scholarly journals The selectivity of statine-based inhibitors against various human aspartic proteinases

1990 ◽  
Vol 265 (3) ◽  
pp. 871-878 ◽  
Author(s):  
R A Jupp ◽  
B M Dunn ◽  
J W Jacobs ◽  
G Vlasuk ◽  
K E Arcuri ◽  
...  
Keyword(s):  
Cathepsin D ◽  
Aspartic Proteinase ◽  
The Other ◽  
Aspartic Proteinases ◽  
Cathepsin E ◽  
Human Renin ◽  
Endothia Parasitica ◽  
Selection Of

The interactions of five human enzymes (renin, pepsin, gastricsin, cathepsin D and cathepsin E) and the aspartic proteinase from Endothia parasitica with several series of synthetic inhibitors were examined. All of the inhibitors contained the dipeptide analogue statine or its phenylalanine or cyclohexylalanine homologues in the P1-P1′ positions. The residues occupying the peripheral sub-sites (P4 to P3′) were varied systematically and inhibitory constants were determined for the interactions with each of the proteinases. Inhibitors were elucidated that specifically inhibited human renin and did not affect any of the other human enzymes or the fungal proteinase. With suitable selection of residues to occupy individual sub-sites, effective inhibitors of specific human aspartic proteinases may now be designed.

scholarly journals A new chromophoric substrate for penicillopepsin and other fungal aspartic proteinases

1982 ◽  
Vol 203 (3) ◽  
pp. 603-610 ◽  
Author(s):  
Theo Hofmann ◽  
Robert S. Hodges
Keyword(s):  
Catalytic Efficiency ◽  
Aspartic Proteinase ◽  
Spectrophotometric Assay ◽  
Water Soluble ◽  
Burst Release ◽  
Penicillium Roqueforti ◽  
Aspartic Proteinases ◽  
Catalytic Rate Constant ◽  
Human Renin ◽  
Hydrolysis Of

The hexapeptide N-α-acetylalanylalanyl-lysyl-p- nitrophenylalanylalanylalanylamide has been synthesized and was found to be a good substrate for fungal aspartic proteinases that possess trypsinogen-activating activity, namely penicillopepsin, Rhizopus aspartic proteinase, Endothia aspartic proteinase and the aspartic proteinases from Aspergillus oryzae and Penicillium roqueforti. The peptide is rapidly cleaved between the lysine and p-nitrophenylalanine residues. Calf chymosin and human renin cleave the same bond, but only very slowly. The cleavage is accompanied by an absorbance decrease with a maximum at 296nm (Δε —1800m−1·cm−1). Pig pepsin and the aspartic proteinases from two Rhizomucor species cleave the peptide slowly on the carboxy side of p-nitrophenylalanine. For the five enzymes that hydrolysed the peptide rapidly, Km values range from 0.16 to 0.42mm and kcat. from 6 to 46.6s−1 at pH 4.5 and 25°C. A comparison of the kinetic parameters of the hexapeptide with those of the dipeptide N-α-acetyllysyl-p-nitrophenylalanylamide obtained with penicillopepsin shows that at pH 6.0 the catalytic rate constant kcat. is over 5000-fold greater for the hexapeptide, whereas the Km values are essentially the same, showing that the catalytic efficiency is strongly dependent on secondary binding. The new substrate with a p-nitrophenylalanine residue in the P′1 position has advantages over previously used substrates for aspartic proteinases in that it offers a more sensitive spectrophotometric assay that is independent of pH up to 5.5 and can readily be used up to pH 7.0. The presence of lysine makes it very water-soluble. Stopped-flow spectrophotometric experiments with penicillopepsin gave clear evidence that the hydrolysis of the substrate by penicillopepsin is not accompanied by a ‘burst’ release of p-nitrophenylalanylalanylalanylamide.

scholarly journals Inhibition of aspartic proteinases by α2-macroglobulin

1989 ◽  
Vol 259 (3) ◽  
pp. 905-907 ◽  
Author(s):  
D J Thomas ◽  
A D Richards ◽  
J Kay
Keyword(s):  
Cathepsin D ◽  
Serine Proteinases ◽  
Cysteine Proteinases ◽  
Aspartic Proteinases ◽  
Protein Substrates ◽  
Cathepsin E ◽  
Α2 Macroglobulin

The effect of alpha 2-macroglobulin, one of the major antiproteinases in the plasma of vertebrates, on the action of the aspartic proteinases chymosin, cathepsin D and cathepsin E towards peptide and protein substrates at pH 6.2 was examined. Activities towards protein substrates were blocked, thus demonstrating that alpha 2-macroglobulin can inhibit aspartic proteinases, in addition to serine proteinases, cysteine proteinases and metalloproteinases.

Note on Selection of Coordinate Systems for Geodynamics

1975 ◽  
Vol 26 ◽  
pp. 395-407
Author(s):  
S. Henriksen
Keyword(s):  
Sea Level ◽  
The Other ◽  
Coordinate Systems ◽  
Mean Sea Level ◽  
The Earth ◽  
The One ◽  
Static Systems ◽  
Selection Of

The first question to be answered, in seeking coordinate systems for geodynamics, is: what is geodynamics? The answer is, of course, that geodynamics is that part of geophysics which is concerned with movements of the Earth, as opposed to geostatics which is the physics of the stationary Earth. But as far as we know, there is no stationary Earth – epur sic monere. So geodynamics is actually coextensive with geophysics, and coordinate systems suitable for the one should be suitable for the other. At the present time, there are not many coordinate systems, if any, that can be identified with a static Earth. Certainly the only coordinate of aeronomic (atmospheric) interest is the height, and this is usually either as geodynamic height or as pressure. In oceanology, the most important coordinate is depth, and this, like heights in the atmosphere, is expressed as metric depth from mean sea level, as geodynamic depth, or as pressure. Only for the earth do we find “static” systems in use, ana even here there is real question as to whether the systems are dynamic or static. So it would seem that our answer to the question, of what kind, of coordinate systems are we seeking, must be that we are looking for the same systems as are used in geophysics, and these systems are dynamic in nature already – that is, their definition involvestime.

INTERFERENSI GRAMATIKAL DALAM KUMPULAN CERPEN BIARKAN AKU MEMULAI KARYA NURUL F. HUDA

2019 ◽  
Vol 1 (01) ◽  
pp. 16-23
Author(s):  
Zimmatul Liviana
Keyword(s):  
Short Stories ◽  
Data Collection ◽  
Qualitative Method ◽  
Language Variation ◽  
The Other ◽  
Qualitative Descriptive ◽  
Ofthe Object ◽  
Selection Of ◽  
Descriptive Qualitative

The research grammatical interference in a collection ofshort stories Biarkan Aku Memula iwork Nurul F. Hudaisa collection ofshort storiesset in the back that Is start work Let Nurul F. Huda contains many grammatical interference.The problem of this   study were(1)how   the various morphologi calinterference containedin   a   collection of short stories Biarkan Aku Memulai work Nurul F. Huda. (2)how the various syntactic interference contained in a collection of short stories Biarkan Aku Memulai work Nurul F. Huda. The purposeof this studyis to describe the morphological and         Syntactic interference contained in a collection of short stories Biarkan Aku Memulai work Nurul F. Huda. Sociolinguistics is the study of language variation and use in society. Interference is the event of the use of language elements of one into the other language elements that occur in the speakers themselves. This research uses descriptive qualitative method because to describe the actual realityin order to obtainan accurateand objective. Qualitative descriptive methods were used to analyzethe elements ofa word orphrase that incorporated elements of other languages with the analysis and description of the formulation of the problem is the answer. Data collection techniques using observation techniques, the determination ofthe object of research, the selection of short stories.Based on the analysis of the data in this study can be found that there are six forms of interference morphology, namely (1) the prefix nasal N-sound, (2) the addition of the suffix, (3) the exchange prefix, (4) exchange suffixes, (5) exchange konfiks, (6) removal affixes. While the syntactic interference only on the words and phrases in a sentence. The results of the study it can be concluded that the interference morphology more common than syntactic interference.

The Propaganda Feedback Loop

2018 ◽  
Author(s):  
Yochai Benkler ◽  
Robert Faris ◽  
Hal Roberts
Keyword(s):  
Case Studies ◽  
Feedback Loop ◽  
The Other ◽  
Hillary Clinton ◽  
Donald Trump ◽  
The Public ◽  
False Reporting ◽  
Media Ecosystem ◽  
Crowd Out ◽  
Selection Of

This chapter presents a model of the interaction of media outlets, politicians, and the public with an emphasis on the tension between truth-seeking and narratives that confirm partisan identities. This model is used to describe the emergence and mechanics of an insular media ecosystem and how two fundamentally different media ecosystems can coexist. In one, false narratives that reinforce partisan identity not only flourish, but crowd-out true narratives even when these are presented by leading insiders. In the other, false narratives are tested, confronted, and contained by diverse outlets and actors operating in a truth-oriented norms dynamic. Two case studies are analyzed: the first focuses on false reporting on a selection of television networks; the second looks at parallel but politically divergent false rumors—an allegation that Donald Trump raped a 13-yearold and allegations tying Hillary Clinton to pedophilia—and tracks the amplification and resistance these stories faced.

scholarly journals Design Concepts for NiTiNOL Wires to Function as a Sensor

2021 ◽  
Author(s):  
D. Josephine Selvarani Ruth
Keyword(s):  
Shape Memory Alloy ◽  
Electrical Resistance ◽  
Nickel Titanium ◽  
The Other ◽  
Sensing Element ◽  
Proper Selection ◽  
Design Concepts ◽  
Mechanical Element ◽  
Selection Of ◽  
Inverse Hysteresis

AbstractNickel Titanium Naval Ordinance Laboratory (NiTiNOL) is widely called as a shape memory alloy (SMA), a class of nonlinear smart material inherited with the functionally programmed property of varying electrical resistance during the transformation enabling to be positioned as a sensing element. The major challenge to instrument the SMA wires is to suppress the wires’ nonlinearity by proper selection of two important factors. The first factor is influenced by the mechanical biasing element and the other is to identify the sensing current for the sensing device (SMA wires + biasing). This paper focuses on developing SMA wires for sensing in different orientation types and configurations by removing the non-linearity in the system’s output by introducing inverse hysteresis to the wires through the passive mechanical element.

scholarly journals An Algorithm for Choosing the Optimal Number of Muscle Synergies during Walking

Sensors ◽  
2021 ◽  
Vol 21 (10) ◽  
pp. 3311
Author(s):  
Riccardo Ballarini ◽  
Marco Ghislieri ◽  
Marco Knaflitz ◽  
Valentina Agostini
Keyword(s):  
Motor Task ◽  
Optimal Number ◽  
The Other ◽  
Simulated Dataset ◽  
Muscle Synergies ◽  
Mean Square ◽  
Real Dataset ◽  
Traditional Approaches ◽  
Selection Of ◽  
Semg Signals

In motor control studies, the 90% thresholding of variance accounted for (VAF) is the classical way of selecting the number of muscle synergies expressed during a motor task. However, the adoption of an arbitrary cut-off has evident drawbacks. The aim of this work is to describe and validate an algorithm for choosing the optimal number of muscle synergies (ChoOSyn), which can overcome the limitations of VAF-based methods. The proposed algorithm is built considering the following principles: (1) muscle synergies should be highly consistent during the various motor task epochs (i.e., remaining stable in time), (2) muscle synergies should constitute a base with low intra-level similarity (i.e., to obtain information-rich synergies, avoiding redundancy). The algorithm performances were evaluated against traditional approaches (threshold-VAF at 90% and 95%, elbow-VAF and plateau-VAF), using both a simulated dataset and a real dataset of 20 subjects. The performance evaluation was carried out by analyzing muscle synergies extracted from surface electromyographic (sEMG) signals collected during walking tasks lasting 5 min. On the simulated dataset, ChoOSyn showed comparable performances compared to VAF-based methods, while, in the real dataset, it clearly outperformed the other methods, in terms of the fraction of correct classifications, mean error (ME), and root mean square error (RMSE). The proposed approach may be beneficial to standardize the selection of the number of muscle synergies between different research laboratories, independent of arbitrary thresholds.

Romance and Latin approaches to word structure features

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Elisabeth Gibert-Sotelo ◽  
Isabel Pujol Payet
Keyword(s):  
The Other ◽  
Special Issue ◽  
Valuable Contribution ◽  
Field Of Study ◽  
Word Structure ◽  
New Approaches ◽  
Theoretical Approaches ◽  
Special Collection ◽  
Introductory Paper ◽  
Selection Of

Abstract The interest in morphology and its interaction with the other grammatical components has increased in the last twenty years, with new approaches coming into stage so as to get more accurate analyses of the processes involved in morphological construal. This special issue is a valuable contribution to this field of study. It gathers a selection of five papers from the Morphology and Syntax workshop (University of Girona, July 2017) which, on the basis of Romance and Latin phenomena, discuss word structure and its decomposition into hierarchies of features. Even though the papers share a compositional view of lexical items, they adopt different formal theoretical approaches to the lexicon-syntax interface, thus showing the benefit of bearing in mind the possibilities that each framework provides. This introductory paper serves as a guide for the readers of this special collection and offers an overview of the topics dealt in each contribution.

Patterns of Searching for Information on the World Wide Web: A Pilot Study

2003 ◽  
Vol 92 (3_suppl) ◽  
pp. 1091-1096 ◽  
Author(s):  
Nobuhiko Fujihara ◽  
Asako Miura
Keyword(s):  
World Wide Web ◽  
Undergraduate Students ◽  
Search Engines ◽  
World Wide ◽  
Information Sources ◽  
Task Type ◽  
The Other ◽  
The World ◽  
Selection Of ◽  
Search Domain

The influences of task type on search of the World Wide Web using search engines without limitation of search domain were investigated. 9 graduate and undergraduate students studying psychology (1 woman and 8 men, M age = 25.0 yr., SD = 2.1) participated. Their performance to manipulate the search engines on a closed task with only one answer were compared with their performance on an open task with several possible answers. Analysis showed that the number of actions was larger for the closed task ( M = 91) than for the open task ( M = 46.1). Behaviors such as selection of keywords (averages were 7.9% of all actions for the closed task and 16.7% for the open task) and pressing of the browser's back button (averages were 40.3% of all actions for the closed task and 29.6% for the open task) were also different. On the other hand, behaviors such as selection of hyperlinks, pressing of the home button, and number of browsed pages were similar for both tasks. Search behaviors were influenced by task type when the students searched for information without limitation placed on the information sources.

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