Article
Chemistry, Multidisciplinary
Michael A. Morris, Alexander Vallmitjana, Fabian Grein, Tanja Schneider, Melina Arts, Chelsea R. Jones, Betty T. Nguyen, Mohammad H. Hashemian, Melody Malek, Enrico Gratton, James S. Nowick
Summary: Teixobactin is a promising antibiotic with excellent activity against drug-resistant Gram-positive pathogens and a novel mechanism of action that prevents drug resistance. Recent studies have shown that the supramolecular assembly of Teixobactin plays a critical role in its binding process. Fluorescence microscopy and FRET microscopy have provided insights into the binding of Teixobactin to bacteria and its molecular targets.
Article
Chemistry, Multidisciplinary
Chelsea R. Jones, Gretchen Guaglianone, Grant H. Lai, James S. Nowick
Summary: The antibiotic teixobactin shows potential as a candidate drug to combat drug-resistant pathogens, but its gel-like form limits its use in intravenous administration. O-Acyl isopeptide prodrug analogues of teixobactin provide a solution to the gel formation issue while retaining antibiotic activity. These prodrug analogues convert to the corresponding amides in a clean manner and exhibit good antibiotic activity against Gram-positive bacteria.
Article
Chemistry, Multidisciplinary
Zhenquan Sun, Xuechen Li
Summary: The study aims to develop a chemoselective ligation strategy for assembling unprotected peptide segments, with a focus on improving ligation efficiency and selectivity. The experiment demonstrates that the use of peptide acyl ester of 2-formylphenylboronic acid can enhance stability and reactivity in Ser/Thr ligation and Cys/Pen ligation, but further efforts are needed to enhance ligation chemistry.
CHINESE JOURNAL OF CHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Tyler K. Heiss, Robert S. Dorn, Jennifer A. Prescher
Summary: Bioorthogonal phosphines were introduced in the context of the Staudinger ligation and have since been widely used to tag azide-functionalized biomolecules in biological experiments. Recent advances in this field have highlighted the versatility and importance of bioorthogonal phosphines in various biological pursuits.
Article
Chemistry, Medicinal
Anish Parmar, Rajamani Lakshminarayanan, Abhishek Iyer, Eunice Tze Leng Goh, Tsz Ying To, Joey Kuok Hoong Yam, Liang Yang, Enas Newire, Maria C. Robertson, Stephen H. Prior, Eefjan Breukink, Annemieke Madder, Ishwar Singh
Summary: Teixobactin analogues with simplified structures, consisting of commercially available hydrophobic amino acid residues and various combinations of arginines, showed potent antibacterial activity against a broad range of Gram-positive bacteria, including MRSA and VRE strains. These analogues also demonstrated strong antibiofilm activity against Staphylococcus species associated with chronic infections, providing insights for the synthesis of highly potent Teixobactin analogues to combat resistant bacterial infections and biofilms.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Organic
Yuhua Ge, Xingyue Chen, Shah Nawaz Khan, Shuhe Jia, Gang Chen
Summary: Herein, an efficient and practical synthetic route was developed to assemble novel highly-tens [5,5] trans-fused B/C strigolactam/strigolactone analogues along with cis-fused strigolactams. The synthetic strategy involves palladium-catalyzed carboxylate-directed olefination of commercially available N-Boc phenylalanines followed by direct photocatalytic decarboxylative Giese cyclization. SAR studies showed that the trans-fused compounds exhibited better activity than the cis-fused compounds. Notably, strigolactones 35/36 and 39/40 demonstrated superior bioactivity compared to GR245DS and GR244DO.
TETRAHEDRON LETTERS
(2023)
Article
Chemistry, Physical
Abdullah Yahya Abdullah Alzahrani, Bushra Adalat, Hayat Ullah, Muhammad Taha, Mohamed S. Othman, Mohamed A. Fareid, Azza M. Khaled, Fazal Rahim
Summary: This study synthesized benzimidazole thiosemicarbazides and sulphonamide derivatives as potent urease inhibitors, which showed good inhibition potential and stable interactions. This is significant for reducing the negative effects of ureolytic bacteria.
JOURNAL OF MOLECULAR STRUCTURE
(2024)
Article
Biochemistry & Molecular Biology
Jiayu Sun, Jie Li, Hongbao Sun, Chunling Li, Haoxing Wu
Summary: The study presents the concise synthesis of a series of aryl-functionalized cyclobutene analogues using commercially available starting materials, demonstrating their suitability as stable substrates for bioorthogonal tetrazine ligation.
Article
Engineering, Electrical & Electronic
Weijia Han, Xiao Ma, Di Tang, Nan Zhao
Summary: This paper investigates the SER and BER in NOMA considering the downlink/uplink transmission, the number of information streams, and the impact of channel coding, with Gray coding introduced for downlink transmission. Closed-form expressions for SER and BER are derived to efficiently evaluate transmission performance. It is shown that error propagation/error accumulation phenomenon is not present in SIC demodulation in NOMA systems, and a joint Gray-coding scheme is introduced to effectively reduce SER and BER in downlink transmission.
IEEE TRANSACTIONS ON VEHICULAR TECHNOLOGY
(2021)
Review
Infectious Diseases
Rameshwar S. Cheke, Harun M. Patel, Vaishali M. Patil, Iqrar Ahmad Ansari, Jaya P. Ambhore, Sachin D. Shinde, Adel Kadri, Mejdi Snoussi, Mohd Adnan, Prashant S. Kharkar, Visweswara Rao Pasupuleti, Prashant K. Deshmukh
Summary: This study summarizes the research progress of coumarins and their derivatives in the field of antimicrobials, including various synthetic strategies and structure-activity relationships reported. Coumarin analogues demonstrate potential antibacterial effects, providing reference for combating multidrug-resistant bacteria.
Article
Biochemistry & Molecular Biology
Andrea Spallarossa, Matteo Lusardi, Chiara Caneva, Aldo Profumo, Camillo Rosano, Marco Ponassi
Summary: A novel series of pyrimido-pyrimidine analogues have been synthesized with potent antiproliferative activity, although they show differences in binding to topoisomerase II alpha. The activity of the new compounds is influenced by the nature of the basic side chain and the substituents on the pyrimido-pyrimidine moiety.
Article
Multidisciplinary Sciences
Rhythm Shukla, Francesca Lavore, Sourav Maity, Maik G. N. Derks, Chelsea R. Jones, Bram J. A. Vermeulen, Adela Melcrova, Michael A. Morris, Lea Marie Becker, Xiaoqi Wang, Raj Kumar, Joao Medeiros-Silva, Roy A. M. van Beekveld, Alexandre M. J. J. Bonvin, Joseph H. Lorent, Moreno Lelli, James S. Nowick, Harold D. MacGillavry, Aaron J. Peoples, Amy L. Spoering, Losee L. Ling, Dallas E. Hughes, Wouter H. Roos, Eefjan Breukink, Kim Lewis, Markus Weingarth
Summary: The mechanism of action of Teixobactin has been revealed, showing that it damages bacterial cell membranes by binding to lipid II. This unique mode of action allows Teixobactin to target bacteria without harming human cells, making it a highly effective antibiotic.
Article
Chemistry, Physical
Menier Al-Anazi
Summary: The study synthesized a series of thiadiazole-triazole-thiazolidinone hybrids and evaluated their cytotoxicity against various cancer cell lines. The compounds with the most potent activity were identified, and the structure-activity relationship was analyzed to explain their anticancer efficacy.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Medicinal
Adrian Richter, Gagandeep Narula, Ines Rudolph, Ruediger W. Seidel, Christoph Wagner, Yossef Av-Gay, Peter Imming
Summary: 8-Nitrobenzothiazinones (BTZs) are a promising class of antimycobacterial agents currently being investigated in clinical trials. A new synthetic pathway has been established to synthesize various analogues of BTZs, allowing the replacement of the sulphur atom by oxygen or nitrogen. A total of 36 analogues were synthesized and tested for their potential activity against Mycobacterium tuberculosis (Mtb) in in vitro assays.
Article
Chemistry, Medicinal
Ruijia Zhang, Feng Hong, Min Zhao, Xiaoying Cai, Xueqin Jiang, Neng Ye, Kaiyue Su, Na Li, Minghai Tang, Xu Ma, Hengfan Ni, Lun Wang, Li Wan, Lijuan Chen, Wenshuang Wu, Haoyu Ye
Summary: Compound 14c, a novel NLRP3 inhibitor, was developed through structural optimization with significantly enhanced inhibitory activity, reducing neutrophil influx and IL-1 beta expression in a mouse model of peritonitis, showing promising potential as a lead compound in the discovery of NLRP3 inflammasome inhibitors.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Ping Zeng, Qipeng Cheng, Lanhua Yi, Sharon Shui Yee Leung, Sheng Chen, Kin-Fai Chan, Kwok-Yin Wong
Summary: In this study, a small peptide library was constructed by capping a macrolactam ring at the C-terminus of a designed peptide. Eight different peptides with aspartic acid-rich macrolactam rings were found to exhibit improved antibacterial activities, and mechanistic studies revealed their mode of action.
BIOORGANIC CHEMISTRY
(2023)
Article
Food Science & Technology
Yan Li, Zhiqiang Wang, Huiyue Dong, Mianzhi Wang, Shangshang Qin, Sheng Chen, Ruichao Li
Summary: Six tet(X4)-positive Klebsiella pneumoniae strains were isolated from pork samples in China, one of which was hypermucoviscous and hypervirulent. The tet(X4) gene was located on a plasmid with a similar structure to blaKPC-2-positive plasmids in hvKp, and it could be transferred to E. coli and ST11 hvKp without a significant fitness cost and persist stably. This is the first report of tet(X4)-positive hvKp in animals, highlighting the urgent need for global surveillance in clinical and animal farming settings.
LWT-FOOD SCIENCE AND TECHNOLOGY
(2023)
Article
Microbiology
Yating Xu, Zhiwei Zheng, Lianwei Ye, Edward Wai-chi Chan, Sheng Chen
Summary: This study investigated the prevalence of qnrVC genes in foodborne Vibrio strains collected in Shenzhen, China, from August 2015 to April 2017. The presence of qnrVC genes was shown to enhance ciprofloxacin resistance in Vibrio strains. Mutations in the gyrA and parC genes were commonly associated with ciprofloxacin resistance. The study also found 14 variant genes containing novel mutations, with 85.7% being qnrVC5-like alleles.
MICROBIOLOGICAL RESEARCH
(2023)
Article
Infectious Diseases
Yanyan Zhang, Xuemei Yang, Congcong Liu, Ling Huang, Lingbin Shu, Qiaoling Sun, Hongwei Zhou, Yonglu Huang, Chang Cai, Xiaoyan Wu, Sheng Chen, Rong Zhang
Summary: This study investigated the prevalence and characteristics of OXA-232 type carbapenemase in Zhejiang Province, China from 2018 to 2021. The results showed that OXA-232 is the most prevalent OXA-48-like derivative, and ST15 K. pneumoniae isolates are the major carriers. The transmission of ColKP3-type plasmid to E. coli highlighted the importance of understanding the transmission mechanism to prevent the spread of OXA-232 to other species.
INFECTIOUS DISEASES OF POVERTY
(2023)
Article
Microbiology
Xuemei Yang, Xiaoxuan Liu, Edward Wai-Chi Chan, Rong Zhang, Sheng Chen
Summary: Klebsiella pneumoniae has become a major bacterial pathogen in hospitals, with a high mortality rate. Factors contributing to its virulence are the overproduction of capsular polysaccharide (CPS) and the hypermucoviscosity (HMV) phenotype. This study investigated the functional characteristics of plasmid-borne rmp homologues in clinical hypervirulent K. pneumoniae strains. The results showed that the rmp homologues play a key role in regulating the HMV phenotype and CPS production in K. pneumoniae.
MICROBIOLOGY SPECTRUM
(2023)
Article
Microbiology
Xiaobo Liu, Ruichao Li, Edward Wai-Chi Chan, Sheng Chen
Summary: Bacterial antimicrobial resistance, especially phenotypic resistance to multiple drugs (MDR), has posed a serious threat to public health worldwide. Understanding the mechanisms of transmission of multidrug resistance encoding plasmids in Enterobacterales is crucial for controlling the spread of MDR pathogens. In this study, plasmids in an Escherichia coli strain isolated from chicken meat samples were characterized, revealing the presence of multiple antimicrobial resistance genes and the potential for transmission of resistance determinants.
MICROBIOLOGY SPECTRUM
(2023)
Article
Microbiology
Yonggang Zhao, Dingqiang Chen, Kaichao Chen, Miaomiao Xie, Jiubiao Guo, Edward Wai Chi Chan, Lu Xie, Jingbo Wang, Enqi Chen, Sheng Chen, Weijun Chen, Lars Jelsbak
Summary: By sequencing and analyzing the genomes of 416 Pseudomonas aeruginosa strains from hospitals in China, the genetic, phenotypic, and transmission characteristics of carbapenem-resistant strains were elucidated, and the molecular signatures responsible for the increased prevalence of CRPA infections in China were identified. These findings may provide new insight into the development of effective strategies for worldwide control of CRPA and minimize the occurrence of untreatable infections in clinical settings.
MICROBIOLOGY SPECTRUM
(2023)
Article
Chemistry, Multidisciplinary
Samir Manna, Swagata Paul, Wang-Yeuk Kong, Debasis Aich, Rupam Sahoo, Dean J. Tantillo, Santanu Panda
Summary: Stereoselective Zweifel olefination using boronate complexes carrying two different reactive π-systems was achieved for the synthesis of vinyl heteroarenes and conjugated 1,3-dienes. The unprecedented formation of E vs. Z-vinyl heteroarenes for different heteroarenes under identical conditions was reported. Density functional theory (DFT) investigations revealed the mechanistic dichotomy between olefin and heteroarene activation followed by 1,2-migration, leading to E or Z-vinyl heteroarenes respectively. A previously unknown reversal of stereoselectivity was also reported using 2,3-Dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) as an electrophile.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Neha Jha, Wentao Guo, Wang-Yeuk Kong, Dean J. Tantillo, Manmohan Kapur
Summary: A site-selective C(3)/C(4)-alkylation of N-pyridylisoquinolones is achieved through C-C bond activation of cyclopropanols under Ru(II)-catalyzed/Cu(II)-mediated conditions. The regioisomeric ratios of the products depend on the electronic nature of the cyclopropanols and isoquinolones used. The methodology has the potential for synthesizing relevant scaffolds.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Applied
Ping Zeng, Pengfei Zhang, Lanhua Yi, Kwok-Yin Wong, Sheng Chen, Kin-Fai Chan, Sharon Shui Yee Leung
Summary: Researchers have developed a new antibacterial peptide (zp80r) by modifying the structure of a reported peptide. This peptide has shown promise in reducing the quantity of pathogenic bacteria on the surface of pork products, making it a potential candidate for controlling foodborne pathogens during storage.
Article
Chemistry, Multidisciplinary
Joseph P. Mancinelli, Wang-Yeuk Kong, Wentao Guo, Dean J. Tantillo, Sidney M. Wilkerson-Hill
Summary: In this study, a method for synthesizing tert-alkyl cyclopropanes through C-F bond functionalization of gem-difluorocyclopropenes using tris(pentafluorophenyl)borane catalysis is disclosed. The reaction proceeds through the intermediacy of a fluorocyclopropenium ion, which was confirmed by the isolation of [Ph-2(C6D5)C-3](+)[(C6F5)(3)BF](-). It was found that silylketeneacetal nucleophiles were optimal reaction partners, yielding fully substituted cyclopropenes functionalized with two α-tert-alkyl centers (63-93% yield).
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Multidisciplinary
Andre Sanchez, Anjali Gurajapu, Wentao Guo, Wang-Yeuk Kong, Croix J. Laconsay, Nicholas S. Settineri, Dean J. Tantillo, Thomas J. Maimone
Summary: Polycyclic ring systems are crucial for the function of biologically active small molecules and organic materials, and slight changes in their molecular shape and connectivity can greatly impact their properties. By utilizing unique molecular topology involving pi-orbital interactions, a common skeletal ancestor can evolve into a complex network of valence isomers, allowing for controllable and continuous isomerization processes with just two chemical steps. Computational and photophysical studies provide insight into the reactivity and mechanism of these isomer networks, which can inform the design and synthesis of new dynamic and shapeshifting systems.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Microbiology
Zhiwei Zheng, Lizhang Liu, Lianwei Ye, Yating Xu, Sheng Chen
Summary: A nationwide survey in China identified seven blaIMP-4-carrying CRKP isolates, which exhibited MDR and were linked to different regions. Genetic analysis revealed significant variation among these CRKP strains and identified multiple resistance factors. This highlights the need for expanded surveillance and control measures to prevent dissemination of CRKP strains and improve antibiotic stewardship and infection control.
MICROBIOLOGICAL RESEARCH
(2023)
Article
Microbiology
Yating Xu, Zhiwei Zheng, Lianwei Ye, Edward Wai-Chi Chan, Sheng Chen
Summary: A new quinolone resistance gene, qnrS, was found in foodborne Vibrio spp., which could mediate resistance to ciprofloxacin and cephalosporins. The qnrS2 gene could be found on both the chromosome and plasmids, with the pAQU-type qnrS2-bearing conjugative plasmids able to mediate resistance to both ciprofloxacin and cephalosporins. Transmission of this plasmid among Vibrio spp. may lead to the emergence of multidrug-resistant pathogens.
MICROBIOLOGY SPECTRUM
(2023)
Letter
Biochemistry & Molecular Biology
Qi Xu, Miaomiao Xie, Xiaoxuan Liu, Heng Heng, Han Wang, Chen Yang, Edward Wai-Chi Chan, Rong Zhang, Guan Yang, Sheng Chen
SIGNAL TRANSDUCTION AND TARGETED THERAPY
(2023)
