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Antimicrobial Pepti...
Antimicrobial Peptides Incorporating Halogenated Marine-Derived Amino Acid Substituents
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- Craig, Alexander J. (author)
- Uppsala universitet,Läkemedelsdesign och läkemedelsutveckling,Institutionen för kemi - BMC
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- Ermolovich, Yuri (author)
- Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark
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- Cameron, Alan (author)
- Univ Auckland, Sch Chem Sci, Auckland 1010, New Zealand
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- Rodler, Agnes (author)
- Uppsala universitet,Institutionen för farmaci,Institutionen för läkemedelskemi
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- Wang, Helen (author)
- Uppsala universitet,Institutionen för medicinsk biokemi och mikrobiologi
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- Hawkes, Jeffrey A. (author)
- Uppsala universitet,Analytisk kemi
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- Hubert, Madlen (author)
- Uppsala universitet,Institutionen för farmaci
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- Bjöerkling, Fredrik (author)
- Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark
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- Molchanova, Natalia (author)
- Lawrence Berkeley Natl Lab, Mol Foundry, Berkeley, CA 94720 USA
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- Brimble, Margaret A. (author)
- Univ Auckland, Sch Chem Sci, Auckland 1010, New Zealand
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- Moodie, Lindon W. K. (author)
- Uppsala universitet,Läkemedelsdesign och läkemedelsutveckling
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- Svenson, Johan (author)
- Cawthron Inst, Nelson 7010, New Zealand
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(creator_code:org_t)
- American Chemical Society (ACS), 2023
- 2023
- English.
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In: ACS Medicinal Chemistry Letters. - : American Chemical Society (ACS). - 1948-5875. ; 14:6, s. 802-809
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- Small synthetic mimics of cationic antimicrobial peptides represent a promising class of compounds with leads in clinical development for the treatment of persistent microbial infections. The activity and selectivity of these compounds rely on a balance between hydrophobic and cationic components, and here, we explore the activity of 19 linear cationic tripeptides against five different pathogenic bacteria and fungi, including clinical isolates. The compounds incorporated modified hydrophobic amino acids inspired by motifs often found in bioactive marine secondary metabolites in combination with different cationic residues to probe the possibility of generating active compounds with improved safety profiles. Several of the compounds displayed high activity (low mu M concentrations), comparable with the positive controls AMC-109, amoxicillin, and amphotericin B. A higher activity was observed against the fungal strains, and a low in vitro off-target toxicity was observed against erythrocytes and HeLa cells, thereby illustrating effective means for tuning the activity and selectivity of short antimicrobial peptides.
Subject headings
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- Halogenated
- Synthesis
- Antimicrobial Peptide
- Marine Natural Products
- Bromotyrosine
Publication and Content Type
- ref (subject category)
- art (subject category)
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- By the author/editor
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Craig, Alexander ...
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Ermolovich, Yuri
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Cameron, Alan
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Rodler, Agnes
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Wang, Helen
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Hawkes, Jeffrey ...
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show more...
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Hubert, Madlen
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Bjöerkling, Fred ...
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Molchanova, Nata ...
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Brimble, Margare ...
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Moodie, Lindon W ...
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Svenson, Johan
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- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Chemical Science ...
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and Organic Chemistr ...
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Biological Scien ...
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and Biochemistry and ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Medicinal Chemis ...
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Basic Medicine
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and Pharmaceutical S ...
- Articles in the publication
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ACS Medicinal Ch ...
- By the university
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Uppsala University