Chemistry-Switzerland最新文献

Photocyclization of Alkenes and Arenes: Penetrating Through Aromatic Armor with the Help of Excited State Antiaromaticity. 烯烃和芳烃的光环化：借助激发态抗芳性穿透芳甲。

IF 2.4

Chemistry-Switzerland Pub Date : 2025-06-01 Epub Date: 2025-05-09 DOI: 10.3390/chemistry7030079

Nikolas R Dos Santos, Judy I Wu, Igor V Alabugin

引用次数: 0

Transformation of Linear Alkenyl N-Alkoxy Carbamates into Cyclic Bromo Carbonates. 线性炔基n -烷氧基氨基甲酸酯转化为环碳酸溴酯。

IF 2.4

Chemistry-Switzerland Pub Date : 2025-06-01 Epub Date: 2025-06-16 DOI: 10.3390/chemistry7030099

Shyam Sathyamoorthi, Steven P Kelley

引用次数: 0

Tethered Antigenic Suppression Shields the Hemagglutinin Head Domain and Refocuses the Antibody Response to the Stalk Domain. 栓系抗原抑制屏蔽血凝素头部结构域，并将抗体反应重新集中到茎结构域。

IF 2.4

Chemistry-Switzerland Pub Date : 2025-02-01 Epub Date: 2025-01-21 DOI: 10.3390/chemistry7010012

Donguk Kim, Kathryn Loeffler, Yixin Hu, Ammar Arsiwala, Steven Frey, Shruthi Murali, Vivek Hariharan, Alberto Moreno, Ravi S Kane

{"title":"Tethered Antigenic Suppression Shields the Hemagglutinin Head Domain and Refocuses the Antibody Response to the Stalk Domain.","authors":"Donguk Kim, Kathryn Loeffler, Yixin Hu, Ammar Arsiwala, Steven Frey, Shruthi Murali, Vivek Hariharan, Alberto Moreno, Ravi S Kane","doi":"10.3390/chemistry7010012","DOIUrl":"10.3390/chemistry7010012","url":null,"abstract":"Influenza has been a global health concern for the past century. Current seasonal influenza vaccines primarily elicit an antibody response that targets the immunodominant head domain of the viral glycoprotein hemagglutinin (HA), which consistently mutates due to selective pressure. To circumvent this problem, we introduce a \"tethered antigenic suppression\" strategy to shield the HA head domain and refocus the immune response towards the conserved but immunosubdominant stalk domain of HA. Specifically, we tethered an antibody fragment (Fab) that recognizes the Sb antigenic site in the HA head domain to the HA protein with a linker. We immunized separate groups of female mice with the Fab-tethered HA or regular HA and characterized the elicited antibody response. We demonstrate that shielding the HA head domain with a tethered Fab suppresses the antibody titers towards all five key antigenic sites in the HA head domain while eliciting a robust anti-stalk antibody response. Our work highlights the potential of tethered antigenic suppression as a strategy to refocus the antibody response towards conserved epitopes on protein antigens.","PeriodicalId":53216,"journal":{"name":"Chemistry-Switzerland","volume":"7 1","pages":""},"PeriodicalIF":2.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12468577/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145187455","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

The Non-Anhydrous, Minimally Basic Synthesis of the Dopamine D₂ Agonist [18F]MCL-524. 多巴胺D2激动剂[18F]MCL-524的非无水、最低碱性合成。

IF 2.1

Chemistry-Switzerland Pub Date : 2021-09-01 Epub Date: 2021-09-09 DOI: 10.3390/chemistry3030075

James A H Inkster, Anna W Sromek, Vamsidhar Akurathi, John L Neumeyer, Alan B Packard

{"title":"The Non-Anhydrous, Minimally Basic Synthesis of the Dopamine D2 Agonist [18F]MCL-524.","authors":"James A H Inkster, Anna W Sromek, Vamsidhar Akurathi, John L Neumeyer, Alan B Packard","doi":"10.3390/chemistry3030075","DOIUrl":"10.3390/chemistry3030075","url":null,"abstract":"The dopamine D2 agonist MCL-524 is selective for the D2 receptor in the high-affinity state (D2high), and, therefore, the PET analogue, [18F]MCL-524, may facilitate the elucidation of the role of D2high in disorders such as schizophrenia. However, the previously reported synthesis of [18F]MCL-524 proved difficult to replicate and was lacking experimental details. We therefore developed a new synthesis of [18F]MCL-524 using a \"non-anhydrous, minimally basic\" (NAMB) approach. In this method, [18F]F- is eluted from a small (10-12 mg) trap-and-release column with tetraethylammonium tosylate (2.37 mg) in 7:3 MeCN:H2O (0.1 mL), rather than the basic carbonate or bicarbonate solution that is most often used for [18F]F- recovery. The tosylated precursor (1 mg) in 0.9 mL anhydrous acetonitrile was added directly to the eluate, without azeotropic drying, and the solution was heated (150 °C/15 min). The catechol was then deprotected with the Lewis acid In(OTf)3 (10 equiv.; 150 °C/20 min). In contrast to deprotection with protic acids, Lewis-acid-based deprotection facilitated the efficient removal of byproducts by HPLC and eliminated the need for SPE extraction prior to HPLC purification. Using the NAMB approach, [18F]MCL-524 was obtained in 5-9% RCY (decay-corrected, n = 3), confirming the utility of this improved method for the multistep synthesis of [18F]MCL-524 and suggesting that it may applicable to the synthesis of other 18F-labeled radiotracers.","PeriodicalId":53216,"journal":{"name":"Chemistry-Switzerland","volume":"3 3","pages":"1047-1056"},"PeriodicalIF":2.1,"publicationDate":"2021-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10569134/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41219982","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