Search results for " screen"
showing 10 items of 970 documents
Higher plants possess two different types of ATX1-like copper chaperones.
2007
Abstract Copper (Cu) chaperones constitute a family of small Cu+-binding proteins required for Cu homeostasis in eukaryotes. The ATX1 family of Cu chaperones specifically delivers Cu to heavy metal P-type ATPases. The plant Arabidopsis thaliana expresses the ATX1-like Cu chaperone CCH, which exhibits a plant-specific carboxy-terminal domain (CTD) with unique structural properties. We show that CCH homologues from other higher plants contain CTDs with structural properties similar to Arabidopsis CCH. Furthermore, we identify a new ATX1-like Cu chaperone in Arabidopsis, AtATX1, which functionally complements yeast atx1Δ and sod1Δ associated phenotypes, and localizes to the cytosol of Arabidop…
A Practical Perspective : The Effect of Ligand Conformers on the Negative Image-Based Screening
2019
Negative image-based (NIB) screening is a rigid molecular docking methodology that can also be employed in docking rescoring. During the NIB screening, a negative image is generated based on the target protein’s ligand-binding cavity by inverting its shape and electrostatics. The resulting NIB model is a drug-like entity or pseudo-ligand that is compared directly against ligand 3D conformers, as is done with a template compound in the ligand-based screening. This cavity-based rigid docking has been demonstrated to work with genuine drug targets in both benchmark testing and drug candidate/lead discovery. Firstly, the study explores in-depth the applicability of different ligand 3D conformer…
Nueva era en el combate contra el cáncer: Evolución y cáncer: progreso y tratamiento de tumores
2013
L’oncohematologia ha assistit en les últimes dècades a importants avenços en el tractament i supervivència. La toxicitat derivada de la quimioteràpia clàssica i la necessitat de millorar l’eficàcia i tolerància als tractaments han fet que es desencadene un allau d’activitat investigadora que constantment proporciona fruits. Gran part d’aquest esforç s’ha enfocat al desenvolupament de «teràpies diana» dirigides contra determinades alteracions funcionals, clau per a la supervivència de la cèl·lula tumoral. Així es pretén aconseguir major eficàcia en el tractament i que el pacient pague un menor cost en toxicitat. Avenços en altres disciplines de l’oncologia com l’epidemiologia, la cirurgia i …
Effect of extraction solvent on total phenolic content, total flavonoid content and antioxidant activity of Cetraria islandica
2020
Oxidative stress may lead to a number of diseases such as atherosclerosis, nephrotoxicity, liver cirrhosis, cancers, diabetes, and Alzheimer disease. Medicinal plants are an important source of antioxidants. Therefore, the antioxidant potential of Cetraria islandica was evaluated in this work. The coarse powder of leaf of Cetraria islandica was extracted in Soxhlet apparatus, with ethanol (90%) and ethanolic extract of Cetraria islandica (EECI) was further processed for phytochemical screening, total phenol content, total flavonoid content, and various in vitro antioxidant assays. The phytochemicals present in EECI were glycosides, carbohydrates, triterpenoids, proteins and amino acids, gum…
New 2-Methoxy Acetylenic Acids and Pyrazole Alkaloids from the Marine Sponge Cinachyrella sp.
2017
Three new 2-methoxy acetylenic acids (1–3) and a known derivative (4), in addition to three new natural pyrazole alkaloids (5–7) were isolated from an Indonesian marine sponge of the genus Cinachyrella. Compounds 5 and 6 have previously been reported as synthetic compounds. The structures of the new compounds were established on the basis of one- and two-dimensional NMR spectroscopy as well as by mass spectrometric data. The absolute configuration of the new acetylenic acid derivatives (1–3) was established by ECD spectroscopy. All isolated compounds were evaluated for their cytotoxicity against L5178Y mouse lymphoma cells. Compounds 1–4 exhibited strong activity with an IC50 value of 0.3 µ…
Impact of
2018
Drosophila melanogaster has been for over a century the model of choice of several neurobiologists to decipher the formation and development of the nervous system as well as to mirror the pathophysiological conditions of many human neurodegenerative diseases. The rare disease Friedreich’s ataxia (FRDA) is not an exception. Since the isolation of the responsible gene more than two decades ago, the analysis of the fly orthologue has proven to be an excellent avenue to understand the development and progression of the disease, to unravel pivotal mechanisms underpinning the pathology and to identify genes and molecules that might well be either disease biomarkers or promising targets for therap…
Modular Point-of-Care Breath Analyzer and Shape Taxonomy-Based Machine Learning for Gastric Cancer Detection
2022
Background: Gastric cancer is one of the deadliest malignant diseases, and the non-invasive screening and diagnostics options for it are limited. In this article, we present a multi-modular device for breath analysis coupled with a machine learning approach for the detection of cancer-specific breath from the shapes of sensor response curves (taxonomies of clusters). Methods: We analyzed the breaths of 54 gastric cancer patients and 85 control group participants. The analysis was carried out using a breath analyzer with gold nanoparticle and metal oxide sensors. The response of the sensors was analyzed on the basis of the curve shapes and other features commonly used for comparison. These f…
Standards for the diagnosis and management of complex regional pain syndrome: Results of a European Pain Federation task force.
2019
Background: Complex regional pain syndrome is a painful and disabling post-traumatic primary pain disorder. Acute and chronic complex regional pain syndrome (CRPS) are major clinical challenges. In Europe, progress is hampered by significant heterogeneity in clinical practice. We sought to establish standards for the diagnosis and management of CRPS. Methods: The European Pain Federation established a pan-European task force of experts in CRPS who followed a four-stage consensus challenge process to produce mandatory quality standards worded as grammatically imperative (must-do) statements. Results: We developed 17 standards in 8 areas of care. There are 2 standards in diagnosis, 1 in multi…
Structural and functional diversity of Bacillus thuringiensis toxins on animal, plant and microbial cells
2018
Debido a los efectos nocivos de los insecticidas químicos en los ecosistemas y sobre los organismos beneficiosos, la implementación de agentes de control biológico ha recibido considerable atención. Entre los agentes de control biológico, se ha dedicado gran interés a los entomopatógenos, debido a su potencial para controlar plagas agrícolas y domésticas, vectores de enfermedades humanas y animales, sin introducir material no degradable en el medio ambiente. Bacillus thuringiensis (Bt) es el agente de control microbiano comercial más utilizado en la actualidad, con efectividad contra diferentes especies de insectos plaga. Las cepas de Bt producen cristales paraesporales proteináceos durante…
N-Cinnamoyltetraketide Derivatives from the Leaves of Toussaintia orientalis
2015
Seven N-cinnamoyltetraketides (1−7), including the new Ztoussaintine E (2), toussaintine F (6), and toussaintine G (7), were isolated from the methanol extract of the leaves of Toussaintia orientalis using column chromatography and HPLC. The configurations of E-toussaintine E (1) and toussaintines A (3) and D (5) are revised based on single-crystal X-ray diffraction data from racemic crystals. Both the crude methanol extract and the isolated constituents exhibit antimycobacterial activities (MIC 83.3−107.7 μM) against the H37Rv strain of Mycobacterium tuberculosis. Compounds 1, 3, 4, and 5 are cytotoxic (ED50 15.3−105.7 μM) against the MDA-MB-231 triple negative aggressive breast cancer cel…