Filtry
wszystkich: 25
Wyniki wyszukiwania dla: MICROTUBULE
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Inhibitory mikrotubul w terapii przeciwnowotworowej = Inhibitors of microtubule in cancer therapy
PublikacjaW artykule opisano inhibitory mikrotubul, różnorodne związki chemiczne, znajdujące się w zaawansowanych przedklinicznych i wstępnych badaniach klinicznych. Pośród nich na uwagę zasługują półsyntetyczne analogi taksolu, substancje pochodzenia naturalnego, takie jak: epotilony, kombretastatyny, kolchinoidy, dolastatyny oraz syntetyczne związki o niskim ciężarze czasteczkowym: heterokombretastatyny, sulfonamidy, fenostatyny, pochodne...
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Utilizing Genome-Wide mRNA Profiling to Identify the Cytotoxic Chemotherapeutic Mechanism of Triazoloacridone C-1305 as Direct Microtubule Stabilization
PublikacjaRational drug design and in vitro pharmacology profiling constitute the gold standard in drug development pipelines. Problems arise, however, because this process is often dicult due to limited information regarding the complete identification of a molecule’s biological activities. The increasing aordability of genome-wide next-generation technologies now provides an excellent opportunity to understand a compound’s diverse eects...
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Sustainable carbon microtube derived from cotton waste for environmental applications
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Down-regulation of DNA topoisomerase IIalpha leads to prolonged cell cycle transit in G2 and early M phases and increased survival to microtubule-interacting agents
PublikacjaInhibitory polimeryzacji mikrotubul wykazują preferencyjną toksyczność wobec komórek mitotycznych. W ramach tego projektu badaliśmy czy oporność komórek ludzkich białaczek na inhibitor mikrotubul, winkrystynę, prowadzi do zmian w regulacji progresji cyklu komórkowego. Nasze wyniki wskazują, że oporności na winkrystynę towarzyszą zmiany w długości fazy G2 i M w nieobecności i obecności inhibitora wrzeciona mitotycznego, nokodazolu....
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High-performance NdSrCo2O5+δ–Ce0.8Gd0.2O2-δ composite cathodes for electrolyte-supported microtubular solid oxide fuel cells
PublikacjaNdSrCo2O5+δ (NSCO) is a perovskite with an electrical conductivity of 1551.3 S cm−1 at 500 °C and 921.7 S cm−1 at 800 °C and has a metal-like temperature dependence. This perovskite is used as the cathode material for Ce0.8Gd0.2O2-δ (GDC)-supported microtubular solid oxide fuel cells (MT-SOFCs). The MT-SOFCs fabricated in this study consist of a bilayer anode, comprising a NiO–GDC composite layer and a NiO layer, and a NSCO–GDC...
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Cross-talk between DNA damage and cell survival checkpoints during G2 and mitosis: pharmacological implications
PublikacjaW pracy wyjaśnialiśmy rolę surwiwiny w ochronie komórek w czasie przejścia między G2 i mitozą, traktowanych związkiem uszkadzającym DNA. Jako model komórkowy wybraliśmy komórki ludzkiej białaczki MOLT-4, które wykazują zwiększoną ekspresję białka surwiwiny i niefunkcjonalnym p53. Ekspozycja tych komórek na melfalan, klasyczny związek uszkadzający DNA, prowadzi do uruchomienia punktu kontrolnego w G2 i zablokowania progresji cyklu...
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Combretastatin A-4 (CA-4) and its analogues. Synthesis and biological activity
PublikacjaSpośród wielu związków przeciwnowotworowych otrzymanych w ostatnich dwóch dekadach, na szczególną uwagę zasługują te, które powodują reorganizację mikrotubul. Jedną z takich substancji jest opisana w artykule kombretastatyna A-4 (CA-4), związek który indukuje apoptozęproliferujących komórek śródbłonka naczyń guza nowotworowego. Hamuje on polimeryzację tubuliny, prowadząc do rozpadu mikrotubul. CA-4 wyizolowana została z kory wierzby...
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Triazoloacridone C-1305 impairs XBP1 splicing by acting as a potential IRE1α endoribonuclease inhibitor
PublikacjaInositol requiring enzyme 1 alpha (IRE1α) is one of three signaling sensors in the unfolding protein response (UPR) that alleviates endoplasmic reticulum (ER) stress in cells and functions to promote cell survival. During conditions of irrevocable stress, proapoptotic gene expression is induced to promote cell death. One of the three signaling stressors, IRE1α is an serine/threonine-protein kinase/endoribonuclease (RNase) that...
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A simple approach to heat exchanger sizing optimisation by means of entrophy generation minimisation
PublikacjaIn the paper an attempt is presented to find the method of optimization of microtube diameter with respect to optimal thermal-hydraulic conditions in the single-phase shell-and-tube heat exchangers. The approach is based on consideration of pumping power at the condition of maximum heat transfer by the heat exchanger tube system. In the optimization method the tube diameter is first specified and then appropriate calculations are...
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The significance of the properties of water for the working cycle of the kinesin molecular motor
PublikacjaExplicit solvent molecular dynamics simulations were performed in this study to investigate and discuss several aspects of the influence of the properties of water on the working cycle of a molecular motor from the kinesin superfamily. The main objects of attention were: the binding of the neck linker and the association of the kinesin and the tubulin. The docking of the neck linker is considered a crucial event during the working...
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Novel chalcone-derived pyrazoles as potential therapeutic agents for the treatment of non-small cell lung cancer
PublikacjaLung cancer is considered to account for approximately one-fifth of all malignant tumor-related deaths worldwide and is therefore one of the most lethal malignancies. Pyrazole scaffold possesses a wide range of biological and pharmacological activities, which play important roles in medicinal chemistry. The present study reports the synthesis and in vitro biological characterization of nine pyrazoles derived from chalcones as potential...
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Synthesis of Combretastatin A-4 Analogs and their Biological Activities
PublikacjaCombretastatin A-4 (CA-4) is a natural product, which consists of two phenyl rings, linked by an ethylene bridge. CA-4, inhibitor of polymerization of tubulin to microtubules, possesses a strong antitumor and anti-vascular properties both in vitro and in vivo. Previous studies showed that disodium phosphate salt of CA-4, a water-soluble prodrug is well tolerated at therapeutically useful doses. However, it should be noted that...
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Properties of water in the region between a tubulin dimer and a single motor head of kinesin
PublikacjaA kinesin is a molecular motor that can perform movement on a microtubule track in a stepping-like manner. This motion is connected with processes of association and dissociation of kinesin and tubulin. Water is an important participant in these kinds of molecular interactions. This is why we have decided to investigate the dynamical and structural properties of water in the region between the kinesin catalytic domain and the tubulin...
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Combined anticancer therapy with imidazoacridinone analogue C‐1305 and paclitaxel in human lung and colon cancer xenografts—Modulation of tumour angiogenesis
PublikacjaThe acridanone derivative 5-dimethylaminopropylamino- 8- hydroxytriazoloacridinone (C-1305) has been described as a potent inhibitor of cancer cell growth. Its mechanism of action in in vitro conditions was attributed, among others, to its ability to bind and stabilize the microtubule network and subsequently exhibit its tumour- suppressive effects in synergy with paclitaxel (PTX). Therefore, the objective of the present study...
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010649801]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010649461]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010648211]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010644461]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010642231]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010642141]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010648401]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010644561]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010647871]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Adenocarcinoma, metastatic, NOS - Female, 76 - Tissue image [4080730010646921]
Dane BadawczeThis is the histopathological image of BRONCHUS AND LUNG tissue sample obtained in Medical University Gdańsk and deposited in ZMDL-GUMED. The sample image was taken using: VS200 Olympus slide scanner (20x magnification) and saved to DICOM format.
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Hydratacja domeny katalitycznej kinezyny
PublikacjaKinezyna należy do białek zwanych motorami molekularnymi, które są zdolne do wykonywania pracy mechanicznej. Konwencjonalna kinezyna wyposażona jest w dwie domeny motoryczne. Potrafi ona poruszać się w uporządkowany sposób przemieszczając się po szlakach wyznaczanych przez tzw. mikrotubule, które tworzone są przez białko tubulinę. Jej rola polega m.in. na transporcie białek i organelli komórkowych. Naturalnym środowiskiem działania...