Search results for "inope"

The role of bestatin, an inhibitor of cell surface proteases, in the interaction of serum with untransformed cells in culture.

1981

Bestatin is an inhibitor of cell surface-associated aminopeptidase B and leucine aminopeptidase. This microbial product simulates the role of serum as an activator of uridine uptake in quiescent BHK cells. The compound significantly stimulates the incorporation of labelled thymidine into the acid-insoluble fraction of serum-starved Nil 8 cells in the presence of low concentration of serum. The possible mechanisms of these interactions are discussed.

Unnatural amino acids increase activity and specificity of synthetic substrates for human and malarial cathepsin C

2014

Mammalian cathepsin C is primarily responsible for the removal of N-terminal dipeptides and activation of several serine proteases in inflammatory or immune cells, while its malarial parasite ortholog dipeptidyl aminopeptidase 1 plays a crucial role in catabolizing the hemoglobin of its host erythrocyte. In this report, we describe the systematic substrate specificity analysis of three cathepsin C orthologs from Homo sapiens (human), Bos taurus (bovine) and Plasmodium falciparum (malaria parasite). Here, we present a new approach with a tailored fluorogenic substrate library designed and synthesized to probe the S1 and S2 pocket preferences of these enzymes with both natural and a broad ran…

Characterizing the N-terminal processing motif of MHC class I ligands.

2008

Abstract Most peptide ligands presented by MHC class I molecules are the product of an intracellular pathway comprising protein breakdown in the cytosol, transport into the endoplasmic reticulum, and successive N-terminal trimming events. The efficiency of each of these processes depends on the amino acid sequence of the presented ligand and its precursors. Thus, relating the amino acid composition N-terminal of presented ligands to the sequence specificity of processes in the pathway gives insight into the usage of ligand precursors in vivo. Examining the amino acid composition upstream the true N terminus of MHC class I ligands, we demonstrate the existence of a distinct N-terminal proces…

Rektummelanome – Stellenwert der modernen Therapie

2008

Rectal melanoma is a rare disease. There is much controversy concerning cause, incidence and treatment of the disease and the spreading of recurrence. In this article, we discuss actual aspects of diagnostic, therapy and prognosis on the basis of our series of seven patients as well as a literature review. The surgical therapy in the form of local tumour excision with a disease-free margin of up to 1-2 cm is the initial therapeutic modality of choice. Large tumours that obviously could not be removed in sano should be treated with a multimodal concept. Such tumours should be treated by a combination of neoadjuvant radiation and chemotherapy for down-staging with subsequent local excision (L…

Novel Penicillin-Type Analogues Bearing a Variable Substituted 2-Azetidinone Ring at Position 6: Synthesis and Biological Evaluation

2015

The synthesis and the biological activity of novel semi-synthetic β-lactam compounds containing an azetidinone moiety joined to the amino-nitrogen of the (+)-6-aminopenicillanic acid (6-APA) as new antibacterial agents is reported. The synthesized compounds were screened for their in vitro antimicrobial activity against a panel of Gram positive and Gram negative pathogens and environmental bacteria. Tested compounds displayed good antimicrobial activity against all tested Gram positive bacteria and for Staphylococcus aureus and Staphylococcus epidermidis antimicrobial activity resulted higher than that of the reference antibiotic. Additionally, in vitro cytotoxic screening was also carried …

La vita e l’azione. Il carattere moderno del biografico italiano

2022

Usually, fictional biography – both written or filmed – seems to trace back the distinctive aspect of a certain life only into the sphere of the activity characterizing it. In this sense, the biographical fiction considers an individual life as an exemplary moment to analyze to superimposition between oeuvre and operation, action and production, always linkable to an end. But what happens when the center of the narration is occupied by the absence of action, of any actions? Through Giorgio Agamben’s interpretation of Aristotle’s categories of oeuvre and action, this paper aims to define a paradigm of inoperosity in Italian biographical cinema to highlight its peculiar modern character and s…

Trattamento delle piastrinopenie: esperienza annuale

2010

CCDC 1875843: Experimental Crystal Structure Determination

2019

Related Article: Oana Moncea, Juan Casanova-Chafer, Didier Poinsot, Lukas Ochmann, Clève D. Mboyi, Houssein O. Nasrallah, Eduard Llobet, Imen Makni, Molka El Atrous, Stéphane Brandès, Yoann Rousselin, Bruno Domenichini, Nicolas Nuns, Andrey A. Fokin, Peter R. Schreiner, Jean-Cyrille Hierso|2019|Angew.Chem.,Int.Ed.|58|9933|doi:10.1002/anie.201903089

Individual stereoisomers of phosphinic dipeptide inhibitor of leucine aminopeptidase

2008

Abstract Individual stereoisomers of the phosphinic pseudodipeptide hPheψ[P(O)(OH)CH2]Phe were obtained by stereoselective liquid chromatographic separation as N- and C-terminally protected derivative on quinidine carbamate modified silica stationary phase. The stereoisomeric purity, exceeding 95% for each fraction, was determined before and after deprotection using two independent methods. The absolute configuration was rationally assigned by application of enantiomerically pure phosphinic acid substrates in the synthetic procedure and correlation with biological activity of the products. Substantial differences in inhibition of leucine aminopeptidase by the individual isomers revealed nov…

Determinants essential for the transmissible gastroenteritis virus-receptor interaction reside within a domain of aminopeptidase-N that is distinct f…

1994

The swine-specific coronavirus transmissible gastroenteritis virus (TGEV) uses pig aminopeptidase-N (pAPN) as a cellular receptor. We showed that the human aminopeptidase-N (hAPN) cannot substitute for pAPN in this respect, although the two enzymes have 80% amino acid sequence identity. In order to map the TGEV binding site on pAPN, we constructed a series of APN cDNA chimeras between pAPN and hAPN and analyzed them for their capacity to confer infectivity. The region between residues 717 and 813 was found to be essential for infectivity. This region also contains the epitopes for three TGEV-blocking monoclonal antibodies directed against pAPN. These data support the view that the catalytic…