87512-31-0Relevant articles and documents
Alaninyl variants of the marine natural product halocyamine A and their antibacterial properties
Fong, Hugo K.H.,Cadelis, Melissa M.,Brunel, Jean Michel,Bourguet-Kondracki, Marie-Lise,Barker, David,Copp, Brent R.
, p. 6929 - 6938 (2018)
In an effort to explore the antibacterial potential of the marine natural product halocyamine A, a series of analogues including desbromo and alanine-substituted variants were synthesised and evaluated for biological activity against a panel of Gram-positive and –negative bacteria. The analogues were synthesised by a combination of solid-phase peptide synthesis and ruthenium complex/ytterbium triflate catalysed hydroamidation chemistry. Single alanine substitutions ([Ala1]-halocyamine A and [Ala2]-halocyamine A) gave only modest increases in activity towards Gram-positive bacteria, while di-alaninyl variants exhibited more potent activity with MIC values of 12.5–50 μM towards the Gram-positive bacteria Staphylococcus aureus and Enterococcus faecalis. A lipophilic trityl-protected intermediate of [Ala2]-halocyamine was the most active against the Gram-negative bacterium Escherichia coli.
ANTI-EGFR ANTIBODY DRUG CONJUGATES
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Paragraph 0936, (2019/06/07)
The invention relates to anti-Epidermal Growth Factor Receptor (EGFR) antibody drug conjugates (ADCs) which inhibit Bcl-xL, including compositions and methods of using said ADCs.
Localized Supramolecular Peptide Self-Assembly Directed by Enzyme-Induced Proton Gradients
Rodon Fores, Jennifer,Martinez Mendez, Miguel Leonardo,Mao, Xiyu,Wagner, Déborah,Schmutz, Marc,Rabineau, Morgane,Lavalle, Philippe,Schaaf, Pierre,Boulmedais, Fouzia,Jierry, Lo?c
supporting information, p. 15984 - 15988 (2017/11/22)
Electrodes are ideal substrates for surface localized self-assembly processes. Spatiotemporal control over such processes is generally directed through the release of ions generated by redox reactions occurring specifically at the electrode. The so-used gradients of ions proved their effectiveness over the last decade but are in essence limited to material-based electrodes, considerably reducing the scope of applications. Herein is described a strategy to enzymatically generate proton gradients from non-conductive surfaces. In the presence of oxygen, immobilization of glucose oxidase (GOx) on a multilayer film provides a flow of protons through enzymatic oxidation of glucose by GOx. The confined acidic environment located at the solid–liquid interface allows the self-assembly of Fmoc-AA-OH (Fmoc=fluorenylmethyloxycarbonyl and A=alanine) dipeptides into β-sheet nanofibers exclusively from and near the surface. In the absence of oxygen, a multilayer nanoreactor containing GOx and horseradish peroxidase (HRP) similarly induces Fmoc-AA-OH self-assembly.