Acridinium‐conjugated aromatic heterocycles as highly potent FtsZ inhibitors: Design, synthesis, and biological evaluation
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202100400
Abstract: The epidemic of multidrug resistance (MDR) is a serious threat to public health, and new classes of antibiotics with novel mechanisms of action are in critical need. We rationally designed and efficiently synthesized three series… read more here.
Keywords: evaluation; acridinium conjugated; conjugated aromatic; heterocycles highly ... See more keywords
An enhancer sequence in the intrinsically disordered region of FtsZ promotes polymer‐guided substrate processing by ClpXP protease
Sign Up to like & getrecommendations! Published in 2022 at "Protein Science"
DOI: 10.1002/pro.4306
Abstract: The essential bacterial division protein in Escherichia coli, FtsZ, assembles into the FtsZ‐ring at midcell and recruits other proteins to the division site to promote septation. A region of the FtsZ amino acid sequence that… read more here.
Keywords: intrinsically disordered; region ftsz; region; polymer guided ... See more keywords
Computer-aided identification of lead compounds as Staphylococcal epidermidis FtsZ inhibitors using molecular docking, virtual screening, DFT analysis, and molecular dynamic simulation
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Modeling"
DOI: 10.1007/s00894-019-4238-6
Abstract: In an effort to face the multiple drug-resistant bacteria, various approaches have been discovered to design potent compounds and search new targets through computational design tools. With an aim to identify selective inhibitors against filamentous… read more here.
Keywords: virtual screening; staphylococcal epidermidis; ftsz; compounds staphylococcal ... See more keywords
A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of pharmacological sciences"
DOI: 10.1016/j.jphs.2018.07.005
Abstract: The antibacterial activity and the synergistic effect with β-lactam antibiotics of a new 1-methylquinolinium iodide derivative were investigated. The experimental results indicate that the compound possesses a strong antibacterial activity against a panel of bacteria… read more here.
Keywords: ftsz; lactam antibiotics; activity synergistic; compound ... See more keywords
Synthesis and Docking Study of N-(Cinnamoyl)-N'-(Substituted)acryloyl Hydrazide Derivatives Containing Pyridinium Moieties as a Novel Class of FtsZ Inhibitors against the Intractable Xanthomonas oryzae pv. oryzae Infections in Rice.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.0c01565
Abstract: Xanthomonas oryzae pv. oryzae (Xoo) is an offensive phytopathogen that can invade a wide range of plant hosts to develop bacterial diseases, including the well-known rice bacterial leaf blight. However, few agrochemicals have been identified… read more here.
Keywords: ftsz; xoo; oryzae oryzae; cinnamoyl substituted ... See more keywords
Structural and Antibacterial Characterization of a New Benzamide FtsZ Inhibitor with Superior Bactericidal Activity and In Vivo Efficacy Against Multidrug-Resistant Staphylococcus aureus.
Sign Up to like & getrecommendations! Published in 2023 at "ACS chemical biology"
DOI: 10.1021/acschembio.2c00934
Abstract: Methicillin-resistant Staphylococcus aureus (MRSA) is a multidrug-resistant (MDR) bacterial pathogen of acute clinical significance. Resistance to current standard-of-care antibiotics, such as vancomycin and linezolid, among nosocomial and community-acquired MRSA clinical isolates is on the rise.… read more here.
Keywords: benzamide ftsz; ftsz; new benzamide; ftsz inhibitor ... See more keywords
FtsZ induces membrane deformations via torsional stress upon GTP hydrolysis
Sign Up to like & getrecommendations! Published in 2021 at "Nature Communications"
DOI: 10.1038/s41467-021-23387-3
Abstract: FtsZ is a key component in bacterial cell division, being the primary protein of the presumably contractile Z ring. In vivo and in vitro, it shows two distinctive features that could so far, however, not… read more here.
Keywords: gtp hydrolysis; ftsz; torsional stress; membrane deformations ... See more keywords
In silico Analysis of FtsZ Crystal Structures Towards a New Target for Antibiotics
Sign Up to like & getrecommendations! Published in 2019 at "Australian Journal of Chemistry"
DOI: 10.1071/ch18347
Abstract: The bacterial cell division protein FtsZ is conserved in most bacteria and essential for viability. There have been concerted efforts in developing inhibitors that target FtsZ as potential antibiotics. Key to this is an in-depth… read more here.
Keywords: interdomain cleft; silico analysis; analysis ftsz; ftsz structures ... See more keywords
MipZ caps the plus-end of FtsZ polymers to promote their rapid disassembly.
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2208227119
Abstract: Significance Cytoskeletal proteins are tightly controlled to ensure their proper dynamics and function. Here, we study the regulation of the bacterial tubulin homolog FtsZ, a core component of the bacterial cell division apparatus, by its… read more here.
Keywords: caps plus; end ftsz; mipz caps; ftsz ... See more keywords
A mechanism of salt bridge–mediated resistance to FtsZ inhibitor PC190723 revealed by a cell-based screen
Sign Up to like & getrecommendations! Published in 2022 at "Molecular Biology of the Cell"
DOI: 10.1091/mbc.e22-12-0538
Abstract: Bacterial cell division proteins, especially the tubulin homolog FtsZ, have emerged as strong targets for developing new antibiotics. Here, we have utilized the fission yeast heterologous expression system to develop a cell-based assay to screen… read more here.
Keywords: pc190723; cell based; cell; resistance ... See more keywords
Structure Based in Silico Screening Revealed a Potent Acinetobacter baumannii Ftsz Inhibitor from Asinex Antibacterial Library.
Sign Up to like & getrecommendations! Published in 2021 at "IEEE/ACM transactions on computational biology and bioinformatics"
DOI: 10.1109/tcbb.2021.3103899
Abstract: The superbug Acinetobacter baumannii is an increasingly prevalent pathogen of the intensive care units where its treatment is challenging. The identification of newer drug targets and the development of propitious therapeutics against this pathogen is… read more here.
Keywords: antibacterial library; structure based; asinex antibacterial; inhibitor ... See more keywords