ACS Bio & Med Chem Au最新文献

{"title":"","authors":"Federica Scollo*, Waldemar Kulig, Gabriele Nicita, Anna-Kristin Ludwig, Joana C. Ricardo, Valeria Zito, Peter Kapusta, Ilpo Vattulainen, Marek Cebecauer, Hans-Joachim Gabius, Herbert Kaltner, Giuseppe Maccarrone* and Martin Hof*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00040","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144429488","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}

{"title":"","authors":"Fatemeh S. Hosseini, Ho-Man Kan, Taraje Whitfield, Chrysoula Argyrou, Amir A. Abedini, Nicholas S. Allen and Cato T. Laurencin*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.4c00152","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144429478","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}

{"title":"","authors":"Cheryl Kang-Rou Wong, Ye-Yu Chun, Tong Su and Lok-To Sham*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00010","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144429494","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}

{"title":"","authors":"Danae K. R. Bardaji, Nagela B. S. Silva, Renata R. Miranda, Carlos Henrique G. Martins, Michael A. Savka and André O. Hudson*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00069","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144429474","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}

{"title":"","authors":"Madhav V. Samudrala, Somanath Dandibhotla, Arjun Kaneriya and Sivanesan Dakshanamurthy*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00053","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144429482","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}

{"title":"","authors":"Karim Almahayni, Jana Bachir Salvador, Dijo Moonnukandathil Jospeh, Nazlican Yürekli, Stephanie Möllmert and Leonhard Möckl*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.4c00096","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144429471","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}

{"title":"","authors":"Marc-Antoine Turcotte,  and , Jean-Pierre Perreault*, ","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 3","pages":"XXX-XXX XXX-XXX"},"PeriodicalIF":3.8,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00004","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144355179","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}

{"title":"Consolidated 3-Fold Isotopic Lens for Probing RNAs","authors":"Solomon K. Attionu,&nbsp;Lukasz T. Olenginski,&nbsp;Frances P. Stump and Theodore K. Dayie*,&nbsp;","doi":"10.1021/acsbiomedchemau.5c00075","DOIUrl":"https://doi.org/10.1021/acsbiomedchemau.5c00075","url":null,"abstract":"<p >Undesired scalar and dipolar couplings are two major interactions that complicate structural and dynamic studies in solution nuclear magnetic resonance (NMR) spectroscopy. Recent developments in site-specific isotopic labeling technologies have gone a long way toward alleviating these problems. While some nuclei have intrinsic properties that make them suitable for specific NMR experiments, these same properties render them inefficient in other experiments. Site-specific isotopic labeling facilitates the controlled incorporation of isotopes to enable facile analysis of RNAs. Here, we describe the synthesis and incorporation of [1′-¹³C, 2-¹⁹F, 7-¹⁵N] adenosine 5′-triphosphate into the 9 kDa <i>Escherichia coli</i> rRNA, thus expanding the applications of previously synthesized [2-¹³C, 7-¹⁵N]-adenosine 5′-triphosphate, with the added benefit of ¹⁹F incorporation. We utilized these ¹³C and ¹⁵N probes to characterize the structural dynamic features within this RNA, and ¹⁹F was used to monitor binding interactions. Finally, we leveraged the chemical shielding anisotropy-dominated relaxation of ¹⁵N7-adenosine for straightforward analysis of <i>R</i>₁ and <i>R</i>_1ρ rates.</p>","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 4","pages":"694–705"},"PeriodicalIF":4.3,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00075","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144863124","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}

{"title":"Phenylalkyl Acetophenones and Anacardic Acids from Knema oblongifolia with Synthetic Analogues as Anti-infectives and Antibacterial Agents","authors":"Olivier Auguste Kirchhoffer,&nbsp;Jahn Nitschke,&nbsp;Alexandre Luscher,&nbsp;Louis-Félix Nothias,&nbsp;Laurence Marcourt,&nbsp;Nabil Hanna,&nbsp;Antonio Grondin,&nbsp;Thilo Köhler,&nbsp;Emerson Ferreira Queiroz*,&nbsp;Thierry Soldati and Jean-Luc Wolfender*,&nbsp;","doi":"10.1021/acsbiomedchemau.5c00052","DOIUrl":"https://doi.org/10.1021/acsbiomedchemau.5c00052","url":null,"abstract":"<p >The present study investigates the potential anti-infective and antibacterial properties of phenylalkyl acetophenones and anacardic acids isolated from the ethyl acetate extract of the leaves of Knema oblongifolia, along with synthetic derivatives that were generated. As antibiotic resistance grows, the discovery of new anti-infective agents becomes crucial. The study utilizes a phenotypic screening approach, employing a 3R infection model with <i>Mycobacterium marinum</i> (Mm) and <i>Dictyostelium discoideum</i> (Dd) as proxies for <i>Mycobacterium tuberculosis</i> and human macrophages. This model helps to distinguish between general antibiotics and specific anti-infectives that inhibit bacterial growth inside host cells. A previous screening carried out on a collection of 1600 plant natural extracts revealed <i>K. oblongifolia</i> as a significant source of anti-infective compounds. The ethyl acetate extract of this plant exhibited a strong inhibition of Mm intracellular growth in the infection model while minimally affecting bacterial growth in broth. HPLC bioactivity profiling of this extract based on a high-resolution microfractionation strategy uncovered that the activity was associated with different LC-peaks spread over the chromatogram. LC–MS-based metabolite profiling of the extract revealed that they shared common substructural elements. Based on such information, fractionation of the extract at a larger scale led to the isolation of 12 bioactive natural products (NPs): four newly described acetophenone NPs and eight salicylic acid derivatives (three of which were new). These NPs were further tested for their activities against Mm (antibacterial and anti-infective), <i>Pseudomonas aeruginosa</i>, and <i>Staphylococcus aureus</i>. Additionally, the study involved de novo synthesis of derivatives based on the backbones of the isolated acetophenones to enhance their bioactivity. Hemisynthesis on one of the isolated natural acetophenone was also carried out and resulted in an increase in potency but no increase in selectivity toward the inhibition of Mm intracellular growth. Overall, biological activity assessments revealed that some of the synthetic analogues generated were better candidates in terms of both selectivity and potency, with an improved activity profile compared to natural analogues. The best synthetic candidate reached an IC₅₀ of 0.59 μM for the inhibition of intracellular bacterial growth during infection (anti-infective activity).</p>","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 4","pages":"650–664"},"PeriodicalIF":4.3,"publicationDate":"2025-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00052","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144863082","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}

{"title":"5′-Phosphorothioester Linked Cyclic Dinucleotides, Endo-S-CDNs, Displaying Impressive Antitumor Activities In Vivo when Dosed Subcutaneously","authors":"Simpa K. Yeboah,&nbsp;Sagarika Meher,&nbsp;Haley Anne Harper,&nbsp;Carli McMahan,&nbsp;Bennett D. Elzey and Herman O. Sintim*,&nbsp;","doi":"10.1021/acsbiomedchemau.5c00070","DOIUrl":"https://doi.org/10.1021/acsbiomedchemau.5c00070","url":null,"abstract":"<p >Cyclic dinucleotides (CDNs) have become popular as immunotherapies triggering an immune response achieved via their activation of the cyclic GMP-AMP synthase-stimulator of interferon genes (cGAS-STING) pathway. Many analogs of 2′3′-cGAMP, c-di-GMP, and c-di-AMP have been developed and shown as effective cancer vaccines and immuno-stimulators for the induction of both the adaptive and innate immune systems. Unfortunately, these CDNs have been dosed via intratumor route, which is not convenient, especially for tumors that are difficult to reach. We recently introduced endo-S-CDNs as potent STING agonists but in our prior report we did not evaluate the in vivo efficacies of these novel STING agonists. Herein, we conduct a more extensive structure activity relationship study as well as in vivo evaluation of our best endo-S-CDNs. We demonstrate that endo-S-CDNs can be dosed via subcutaneous route to provide robust protection against MC38 and B16–F10 tumor models.</p>","PeriodicalId":29802,"journal":{"name":"ACS Bio & Med Chem Au","volume":"5 4","pages":"665–693"},"PeriodicalIF":4.3,"publicationDate":"2025-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://pubs.acs.org/doi/pdf/10.1021/acsbiomedchemau.5c00070","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144863081","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}