Recent advancements in mechanistic studies and structure activity relationship of FoF1 ATP synthase inhibitor as antimicrobial agent
Copyright © 2019 Elsevier Masson SAS. All rights reserved..
The emergence of drug resistance in infectious microbial strains can be overcome by development of novel drug molecules against unexploited microbial target. The success of Bedaquiline in recent years, as FoF1 ATP synthase inhibitor against XDR and MDR mycobacterium strains, has resulted in further exploration to identify more potent and safe drug molecules against resistant strains. FoF1 ATP synthase is the main energy production enzyme in almost all eukaryotes and prokaryotes. Development of bacterial ATP synthase inhibitors is a safe approach, without causing harm to mammalian cells due to structural difference between bacterial and mammalian ATP synthase target sites. This review emphasizes on providing the structural insights for FoF1 ATP synthase of different prokaryotes and will help in the design of new potent antimicrobial agents with better efficacy. Further, applications of synthetic and natural active antimicrobial ATP synthase inhibitors, reported by different research groups are summarized. Their SAR and mode of actions are also analysed.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:182 |
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| Enthalten in: |
European journal of medicinal chemistry - 182(2019) vom: 15. Nov., Seite 111644 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Narang, Rakesh [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 30.12.2019 Date Revised 30.12.2019 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2019.111644 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM301026742 |
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| 520 | |a Copyright © 2019 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a The emergence of drug resistance in infectious microbial strains can be overcome by development of novel drug molecules against unexploited microbial target. The success of Bedaquiline in recent years, as FoF1 ATP synthase inhibitor against XDR and MDR mycobacterium strains, has resulted in further exploration to identify more potent and safe drug molecules against resistant strains. FoF1 ATP synthase is the main energy production enzyme in almost all eukaryotes and prokaryotes. Development of bacterial ATP synthase inhibitors is a safe approach, without causing harm to mammalian cells due to structural difference between bacterial and mammalian ATP synthase target sites. This review emphasizes on providing the structural insights for FoF1 ATP synthase of different prokaryotes and will help in the design of new potent antimicrobial agents with better efficacy. Further, applications of synthetic and natural active antimicrobial ATP synthase inhibitors, reported by different research groups are summarized. Their SAR and mode of actions are also analysed | ||
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| 650 | 4 | |a FoF1 ATP synthase inhibitor | |
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| 650 | 4 | |a Oligomycin | |
| 650 | 4 | |a Peptides | |
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| 650 | 4 | |a Steroidal alkaloids | |
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| 700 | 1 | |a Kalra, Sourav |e verfasserin |4 aut | |
| 700 | 1 | |a Nayak, Surendra Kumar |e verfasserin |4 aut | |
| 700 | 1 | |a Khatik, Gopal L |e verfasserin |4 aut | |
| 700 | 1 | |a Kumar, Gadekula Naresh |e verfasserin |4 aut | |
| 700 | 1 | |a Sudhakar, Kalvatala |e verfasserin |4 aut | |
| 700 | 1 | |a Singh, Sachin Kumar |e verfasserin |4 aut | |
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