장재원 교수

Serine hydrolases are one of the largest and most diverse enzyme classes in Nature. Inhibitors of serine hydrolases are used to treat many diseases, including obesity, diabetes, cognitive dementia, and bacterial and viral infections. Nonetheless, the majority of the 200+ serine hydrolases in mammals still lack selective inhibitors for their functional characterization. We and others have shown that activated carbamates, through covalent reaction with the conserved serine nucleophile of serine hy

Profiling enzyme activities: A selective, activity-based imaging probe is described for the integral membrane hydrolase KIAA1363 and used to determine the subcellular localization and half-life of this enzyme in human cancer cells (see picture). Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not respons

Platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3 are poorly characterized serine hydrolases that form a complex with a noncatalytic protein (1b1) to regulate brain development, spermatogenesis, and cancer pathogenesis. Determining physiological substrates and biochemical functions for the PAFAH1b complex would benefit from selective chemical probes that can perturb its activity in living systems. Here, we report a class of tetrahydropyridine reversible inhibitors of PAFAH1b2/3 di

Phosphorylation at aspartic acid residues represents an abundant and critical post-translational modification (PTM) in prokaryotes. In contrast to most characterized PTMs, such as phosphorylation at serine or threonine, the phosphoaspartate moiety is intrinsically labile, and therefore incompatible with common proteomic profiling methods. Herein, we report a nucleophilic, desthiobiotin-containing hydroxylamine (DBHA) chemical probe that covalently labels modified aspartic acid residues in native

Metabolomic profiling studies aim to provide a comprehensive, quantitative, and dynamic portrait of the endogenous metabolites in a biological system. While contemporary technologies permit routine profiling of many metabolites, intrinsically labile metabolites are often improperly measured or omitted from studies due to unwanted chemical transformations that occur during sample preparation or mass spectrometric analysis. The primary glycolytic metabolite 1,3-bisphosphoglyceric acid (1,3-BPG) ty

Abstract Herein, we report the development of an 18 F‐labeled, activity‐based small‐molecule probe targeting the cancer‐associated serine hydrolase NCEH1. We undertook a focused medicinal chemistry campaign to simultaneously preserve potent and specific NCEH1 labeling in live cells and animals, while permitting facile 18 F radionuclide incorporation required for PET imaging. The resulting molecule, [ 18 F]JW199, labels active NCEH1 in live cells at nanomolar concentrations and greater than 1000‐

Enzymaktivitäten: Eine selektive, aktivitätsbasierte Sonde, die das integrale Membranhydrolase-Enzym KIAA1363 abbilden kann, wird beschrieben und zur subzellulären Lokalisation sowie zur Bestimmung der Halbwertszeit des Enzyms in Krebszellen verwendet (siehe Bild).

Photoacoustic imaging (PAI) is an emerging modality in biomedical imaging with superior imaging depth and specificity. However, PAI still has significant limitations, such as the background noise from endogenous chromophores. To overcome these limitations, we developed a covalent activity-based PAI probe, NOx-JS013, targeting NCEH1. NCEH1, a highly expressed and activated serine hydrolase in aggressive cancers, has the potential to be employed for the diagnosis of cancers. We show that NOx-JS013

Morphologies of bamboo-shaped multiwalled carbon nanotubes (BS-MWNTs) grown on Fe catalyst deposited onto SiO2/Tisubstrates by thermal chemical vapor deposition were investigated by means of atomic force microscopy (AFM) and lateral forcemicroscopy (LFM). For the structural speciality, the bamboo structures were more distinctly observed by LFM

The current study investigates the problems of subject observed in The Skin I Live In, directed by Pedro Almodovar in 2011. One of the oldest philosophical questions held by people is: “Who am I?” or “What is the essence of humanity?” Breaking away from traditional Western philosophy that identified humans as rational beings, the contemporary philosophy since the advent of phenomenology views humans as beings of corporeal and generative beings. Among such discourse about the corporeal taking pla

Abstract Phosphorylation at aspartic acid residues represents an abundant and critical post‐translational modification (PTM) in prokaryotes. In contrast to most characterized PTMs, such as phosphorylation at serine or threonine, the phosphoaspartate moiety is intrinsically labile, and therefore incompatible with common proteomic profiling methods. Herein, we report a nucleophilic, desthiobiotin‐containing hydroxylamine (DBHA) chemical probe that covalently labels modified aspartic acid residues

The purpose of this study is to analyze the change in social consciousness after the outbreak of the Black Death, which was revealed in the late medieval Spanish poem Danza General de la muerte, and to reflect on its significance. As is well known, the Black Death Pandemic sacrificed nearly a third of Europe's population between 1347 and 1351, and was taken a significant opportunity to accelerate the transition from the Middle Ages to the Renaissance. Danza de la muerte as new motif in literatur