Anna Mette Hansen

Anna Mette Hansen
PolyPeptide Group · Process Development

PhD Chemistry

About

20
Publications
1,916
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427
Citations
Citations since 2017
11 Research Items
252 Citations
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201720182019202020212022202301020304050
201720182019202020212022202301020304050

Publications

Publications (20)
Article
Full-text available
Solid-phase synthesis of cyclic, branched or side-chain-modified peptides typically involves introduction of a residue carrying a temporary side-chain protecting group that undergoes selective on-resin removal. In particular, Nα-Fmoc-Nε-(4-methyltriphenylmethyl) (Mtt)-protected lysine and its shorter analogues are commercially available and extensi...
Chapter
Exploration of PNA-peptide conjugates as potential antisense antibiotics necessitates a fast and efficient synthesis protocols for amounts that facilitate determination of structure-activity relationships and in vivo studies in animal infection models. Fmoc/Boc-protected PNA monomers are here used for assembly of oligomers by optimized protocols in...
Chapter
Conjugation of a delivery peptide containing a thiol functionality (e.g., a cysteine residue) with a PNA oligomer displaying a single unprotected aliphatic primary amine (e.g., the N-terminus or a C-terminal lysine residue) can be achieved via a one-pot modification with a bisfunctional maleimide linker also displaying a reactive N-hydroxysuccinimi...
Article
Full-text available
Synthetic peptidomimetics may be designed to mimic functions of antimicrobial peptides, including potentiation of antibiotics, yet possessing improved pharmacological properties. Pairwise screening of 42 synthetic peptidomimetics combined with the antibiotics azithromycin and rifampicin in multidrug-resistant (MDR) Escherichia coli ST131 and Klebsi...
Article
Full-text available
α-Peptoids as well as peptide/α-peptoid hybrids and peptide/β-peptoid hybrids constitute major classes of proteolytically stable peptidomimetics that have been extensively investigated as mimetics of biologically active peptides. Representatives of lipidated peptide/β-peptoid hybrids have been identified as promising immunomodulatory lead compounds...
Article
Gram-negative bacterial pathogens are intrinsically resistant to several antibiotics that are not able to penetrate the cell envelope barrier. The aim of this study was to identify peptides that at low concentrations induce susceptibility to these antibiotics in multidrug-resistant (MDR) Gram-negative bacterial strains of clinical relevance. Pairwi...
Article
Mould and yeast contamination constitutes a major problem in food commodities, including dairy products, hence new natural preventive measures are in high demand. The aim of the current study is to identify and characterize novel antifungal peptides produced by lactic acid bacteria (LAB) in sour cream. By the use of a newly developed image-based 96...
Article
Emergence of antibiotic-resistant bacteria constitutes an increasing threat to human health. For example, treatment options for Staphylococcus aureus infections is declining with the worldwide spreading of highly virulent community-associated methicillin-resistant S. aureus (CA-MRSA) strains. Anti-virulence therapy has been proposed as an alternati...
Article
Structural optimization of a peptidomimetic antagonist of formyl peptide receptor 2 (FPR2) was explored by an approach involving combination of elements from the two most potent FPR2 antagonists described: a Rhodamine B-conjugated 10-residue gelsonin-derived peptide (i.e., PBP10: RhB-QRLFQVKGRR-OH) and the palmitoylated α-peptide/β-peptoid hybrid P...
Article
General conditions for efficient on-resin N-formylation of peptides were identified by screening of a number of reagents comprising aliphatic formates (ethyl formate, 2,2,2-trifluoroethyl formate, and cyanomethyl formate), aromatic esters (phenyl formate and p-nitrophenyl formate), and N-formylimidazole and in situ activation of formic acid with th...
Article
Antisense peptide nucleic acid (PNA) oligomers constitute a novel class of potential antibiotics that inhibit bacterial growth via specific knock-down of essential gene expression. However, discovery of efficient, non-toxic delivery vehicles for such PNA oligomers has remained a challenge. In the present study we show that antimicrobial peptides (A...
Article
The BODIPY-functionalized azide (V) can be successfully used in Cu-catalyzed 1,3-dipolar cycloadditions with terminal alkynes which gives an easy access to different substituted BODIPY derivatives.
Article
Full-text available
Novel azido- and amino-functionalised fluorescent probes based on the BODIPY framework have been developed. The probes can be easily and cheaply synthesised, exhibit the highly desirable BODIPY fluorescent properties, and are amenable to 'click' and peptide chemistry methodologies. These probes provide a stable and readily available tool amenable f...
Article
Full-text available
FFA2 is a G protein-coupled receptor that responds to short chain fatty acids and has generated interest as a therapeutic target for metabolic and inflammatory conditions. However, definition of its functions has been slowed by a dearth of selective ligands that can distinguish it from the closely related FFA3. At present, the only selective ligand...
Article
a b s t r a c t The suitability of chiral oxazolidinones in the SmI 2 -mediated C–C bond generation between the imide functionality of an N-acyl oxazolidinone unit and an olefinic radical acceptor, in both inter-and in-tramolecular reactions, was investigated. It was shown that the products from an Evans asymmetric alkylation can undergo direct car...
Article
In this work, mechanistic studies were performed to understand the SmI2/H2O-mediated coupling of N-acyl oxazolidinones with acrylates and acrylamides, providing gamma-keto esters and amides, respectively. Our results provide experimental evidence that C-C bond formation via intermolecular radical addition reactions to carbonyl substrates can be pro...
Article
The application of acyl radicals in radical addition reactions in the absence of a CO atmosphere is generally limited to aryl or alpha-unsubstituted alkyl acyl radicals due to competing decarbonylations where the rate constant for this degradation process surpasses 104 s-1. In this work, a potential solution to avoid the problem of decarbonylations...
Article
Full-text available
Manzamine A has been isolated from various Okinawa Sponges of the genus Haliclona and was first characterised by Higa and co-workers in 1986. The unusual and synthetically challenging structure consists of a pentacyclic core containing an array of 5-, 6-, 8-, and 13-membered rings with a pendant -carboline unit. The complex structure of manzamine A...

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Projects

Projects (2)
Project
Peptides are being explored as potential novel anti-infective agents that act via: (i) Direct antibacterial activity, (ii) Potentiation of traditional antibiotics (e.g., repurposing anti-Gram-positive drugs and/or re-sensitizing Gram-negative MDR strains), (iii) Interference with AgrC-based quorum sensing in S. aureus, (iv) Promoting bacterial uptake (e.g., of antisense PNA oligomers), and (v) Design and synthesis of PNA-peptide conjugates.
Project
The project aims at targeting multi-drug resistant bacteria and biofilm with proteolytically stable peptide analogs having an alternating cationic/hydrophobic design displaying amino acid and peptoid residues. Most recently, the research has focused on how side-chain length and hydrophobicity (including incorporation of fluorinated/halogenated residues) influence the antibacterial activity versus hemolytic and cytotoxic properties (i.e., the cell selectivity).