Antibacterial Peptide Nucleic Acid-Antimicrobial Peptide (PNA-AMP) Conjugates: Antisense Targeting of Fatty Acid Biosynthesis
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Antibacterial Peptide Nucleic Acid-Antimicrobial Peptide (PNA-AMP) Conjugates : Antisense Targeting of Fatty Acid Biosynthesis. / Hansen, Anna Mette; Bonke, Gitte; Larsen, Camilla Josephine; Yavari, Niloofar; Nielsen, Peter E.; Franzyk, Henrik.
In: Bioconjugate Chemistry, Vol. 27, No. 4, 2016, p. 863-867.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Antibacterial Peptide Nucleic Acid-Antimicrobial Peptide (PNA-AMP) Conjugates
T2 - Antisense Targeting of Fatty Acid Biosynthesis
AU - Hansen, Anna Mette
AU - Bonke, Gitte
AU - Larsen, Camilla Josephine
AU - Yavari, Niloofar
AU - Nielsen, Peter E.
AU - Franzyk, Henrik
PY - 2016
Y1 - 2016
N2 - Antisense peptide nucleic acid (PNA) oligomers constitute a novel class of potential antibiotics that inhibit bacterial growth via specific knockdown of essential gene expression. However, discovery of efficient, nontoxic delivery vehicles for such PNA oligomers has remained a challenge. In the present study we show that antimicrobial peptides (AMPs) with an intracellular mode of action can be efficient vehicles for bacterial delivery of an antibacterial PNA targeting the essential acpP gene. The results demonstrate that buforin 2-A (BF2-A), drosocin, oncocin 10, Pep-1-K, KLW-9,13-a, (P59→W59)-Tat48-60, BF-2A-RXR, and drosocin-RXR are capable of transporting PNA effectively into E. coli (MICs of 1-4 μM). Importantly, presence of the inner-membrane peptide transporter SbmA was not required for antibacterial activity of PNA-AMP conjugates containing Pep-1-K, KLW-9,13-a, or drosocin-RXR (MICs of 2-4 μM).
AB - Antisense peptide nucleic acid (PNA) oligomers constitute a novel class of potential antibiotics that inhibit bacterial growth via specific knockdown of essential gene expression. However, discovery of efficient, nontoxic delivery vehicles for such PNA oligomers has remained a challenge. In the present study we show that antimicrobial peptides (AMPs) with an intracellular mode of action can be efficient vehicles for bacterial delivery of an antibacterial PNA targeting the essential acpP gene. The results demonstrate that buforin 2-A (BF2-A), drosocin, oncocin 10, Pep-1-K, KLW-9,13-a, (P59→W59)-Tat48-60, BF-2A-RXR, and drosocin-RXR are capable of transporting PNA effectively into E. coli (MICs of 1-4 μM). Importantly, presence of the inner-membrane peptide transporter SbmA was not required for antibacterial activity of PNA-AMP conjugates containing Pep-1-K, KLW-9,13-a, or drosocin-RXR (MICs of 2-4 μM).
U2 - 10.1021/acs.bioconjchem.6b00013
DO - 10.1021/acs.bioconjchem.6b00013
M3 - Journal article
C2 - 26938833
VL - 27
SP - 863
EP - 867
JO - Bioconjugate Chemistry
JF - Bioconjugate Chemistry
SN - 1043-1802
IS - 4
ER -
ID: 160107762