Corona virus disease 2019 (COVID-19) is a respiratory disease caused by a new coronavirus (SARS-CoV-2) which causes significant morbidity and mortality. The emergence of this novel and highly pathogenic SARS-CoV-2 and its rapid international spread poses a serious global public health emergency. To date 32,174,627 cases, of which 962,613 (2.
View Article and Find Full Text PDFEur J Drug Metab Pharmacokinet
August 2019
Background And Objectives: Since there is no clear evidence in the literature to show how non-modified single-stranded DNA (ssDNA) drugs are metabolized in humans, we assessed the metabolism of BC 007, an ssDNA therapeutic, under development as a neutralizer of autoantibodies against G-protein-coupled receptors. In-vitro, investigating its stability in monkey plasma and serum, a successive 3'-exonuclease degradation resulting in several n-x degradation products has been previously reported. Here, we investigated the metabolism of BC 007 in humans after intravenous application to autoantibody-positive healthy subjects, in line with Phase I safety testing.
View Article and Find Full Text PDFPossible unwanted folding of biopharmaceuticals during manufacturing and storage has resulted in analysis schemes compared to small molecules that include bioanalytical characterization besides chemical characterization. Whether bioanalytical characterization is required for nucleotide-based drugs, may be decided on a case-by-case basis. Nucleotide-based pharmaceuticals, if chemically synthesized, occupy an intermediate position between small-molecule drugs and biologics.
View Article and Find Full Text PDFA 2,3-diaminophenazine bis-urea fluorescent probe monomer (1) was developed. It responds to phenylphosphate and phosphorylated amino acids in a ratiometric fashion with enhanced fluorescence accompanied by the development of a redshifted emission band arising from an excited-state proton transfer (ESPT) process in the hydrogen-bonded probe/analyte complex. The two urea groups of 1 form a cleft-like binding pocket (K >10 L mol for 1:2 complex).
View Article and Find Full Text PDFThe closely related to the Pseudomonas orientalis strain Pseudomonas sp. acc. no.
View Article and Find Full Text PDFThe measurement of biologically relevant anions, such as fluoride, is an important task in analytical chemistry, in particular, for dental health and osteoporosis. Although a large number of fluoride probes are known, the applicability under relevant conditions is limited to a few examples. To improve this situation, BODIPY-amidothiourea dyes with varying hydrogen-bond donating strengths were developed, the most H-acidic of which (1 c) could detect F(-) from an inorganic source (NaF) in 50 % aqueous solution (DMSO/water 1:1, v/v) with 0.
View Article and Find Full Text PDFTo prevent aspartimide formation and related side products in Asp-Xaa, particularly Asp-Gly-containing peptides, usually the 2-hydroxy-4-methoxybenzyl (Hmb) backbone amide protection is applied for peptide synthesis according to the Fmoc-protocols. In the present study, the usefulness of the recently proposed acid-labile dicyclopropylmethyl (Dcpm) protectant was analyzed. Despite the significant steric hindrance of this bulky group, N-terminal H-(Dcpm)Gly-peptides are quantitatively acylated by potent acylating agents, and alternatively the dipeptide Fmoc-Asp(OtBu)-(Dcpm)Gly-OH derivative can be used as a building block.
View Article and Find Full Text PDFThe quantitative analysis of protein mixtures is pivotal for the understanding of variations in the proteome of living systems. Therefore, approaches have been recently devised that generally allow the relative quantitative analysis of peptides and proteins. Here we present proof of concept of the new metal-coded affinity tag (MeCAT) technique, which allowed the quantitative determination of peptides and proteins.
View Article and Find Full Text PDFProteasomes are known to produce major histocompatibility complex (MHC) class I ligands from endogenous antigens. The interferon-gamma-inducible proteasome activator PA28 plays an important role in the generation of MHC ligands by proteasomes. Generation of the HLA-A(*)0201 restricted melanoma antigen TRP2(360-368) by the proteasome has been shown to be dependent on the function of PA28 in vitro and in vivo (Sun, Y.
View Article and Find Full Text PDFA strategy for the rational design of a new optical sensor material for the selective recognition of long-chain carboxylates in water is presented. The approach relies on the combination of structure-property relationships to single out the optimal molecular sensor unit and the tuning of the sensing characteristics of an inorganic support material. A spacer-substituted 7-urea-phenoxazin-3-one was employed as the signaling moiety and a mesoporous trimethylsilylated UVM-7 (MCM-41 type) material served as the solid support.
View Article and Find Full Text PDFA charge transfer-type fluorescent molecular sensor consisting of a bisamidopyridine receptor and two styryl base chromophores shows H(2)PO(4)(-) and acetate-enhanced fluorescence due to the conversion of weak intramolecular hydrogen bonds into strong ones in the host-guest ensemble.
View Article and Find Full Text PDFA hyphenated HPLC-(1)H NMR method for the identification and quantification of PAHs in soil samples has been developed and applied to a PAH reference sample provided by the Federal Institute for Materials Research and Testing (BAM, Berlin, Germany). The results were compared with those obtained by HPLC-DAD, HPLC-F, and GC-MS analyses of the same sample.
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