Search results for "DASE"
showing 10 items of 1891 documents
Phosphonic Analogues of Phenylglycine as Inhibitors of Aminopeptidases: Comparison of Porcine Aminopeptidase N, Bovine Leucine Aminopeptidase and Ami…
2019
Inhibitory activity of 14 phosphonic analogues of phenylglycine, substituted in aromatic ring by fluorine and chlorine, was determined towards porcine aminopeptidase N. The obtained data served as a basis for studying their interaction with the enzyme as modelled by the use of Schrödinger Release 2018 program. The observed linearity between modelled Gibbs free energy differences and inhibitory constants indicated the usefulness of this program. The obtained binding mode was compared with this modelled for bovine lens leucine aminopeptidase. Although both enzymes differ in the number of zinc ions present in the active site, they are considered to exhibit similar activity towards sub…
Reactivity of Neutral Mo(S2C6H4)3 in Aqueous Media: an Alternative Functional Model of Sulfite Oxidase.
2009
The kinetics of the reaction of neutral [Mo(S2C6H4)3] with hydrogen sulfite to produce the anionic Mo(V) complex, [Mo(S2C6H4)3]-, and sulfate have been investigated. It has been shown that [Mo(S2C6H4)3] acts as the electron-proton sink in the oxygenation reaction of HSO3(-) by water. Reaction rates, monitored by UV/vis stopped-flow spectrometry, were studied in THF/water media as a function of the concentration of HSO3(-) and molybdenum complex, pH, ionic strength, and temperature. The reaction exhibits pH-dependent HSO3(-) saturation kinetics, and it is first-order in complex concentration. The kinetic data and MS-ESI spectra are consistent with the formation of [Mo O(S2C6H4)2(S2C6H5)]- (1…
Novel Hydrazine Molecules as Tools To Understand the Flexibility of Vascular Adhesion Protein-1 Ligand-Binding Site: Toward More Selective Inhibitors
2011
Vascular adhesion protein-1 (VAP-1) belongs to a family of amine oxidases. It plays a role in leukocyte trafficking and in amine compound metabolism. VAP-1 is linked to various diseases, such as Alzheimer's disease, psoriasis, depression, diabetes, and obesity. Accordingly, selective inhibitors of VAP-1 could potentially be used to treat those diseases. In this study, eight novel VAP-1 hydrazine derivatives were synthesized and their VAP-1 and monoamine oxidase (MAO) inhibition ability was determined in vitro. MD simulations of VAP-1 with these new molecules reveal that the VAP-1 ligand-binding pocket is flexible and capable of fitting substantially larger ligands than was previously believ…
Animal Models of Stress - Current Knowledge and Potential Directions
2021
Finding new therapies and new antidepressant agents is of high clinical priority given that many cases of depressive disorder do not respond to conventional monoaminergic antidepressants such as selective serotonin reuptake inhibitors, tricyclic antidepressants, and monoamine oxidase inhibitors The authors demonstrated that electroacupuncture and fluoxetine, a second-generation antidepressant categorized as a selective serotonin reuptake inhibitor (Perez-Caballero et al , 2014), regulate the expression of key proteins in the calmodulin kinase (CAMK) signaling pathway, which are related to depression in the hippocampi of rats (Takemoto-Kimura et al , 2017;Xie et al , 2019) In a paper on “Sho…
Synthesis, structure and reactivity of trans-UO22+ complexes of OH-containing ligands †
2000
trans-Dioxouranium dinuclear complexes of a few OH-containing ligands possessing N-, O-binding sites were synthesized and characterised. Seven of these were also structurally characterised by single crystal X-ray diffraction. All these complexes exhibit symmetric U2O2 core structures in addition to having a seven-co-ordinated environment about each uranium centre. Even when the ligand possessed more than one CH2OH group, only one such group was found to be involved both in chelation as well as in bridging. These complexes exhibited facile transmetallation reactions with vanadium and molybdenum precursors. Though their core structures are alike, the complexes differ in their lattice arrangem…
A new genus and species of asteraceae-inhabiting aphid (hemiptera: aphididae) from Costa Rica and Mexico
2013
P. 323-331 Ucrimyzus villalobosi Mier Durante & Pérez Hidalgo gen. n., sp. n. (Hemiptera: Aphididae: Macrosiphini) are described from apterous and alate viviparous females collected on species of genera Bidens, Schkuhria, Senecio and Stevia (Asteraceae: Asteroideae) in Costa Rica and Mexico. Principal components analysis (PCA) was done to verify that the studied aphids belong to a single species regardless of their geographical origin or host plant. Molecular analyses were carried out on the sequences of a fragment of the mitochondrial gene encoding for cytochrome c oxidase subunit 1 (COI) and of a fragment of the nuclear gene encoding elongation factor 1α (EF1α). The taxonomic discussion t…
�ber das Verhalten der Leucin-Aminopeptidase-Aktivit�t im Blutserum bei Patienten mit malignen Tumoren im Mund- und Halsbereich
1959
Nach kurzen Hinweis auf Histotopographie und Bedeutung von Peptidasen im Carcinomgewebe wurde uber die Leucin-Aminopeptidase-Aktivitat des Blutserums bei 53 Patienten der Hals-Nasen-Ohrenklinik mit vorwiegend malignen epithelialen Tumoren (Carcinomen) im Mund- und Halsbereich berichtet. Von Fall zu Fall konnten grose Schwankungen der Leucin-Aminopeptidase-Aktivitat im Blutserum festgestellt werden. In etwa einem Drittel der Falle fanden sich erhohte, in einem Drittel normale und in einem weiteren Drittel gegenuber der Norm erniedrigte Leucin-Aminopeptidase-Aktivitaten im Blutserum, jeweils ohne das eine ausreichende Begrundung dafur angegeben werden konnte. Ausgedehnte und metastasierende C…
Machine Learning Unveils Proteotypic Mimicry in Genetically Defined SCN Variants
2019
Background Novel computational algorithms for multi-omics analysis bear great potential to highlight pathomechanisms of monogenic diseases. We recently defined the in-depth proteome of primary human neutrophil granulocytes (PMID 30630937). Here, we ask the question whether proteotypic patterns differ between defined genetic subtypes associated with severe congenital neutropenia (SCN). We focus on two novel genetic variants in constituents of the signal recognition particle (SRPRA and SRP19) and previously reported SCN genotypes SRP54, HAX1, and ELANE. Methods We analyzed proteomes of highly purified neutrophil granulocytes from a total of 26 SCN patients, including 5 with homozygous splice …
Leucine Aminopeptidase Activity in Mast Cells
1959
DURING investigations of the behaviour of leucine aminopeptidase activity of blood-serum in patients with dermatoses and tumours1–3, in a case of diffuse skin mastocytosis of a new-born, we detected heightened activity of leucine aminopeptidase. After mechanical friction of the affected skin, greater activity of leucine aminopeptidase occurred. From this we supposed a release of leucine aminopeptidase from the mast cell infiltrates of the skin. As is well known, in urticaria pigmentosa mechanical irritation of the skin lesions give rise to a degranulation of mast cells4,5 with liberation of histamine and serotonin. Indeed, there is no doubt that mast cells contain the enzyme leucine aminope…
Inhibitor of the Cytochrome Oxidase of Unfertilized Sea Urchin Eggs
1960
IN a previous communication1 the presence of an inhibitor of cytochrome oxidase in the unfertilized sea urchin egg was described. It was shown that its activity decreases considerably following fertilization, that it is a low-molecular compound, that it is heat- and alkali-labile and that its action is of a competitive type.