Search results for "aminopeptidase"
showing 10 items of 56 documents
Phosphinotripeptidic Inhibitors of Leucylaminopeptidases
2021
Phosphinate pseudopeptide are analogs of peptides containing phosphinate moiety in a place of the amide bond. Due to this, the organophosphorus fragment resembles the tetrahedral transition state of the amide bond hydrolysis. Additionally, it is also capable of coordinating metal ions, for example, zinc or magnesium ions. These two properties of phosphinate pseudopeptides make them an ideal candidate for metal-related protease inhibitors. This research investigates the influence of additional residue in the P2 position on the inhibitory properties of phosphinopeptides. The synthetic strategy is proposed, based on retrosynthetic analysis. The N-C-P bond formation in the desired compounds is …
Constitutive Activation of the Midgut Response to Bacillus thuringiensis in Bt-Resistant Spodoptera exigua
2010
Bacillus thuringiensis is the most effective microbial control agent for controlling numerous species from different insect orders. The main threat for the long term use of B. thuringiensis in pest control is the ability of insects to develop resistance. Thus, the identification of insect genes involved in conferring resistance is of paramount importance. A colony of Spodoptera exigua (Lepidoptera: Noctuidae) was selected for 15 years in the laboratory for resistance to Xentari (TM), a B. thuringiensis-based insecticide, reaching a final resistance level of greater than 1,000-fold. Around 600 midgut ESTs were analyzed by DNA-macroarray in order to find differences in midgut gene expression …
Brief Report: Functional Interaction of Endoplasmic Reticulum Aminopeptidase 2 and HLA-B27 Activates the Unfolded Protein Response.
2017
Objective: The basic mechanisms underlying the pathogenesis of ankylosing spondylitis (AS) remain unresolved. We previously reported an association of the single-nucleotide polymorphism (SNP) rs2549782 in the endoplasmic reticulum aminopeptidase 2 gene (ERAP2) with AS. It is known that patients homozygous for the G allele (GG) of another ERAP2 SNP, rs2248374, lack expression of ERAP2 (ERAP2 null). The present study utilized this information to study the impact of ERAP2 deficiency on HLAâB27 expression in patients with AS, specifically focusing on the functional interaction of ERAP2 and HLAâB27 in peripheral blood mononuclear cells (PBMCs) from patients with AS and assessing the effects …
Disease-associated polymorphisms in ERAP1 do not alter endoplasmic reticulum stress in patients with ankylosing spondylitis
2014
The mechanism by which human leukocyte antigen B27 (HLA-B27) contributes to ankylosing spondylitis (AS) remains unclear. Genetic studies demonstrate that association with and interaction between polymorphisms of endoplasmic reticulum aminopeptidase 1 (ERAP1) and HLA-B27 influence the risk of AS. It has been hypothesised that ERAP1-mediated HLA-B27 misfolding increases endoplasmic reticulum (ER) stress, driving an interleukin (IL) 23-dependent, pro-inflammatory immune response. We tested the hypothesis that AS-risk ERAP1 variants increase ER-stress and concomitant pro-inflammatory cytokine production in HLA-B27(+) but not HLA-B27(-) AS patients or controls. Forty-nine AS cases and 22 healthy…
The Extracellular Vesicles of the Helminth Pathogen, Fasciola hepatica : Biogenesis Pathways and Cargo Molecules Involved in Parasite Pathogenesis
2015
Extracellular vesicles (EVs) released by parasites have important roles in establishing and maintaining infection. Analysis of the soluble and vesicular secretions of adult Fasciola hepatica has established a definitive characterisation of the total secretome of this zoonotic parasite. Fasciola secretes at least two sub-populations of EVs that differ according to size, cargo molecules and site of release from the parasite. The larger EVs are released from the specialised cells that line the parasite gastrodermus and contain the zymogen of the 37 kDa cathepsin L peptidase that performs a digestive function. The smaller exosome-like vesicle population originate from multivesicular bodies with…
Selective inhibition of binding of Bacillus thuringiensis Cry1Ab toxin to cadherin-like and aminopeptidase proteins in brush-border membranes and dis…
2007
Binding analyses with denatured epithelial membrane proteins from Bt (Bacillus thuringiensis) demonstrated at least two kinds of proteins, APNs (aminopeptidases N) and cadherin-like proteins, as possible receptors for the Cry1A class of Bt toxins. Two alternative models have been proposed, both based on initial toxin binding to a cadherin-like protein, but one involving APN and the other not. We have used two Bombyx mori strains (J65 and Kin), which are highly susceptible to Cry1Ab, to study the role of these two types of receptors on Cry1Ab toxin binding and cytotoxicity by means of the inhibitory effect of antibodies. BBMVs (brush-border membrane vesicles) of strain J65 incubated with lab…
Peptidases in Germinating Barley Grain: Properties, Localization and Possible Functions
2008
Barley grain contains about 10% insoluble reserve proteins. When the grain germinates the reserve proteins are hydrolysed to amino acids and transported to the growing tissues of the seedling. In the resting grain most of the reserve proteins are 'packed' into the non-living storage tissue, the starchy endosperm. During germination the internal pH of the starchy endosperm is about 5, and it contains high activities of proteinases (secreted by the living aleurone cells) and carboxypeptidases, all with pH optima between 4 and 6. As a whole the starchy endosperm of a germinating grain resembles a giant secondary lysosome. Adjacent to the starchy endosperm is a specialized absorptive and proces…
Spectrophotometric and voltammetric determination of 2,5-dimethylaniline as potential product of enzymatic splitting of XY-2,5-dimethylanilide type s…
1999
A method for determination of 2,5-dimethylaniline is proposed. The procedure enables both spectrophotometrical and voltammetric measurements. The spectrophotometrical determination at λmax = 385.8 nm is possible for concentrations up to 1.25 × 10-6 mol l-1. The voltammetric method takes more time, however, due to the adsorptive enrichment of the substrate it is possible to determine concentrations in the range of 10-7 mol l-1). In the paper the optimal conditions and parameters for the determination are suggested.
Hydrolytic enzymes in the coelomic cells of the polychaeteNereis virens during sexual maturation
1991
Nereis virens were collected between April 1989 and April 1990 at Yerseke, Oosterscheldt Bay, The Netherlands. Activities of the hydrolytic enzymes arylsulfatase, acid phosphatase, N-acetylglucosaminidase, aminopeptidase, and carboxylesterase were investigated in coelomic cells (elaeocytes) of individuals at different stages of maturation as determined by the time course of oocyte growth. On a protein-content basis, up to ten-fold higher specific activities were present in the elaeocytes compared to the body-wall tissue. Acid phosphatase, N-acetylglucosaminidase, leucine aminopeptidase, and long- and medium-chain esterase increased continuously from the beginning to the later stage of sexua…
In situ formation of pyronin dyes for fluorescence protease sensing
2017
International audience; We report a reaction-based strategy for the fluorogenic detection of protease activity. Based on the "covalent-assembly" probe design principle recently put forward by the Yang group for detection of Sarin related threats (J. Am. Chem. Soc., 2014, 136, 6594-6597), we have designed two unusual nonfluorescent caged precursors (mixed bis-aryl ethers) which are readily converted into a fluorescent unsymmetrical pyronin dye through a domino cyclisation-aromatisation reaction triggered by penicillin G acylase (PGA) or leucine aminopeptidase (LAP). Fluorescence-based in vitro assays and HPLCfluorescence/- MS analyses support the claimed activation mechanism whose the furthe…