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  Caulerpenyne and related bis-enol esters are novel-type inhibitors of human 5-lipoxygenase

Richter, P., Schubert, G., Schaible, A. M., Cavas, L., Werz, O., & Pohnert, G. (2014). Caulerpenyne and related bis-enol esters are novel-type inhibitors of human 5-lipoxygenase. ChemMedChem, 9(8), 1655-1659. doi:10.1002/cmdc.201402065.

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Item Permalink: https://hdl.handle.net/21.11116/0000-0003-7D38-3 Version Permalink: https://hdl.handle.net/21.11116/0000-0003-7D3A-1
Genre: Journal Article

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EXT626.pdf (Publisher version), 251KB
 
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EXT626s1.pdf (Supplementary material), 226KB
 
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 Creators:
Richter, Phillipp, Author
Schubert, Gregor, Author
Schaible, Anja Maria, Author
Cavas, Levent, Author
Werz, Oliver, Author
Pohnert, Georg1, Author           
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1External Organizations, ou_persistent22              

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Free keywords: 15-LIPOXYGENASE; TAXIFOLIA; ANTIOXIDANTPharmacology & Pharmacy; caulerpenyne; inhibition; lipoxygenase; structure activity; synthetic analogues;
 Abstract: Caulerpenyne (CYN) is a sesquiterpene from green algae with known inhibitory properties against soybean lipoxygenase. Here we introduce a detailed structure-activity study elucidating the inhibitory effects of CYN and a library of six synthetic CYN analogues on isolated human 5-lipoxygenase (5-LO) and cellular 5-LO in polymorphonuclear leukocytes. Essential structural elements are identified and a structurally simplified inhibitor is introduced. The modes of 5-LO inhibition by CYN and the synthetic inhibitors cannot be assigned to any of the known categories of lipoxygenase inhibitors. These compounds clearly interfere directly with 5-LO and represent rather small and flexible molecules, with unique structures among 5-LO inhibitors identified thus far.

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Language(s): eng - English
 Dates: 2014
 Publication Status: Issued
 Pages: 5
 Publishing info: -
 Table of Contents: -
 Rev. Type: -
 Identifiers: DOI: 10.1002/cmdc.201402065
Other: EXT626
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Title: ChemMedChem
  Other : ChemMedChem
Source Genre: Journal
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Publ. Info: Weinheim, Germany : Wiley-VCH
Pages: - Volume / Issue: 9 (8) Sequence Number: - Start / End Page: 1655 - 1659 Identifier: ISSN: 1860-7179
CoNE: https://pure.mpg.de/cone/journals/resource/954925399508