeranylation in cells. This dual-targeting approach shows promise for treating K-Ras-driven cancers.","PeriodicalId":144,"journal":{"name":"Chemistry - A European Journal","volume":" ","pages":"e202500306"},"PeriodicalIF":3.9,"publicationDate":"2025-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810280","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}

引用次数: 0

Visible-Light-Promoted Radical Cascade Bicyclization to Access Partially Saturated Pyrrolo[2,3-b]pyridines. 可见光促进自由基级联双联反应制备部分饱和吡咯[2,3-b]吡啶。

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202500787

Guangpeng Yan, Chengyi Jiang, Shangyu Mao, Ting Zou, Siping Wei, Huirong Xia, Bin Chen, Yao Jian, Dong Yi, Ying Xiong

引用次数: 0

Cover Feature: Amino-Substituted Azoxybenzenes as Potential Redox-Active Catholyte Materials (Chem. Eur. J. 21/2025) 封面特征：氨基取代偶氮苯作为潜在的氧化还原活性阴极材料（化学）。欧元。j . 21/2025)

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202582102

Dominic Schatz, Chris Burdenski, Finn M. Schneider, Max M. Hansmann, Prof. Dr. Hermann A. Wegner

引用次数: 0

Optimization of Steroid Photochemistry and Its Application in the Synthesis of 5,6-dihydro-ophiopogonol A. 甾体光化学优化及其在5,6-二氢麦冬甾醇A合成中的应用。

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202500395

Chiara Maioli, Gianluigi Lauro, Anna Sategna, Diego Caprioglio, Hawraz Ibrahim M Amin, Maurizio D'Auria, Daniela Imperio, Giuseppe Bifulco, Alberto Minassi

引用次数: 0

Cover Feature: Unlocking New Frontiers: Photo-Isomerism and Magnetic Properties in Multifunctional Hetero-Tetra-Metallic Complexes (Chem. Eur. J. 21/2025) 封面专题：开启新领域：多功能杂四金属配合物的光异构和磁性（化学）。欧元。j . 21/2025)

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202582103

Dr. Ingrid Suzana, Jérémy Forté, Dr. Sébastien Pillet, Dr. El-Eulmi Bendeif, Dr. Moritz Malischewski, Dr. Valérie Marvaud

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Front Cover: Near-Neutral pH Sensing by Azoheteroarene Dyes (Chem. Eur. J. 21/2025) 封面：偶氮杂二烯染料的近中性pH传感（化学）。欧元。j . 21/2025)

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202582101

Dr. P. K. Hashim, Shifa Ahmad, Nusaiba Madappuram Cheruthu, Dr. Saugata Sahu, Prof. Nobuyuki Tamaoki

引用次数: 0

Osteosarcoma Cell and Osteosarcoma Stem Cell Potent Immunogenic Bi-nuclear Gallium(III) Complexes. 骨肉瘤细胞和骨肉瘤干细胞强免疫原性双核镓（III）复合物。

IF 3.9 2区化学

Chemistry - A European Journal Pub Date : 2025-04-09 DOI: 10.1002/chem.202500747

Xiao Feng, Shruti Dhandore, Yu Liu, Kuldip Singh, Fabrizio Ortu, Kogularamanan Suntharalingam

{"title":"Osteosarcoma Cell and Osteosarcoma Stem Cell Potent Immunogenic Bi-nuclear Gallium(III) Complexes.","authors":"Xiao Feng, Shruti Dhandore, Yu Liu, Kuldip Singh, Fabrizio Ortu, Kogularamanan Suntharalingam","doi":"10.1002/chem.202500747","DOIUrl":"https://doi.org/10.1002/chem.202500747","url":null,"abstract":"We report the synthesis, characterisation, anti-osteosarcoma and anti-osteosarcoma stem cells (OSC) properties (cytotoxic and immunogenic) of a series of bi-nuclear gallium(III) complexes with tridentate Schiff base ligands and 8-hydroxyquinoline (1-4). According to monolayer cytotoxicity studies, 1-4 display micromolar potency towards bulk osteosarcoma cells and OSCs. The most effective complex in the series 2 is up to 13-fold more potent towards OSCs than cisplatin and carboplatin (the only metallodrugs used in the clinic to treat osteosarcoma). Remarkably, the bi-nuclear gallium(III) complexes 1-4 are significantly more potent towards three-dimensionally cultured sarcospheres than OSCs cultured in monolayers indicating effective penetration of the sarcosphere multicellular architecture. The bi-nuclear gallium(III) complexes 1-4 are up to 53-fold more potent towards sarcospheres than cisplatin and carboplatin. Mechanistic studies show that gallium(III) complex 2 kills osteosarcoma cells by caspase-dependent apoptosis and paraptosis, leading to the release of danger-associated molecular patterns associated to immunogenic cell death. Osteosarcoma cells and OSCs treated with gallium(III) complex 2 are effectively phagocytosed by immune cells, highlighting its immunogenic potential. As far as we are aware, gallium(III) complex 2 is the first metal complex to evoke an immunogenic response towards both bulk osteosarcoma cells and OSCs.","PeriodicalId":144,"journal":{"name":"Chemistry - A European Journal","volume":" ","pages":"e202500747"},"PeriodicalIF":3.9,"publicationDate":"2025-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810297","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}

引用次数: 0