Search results for "Hydroxamate"
showing 5 items of 5 documents
Delivering Inorganic and Organic Reagents and Enzymes from Zein and Developing Optical Sensors.
2018
Nowadays, interest in using environmentally friendly materials is increasing in many fields. However, the rational design of sensors with biodegradable materials is a challenge. The main aim of this work is to show the possibility of using zein, a protein from corn, as a biodegradable and low-cost material for immobilizing, stabilizing, and delivering different kind of reagents for developing optical sensors. Enzymes, metallic salts, and aromatic and small organic compounds were tested. In addition, different techniques of immobilization, entrapment and adsorption, were used, and different formats, such as solid devices and also multiwell platforms, were proposed. The capacity of zein for i…
A Primary Evaluation of Potential Small-Molecule Inhibitors of the Astacin Metalloproteinase Ovastacin, a Novel Drug Target in Female Infertility Tre…
2020
Abstract Despite huge progress in hormonal therapy and improved in vitro fertilization methods, the success rates in infertility treatment are still limited. A recently discovered mechanism revealed the interplay between the plasma protein fetuin‐B and the cortical granule‐based proteinase ovastacin to be a novel key mechanism in the regulation of fertilization. Upon sperm–egg fusion, cleavage of a distinct zona pellucida component by ovastacin destroys the sperm receptor, enhances zona robustness, and eventually provides a definitive block against polyspermy. An untimely onset of this zona hardening prior to fertilization would consequently result in infertility. Physiologically, this proc…
Heteroaromatic Inhibitors of the Astacin Proteinases Meprin α, Meprin β and Ovastacin Discovered by a Scaffold-Hopping Approach.
2020
Abstract Astacin metalloproteinases, in particular meprins α and β, as well as ovastacin, are emerging drug targets. Drug‐discovery efforts have led to the development of the first potent and selective inhibitors in the last few years. However, the most recent compounds are based on a highly flexible tertiary amine scaffold that could cause metabolic liabilities or decreased potency due to the entropic penalty upon binding to the target. Thus, the aim of this study was to discover novel conformationally constrained scaffolds as starting points for further inhibitor optimization. Shifting from flexible tertiary amines to rigid heteroaromatic cores resulted in a boost in inhibitory activity. …
Influence of structural elements on iron(III) chelating properties in a new series of amino acid-derived monohydroxamates
2018
Abstract A series of amino acid-derived monohydroxamate compounds A1 – A7 was synthesized and characterized for their coordination properties of Fe(III). The series varies in their skeletal lengths and compositions; some compounds lack external substituents, others are substituted with external functional amino or carboxylic groups, or alternatively inert methyl. Undertaken investigations allowed the determination of stoichiometry, stability constants and spectroscopic parameters of formed ferric complexes. Incorporation of an external functional group with a dissociable proton affects the coordination behavior; the presence of carboxylic or amino groups hampers the formation of mono-, di- …
Complex formation of copper(II), nickel(II) and zinc(II) with ethyl phosphonohydroxamic acid : solution speciation, synthesis and structural characte…
2019
The first example of a Cu(II) 12-MC-4 hydroxamic metallacrown containing an ethylphosphonate group as an additional donor function in the β-position with respect to the hydroxamic group is described. The solution equilibrium of ethylphosphonoacetohydroxamic acid (PAHEt) with Cu(II) was investigated in aqueous solution by a combination of potentiometry, mass spectrometry, UV-Vis and EPR spectroscopies, and isothermal titration calorimetry. A model containing mononuclear [CuL], [CuL2]2− and [CuL2H−1]3− and pentanuclear [Cu5(LH−1)4]2− species is proposed. The predominance of the [Cu5(LH−1)4]2− species in solution over the pH range 4–9 was confirmed by the signals present in the ESI-MS spectra,…