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Advances in Peptide-Targeted Fluorescent Probes for the Diagnosis and Therapy of Brain Disorders 肽靶向荧光探针在脑部疾病诊断和治疗中的研究进展

ChemistryEurope Pub Date : 2026-10-13 DOI: 10.1002/ceur.70370

Shuangjing Yang, Yuting Wang, Yongkang Yue, Fangjun Huo, Caixia Yin

{"title":"Advances in Peptide-Targeted Fluorescent Probes for the Diagnosis and Therapy of Brain Disorders","authors":"Shuangjing Yang, Yuting Wang, Yongkang Yue, Fangjun Huo, Caixia Yin","doi":"10.1002/ceur.70370","DOIUrl":"https://doi.org/10.1002/ceur.70370","url":null,"abstract":"Imbalances in brain tissue homeostasis can trigger a range of neurological disorders. However, diagnosing and treating these diseases remain profoundly challenging due to their complex pathophysiology, the highly selective permeability of the blood–brain barrier (BBB), and the lack of tools capable of early, specific, and quantitative detection. In this article, fluorescent probes have emerged as highly promising theranostic agents, owing to their high sensitivity, capacity for real-time spatiotemporal visualization, and compatibility with multimodal imaging and therapeutic platforms. Among these, peptide-based fluorescent probes have garnered particular interest due to their unique combination of efficient BBB translocation, high target specificity for pathological lesions, and favorable biocompatibility. These properties collectively enable both precise molecular imaging and site-specific therapeutic intervention. Consequently, the rational design of peptide fluorescent probes capable of efficient BBB penetration and selective accumulation at disease sites has become a key frontier in neuroscience probe development. This review comprehensively summarizes recent advances in peptide-based fluorescent probes for brain disorders—including Alzheimer’s disease, Parkinson’s disease, glioblastoma, and ischemic stroke. It critically evaluates their design principles, performance metrics, and translational potential, thereby providing a conceptual framework and technical guidelines for next-generation diagnostic and therapeutic strategies against brain diseases.","PeriodicalId":100234,"journal":{"name":"ChemistryEurope","volume":"4 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ceur.70370","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149205324","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Regioselective Pt(II)-Catalyzed 1,4-Hydrosilylation of α,β-Unsaturated Enamides and Tandem Carboxylation With CO2 区域选择性Pt(II)-催化α，β-不饱和烯酰胺的1,4-硅氢化反应和CO2串联羧化反应

ChemistryEurope Pub Date : 2026-10-08 DOI: 10.1002/ceur.70369

Natalia Salas, Amor Rodríguez, Salvador Conejero

{"title":"Regioselective Pt(II)-Catalyzed 1,4-Hydrosilylation of α,β-Unsaturated Enamides and Tandem Carboxylation With CO2","authors":"Natalia Salas, Amor Rodríguez, Salvador Conejero","doi":"10.1002/ceur.70369","DOIUrl":"https://doi.org/10.1002/ceur.70369","url":null,"abstract":"The regioselective hydrosilylation of α,β-unsaturated carbonyl compounds remains a significant challenge, as multiple reaction pathways are possible, leading to products derived from hydrosilylation of either the C═C or the C═O double bond, or reduction of the carbonyl moiety. Strategies enabling selective 1,4-hydrosilylation reactions that afford N,O-silyl ketene acetals from α,β-unsaturated enamides are very rare. This is likely due, besides the previously mentioned regioselectivity problems, to the highly nucleophilic character of these molecules, which can undergo Michael-type additions with the starting material. Indeed, these species are typically obtained through stoichiometric approaches. We have developed a catalytic protocol for the regioselective 1,4-hydrosilylation of α,β-unsaturated enamides using bench stable, low-electron count platinum complexes [Pt(GePh3)(ItBuR)2)][BArF]. The reaction proceeds under mild conditions and exhibits broad functional-group tolerance, including non-conjugated carbonyl fragments and double bonds that remain intact. Notably, the use of an α,β-unsaturated dienamide enables control over the regioselectivity, allowing the reaction to be steered toward a 1,6-hydrosilylation pathway. Importantly, the N,O-silyl ketene acetals readily undergo reaction with CO2 under mild reaction conditions leading to α-carboxylated amides. This latter process takes place without the need of the catalyst. The tandem hydrosilylation/carboxylation reaction occurs with complete atom economy, highlighting its synthetic efficiency and sustainability.","PeriodicalId":100234,"journal":{"name":"ChemistryEurope","volume":"4 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ceur.70369","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149146315","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Sulfur-Bridged Cationic and Neutral [6]Helicenes: Chiral Trityls With Property and Stability Twists 硫桥接阳离子和中性[6]螺旋烯：具有性能和稳定性旋曲的手性三苯基

ChemistryEurope Pub Date : 2026-10-08 DOI: 10.1002/ceur.70368

Aurélien Chignac, Céline Besnard, Caterina Monti, Francesco Zinna, Gennaro Pescitelli, Jérôme Lacour

{"title":"Sulfur-Bridged Cationic and Neutral [6]Helicenes: Chiral Trityls With Property and Stability Twists","authors":"Aurélien Chignac, Céline Besnard, Caterina Monti, Francesco Zinna, Gennaro Pescitelli, Jérôme Lacour","doi":"10.1002/ceur.70368","DOIUrl":"https://doi.org/10.1002/ceur.70368","url":null,"abstract":"Replacing oxygen or nitrogen bridges with sulfur in cationic [6]helicenes profoundly alters molecular shape, electronic structure, photophysics, chemical reactivity, and configurational stability. A modular strategy combining early sulfur incorporation, heteroatom-bridge diversification, and late-stage functionalization afforded fourteen neutral and cationic doubly bridged chiral trityl derivatives, including sulfoxide, sulfone, and sulfoximine derivatives. X-ray diffraction showed that longer C─S bonds enforce a puckered six-membered sulfur heterocycle, increasing helical pitch and curvature relative to O- and N-bridged analogs. The sulfur-containing carbocations are more electrophilic, displaying lower pKR+ values. Electrochemical, optical, and DFT studies show that sulfur destabilizes the HOMO while stabilizing the LUMO, narrowing the electronic gap and producing absorption up to 636 nm and emission up to 688 nm. Neutral azathia derivatives exhibit Stokes shifts up to 4823 cm−1, consistent with substantial excited-state relaxation. Sulfur oxidation provides orthogonal tuning, inducing blueshifts up to 66 nm in absorption and 124 nm in emission. CSP-HPLC resolution enabled electronic circular dichroism (ECD) and circularly polarized luminescence (CPL) studies, including rare bisignate CPL consistent with dual-state emission. Despite stronger geometric distortion, the cations racemize faster than oxygen and nitrogen analogs, supporting a nucleophile-assisted pathway. Overall, sulfur bridging emerges as a powerful alternative for tunable red-emissive helicenes with distinctive structural and photophysical responses.","PeriodicalId":100234,"journal":{"name":"ChemistryEurope","volume":"4 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ceur.70368","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149146318","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Front Cover: Metal–Ligand Cooperative Control of Reactivity in a Porphyrin Manganese(IV)–Oxo–Phenoxyl Radical Complex for Water Activation (ChemistryEurope 10/2026) 封面：金属-配体协同控制卟啉-锰(IV) -氧-苯氧基配合物的水活化反应性（ChemistryEurope 10/2026）

ChemistryEurope Pub Date : 2026-09-30 DOI: 10.1002/ceur.70375

Adelais Trapali, Rongning Lin, Georgios Charalambidis, Christian Herrero, Régis Guillot, Sylvain Bertaina, Manuel J. Llansola-Portoles, Athanassios Coutsolelos, Maylis Orio, Ally Aukauloo

引用次数: 0

Mechanochemical Birch Reductive Alkylation of Polycyclic Aromatic Hydrocarbons 多环芳烃的机械化学桦木还原烷基化反应

ChemistryEurope Pub Date : 2026-09-30 DOI: 10.1002/ceur.70367

Yoshifumi Toyama, Shota Mikawa, Hideto Ito

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Cover Feature: Direct, Additive-Free N-Formamide Synthesis From Secondary Amines and Oxygen With Visible-Light-Responsive TiO2 Catalysts (ChemistryEurope 10/2026) 封面特色：直接，无添加剂的n -甲酰胺合成从仲胺和氧与可见光响应TiO2催化剂（chemstreurope 10/2026）

ChemistryEurope Pub Date : 2026-09-30 DOI: 10.1002/ceur.70374

Mayu Yuasa, Keita Shichijo, Yohei Kametani, Yoshihito Shiota, Hisashi Shimakoshi

引用次数: 0

Vicinal Difunctionalization of Alkenes With Ketones and 1,2-Bis(phenylsulfonyl)ethylene With One-Electron Oxidation: A Three-Component Route to Functionalized Vinyl Sulfones 烯与酮和1,2-二（苯基磺酰基）乙烯相邻双官能化的单电子氧化：三组分功能化乙烯基砜的途径

ChemistryEurope Pub Date : 2026-09-29 DOI: 10.1002/ceur.70365

Lin-Wei Pan, Shu-Fan Wu, Yen-Ku Wu, Hiroshi Matsubara, Ilhyong Ryu

{"title":"Vicinal Difunctionalization of Alkenes With Ketones and 1,2-Bis(phenylsulfonyl)ethylene With One-Electron Oxidation: A Three-Component Route to Functionalized Vinyl Sulfones","authors":"Lin-Wei Pan, Shu-Fan Wu, Yen-Ku Wu, Hiroshi Matsubara, Ilhyong Ryu","doi":"10.1002/ceur.70365","DOIUrl":"https://doi.org/10.1002/ceur.70365","url":null,"abstract":"Protocols for three-component coupling reactions of ketones, alkenes, and 1,2-bis(phenylsulfonyl)ethylene (BPSE) have been developed using one-electron oxidizing systems based on potassium persulfate and manganese(III) acetate. These methods enable vicinal difunctionalization of alkenes, affording keto-functionalized alkenyl sulfones in good to high yields. The reaction cascade is initiated by oxidative deprotonation of ketones via their enol forms. The resulting α-keto radicals add to alkenes to generate alkyl radicals, which subsequently undergo an addition/β-elimination sequence with BPSE, delivering the corresponding keto-functionalized alkenyl sulfones in good yields. While persulfate is effective for generating α-keto radicals from β-diketones, manganese(III) acetate exhibits broader applicability, accommodating a wider range of mono-ketones and protic C(sp3)-H substrates. To gain insight into the observed preference for unactivated alkene addition over BPSE, DFT calculations were performed.","PeriodicalId":100234,"journal":{"name":"ChemistryEurope","volume":"4 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ceur.70365","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149068314","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Mechanistic Study Reveals Hypoboric Acid Catecholate (HAC): An Enhanced Diboron Reagent for Decarboxylative Borylation 次硼酸儿茶酚酸（HAC）：一种增强的二硼脱羧试剂

ChemistryEurope Pub Date : 2026-09-29 DOI: 10.1002/ceur.70363

B. Meana-Baamonde, W.-J. Wei, S. V. Kohlhepp, M. Montesinos-Magraner, F. Himo, A. Mendoza

{"title":"Mechanistic Study Reveals Hypoboric Acid Catecholate (HAC): An Enhanced Diboron Reagent for Decarboxylative Borylation","authors":"B. Meana-Baamonde, W.-J. Wei, S. V. Kohlhepp, M. Montesinos-Magraner, F. Himo, A. Mendoza","doi":"10.1002/ceur.70363","DOIUrl":"https://doi.org/10.1002/ceur.70363","url":null,"abstract":"The decarboxylative borylation of redox-active esters promoted by bis(catecholato)diboron (B2cat2) and blue light enables the synthesis of versatile organoboron building blocks from carboxylic acid materials. An LED-illuminated NMR kinetic study revealed that the reaction is surprisingly accelerated by water, and this hidden catalysis can be attributed to a novel intermediate formed in situ, namely a hypoboric acid catecholate (HAC). This unsymmetrical diboron species can alternatively be formed by hydrolysis of B2cat2 or transesterification between B2cat2 and hypoboric acid (B2(OH)4). Experimental and computational studies revealed and rationalized the regioselective capture of alkyl radicals by the HAC species, and the concomitant formation of a more reductive boryl radical chain carrier. The regioselectivity is characteristic of the HAC species studied, and is controlled by electronic rather than steric effects.","PeriodicalId":100234,"journal":{"name":"ChemistryEurope","volume":"4 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ceur.70363","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149146839","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

High-Valent Copper(III) Compounds: Structural Diversity and Versatile Applications 高价铜（III）化合物：结构多样性及其广泛应用

ChemistryEurope Pub Date : 2026-09-24 DOI: 10.1002/ceur.70364

Vladimir Motornov

引用次数: 0

Exploiting the B–N/C–C Isosterism Yields Nile-Red Inspired Organoboron Dyes Capable of Singlet-Oxygen Photosensitization 利用B-N / C-C等构制得单重态氧光敏的尼罗红激发有机硼染料

ChemistryEurope Pub Date : 2026-09-23 DOI: 10.1002/ceur.70362

João Felicidade, Francisco G. Blandón-Cumbreras, Jesús F. Arteaga, Patricia Remón, Adelaide Fernandes, Giulia Salluce, Gilles Gasser, Francisco Nájera, Fábio M. F. Santos, Uwe Pischel, Pedro M. P. Gois

{"title":"Exploiting the B–N/C–C Isosterism Yields Nile-Red Inspired Organoboron Dyes Capable of Singlet-Oxygen Photosensitization","authors":"João Felicidade, Francisco G. Blandón-Cumbreras, Jesús F. Arteaga, Patricia Remón, Adelaide Fernandes, Giulia Salluce, Gilles Gasser, Francisco Nájera, Fábio M. F. Santos, Uwe Pischel, Pedro M. P. Gois","doi":"10.1002/ceur.70362","DOIUrl":"https://doi.org/10.1002/ceur.70362","url":null,"abstract":"Small dyes are indispensable tools for probing biological processes. Among them, Nile Red (NR) is widely used for imaging lipid-rich environments. However, the structural diversification of its phenoxazine core remains limited. Herein, we exploit B─N/C─C isosterism to connect the western and eastern fragments of NR through a B─N linkage, enabling the design of NR-inspired boronic acid-derived salicylidenehydrazone (NR-BASHY) dyes with enhanced structural and functional versatility. This strategy allows the modular one-pot synthesis of NR-BASHY dyes, which exhibit promising photophysical properties. These include intense absorption (ε up to 50,800 M–1cm–1) and high brightness (ε × Φf up to 17,000 M–1 cm–1) and a pronounced solvatofluorochromism with emission spanning the red to near-infrared spectral region. In strong contrast to NR, NR-BASHY can act as photosensitizers, featuring efficient singlet-oxygen generation (ΦΔ up to 0.8) and photoinduced cytotoxicity against the U87 glioblastoma cell line in the submicromolar range (IC50 ca. 0.5 μM), while maintaining low dark toxicity (>100 μM). Moreover, the modular architecture of NR-BASHY dyes enables click-reaction mediated bioconjugation with the GV1001 peptide, highlighting the potential of this platform for targeted bioimaging applications.","PeriodicalId":100234,"journal":{"name":"ChemistryEurope","volume":"4 9","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ceur.70362","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149048195","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0