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    Wyświetlanie 1-6 z 6
    Tytuł:
    Nowe celowane leki małocząsteczkowe w leczeniu astmy
    New targeted small molecule drugs in asthma treatment
    Autorzy:
    Romantowski, Jan
    Niedoszytko, Marek Niedoszytko
    Powiązania:
    https://bibliotekanauki.pl/articles/2176137.pdf
    Data publikacji:
    2019-09
    Wydawca:
    Oficyna Wydawnicza Mediton
    Tematy:
    mała cząsteczka
    astma
    fenotyp
    lek
    eozynofil
    small molecule
    asthma
    phenotype
    drug
    eosinophil
    Opis:
    Astma jest częstą chorobą przewlekła oskrzeli, stanowiącą istotny problem społeczny na świecie. Pomimo znacznego postępu w terapii wziewnej w ostatnich dekadach, astma ciężka stanowi nadal wyzwanie dla współczesnej medycyny. Heterogenność mechanizmów stojących za nasileniem objawów i oporność na klasyczne leki wziewne znacznie utrudnia poszukiwanie celowanych leków w grupie chorych nie uzyskujących zadowalającej kontroli choroby w oparciu o podstawowe leki. Dotychczasowe badania nad nowymi lekami w ciężkiej astmie koncentrują się głównie na syntezie przeciwciał. Jednak relatywnie duża cząsteczka tych leków nakłada na nie pewne ograniczenia związane z drogą podania i możliwymi punktami uchwytu. Niniejszy artykuł omawia nowe możliwości terapeutyczne związane z opracowywanymi w ostatnich latach lekami małocząsteczkowymi o masie poniżej 900 Daltonów.
    Asthma is a common chronic bronchial disease that is a major social problem in the world. Despite significant advances in inhalation therapy in recent decades, severe asthma remains a challenge for modern medicine. The heterogeneity of the mechanisms behind the severity of symptoms and resistance to classic inhalation drugs significantly impedes the search for targeted drugs in a group of patients with no satisfactory disease control based on basic drugs. To date, research on new drugs in severe asthma has mainly focused on antibody synthesis. However, a relatively large molecule of these drugs imposes some restrictions on the way of their administration and diagostic targets. The article discusses new therapeutic options associated with low molecular weight drugs under 900 Dalton being developed in recent years
    Źródło:
    Alergia Astma Immunologia - przegląd kliniczny; 2019, 24, 3; 131-136
    1427-3101
    Pojawia się w:
    Alergia Astma Immunologia - przegląd kliniczny
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Prospects for p53-based cancer therapy.
    Autorzy:
    Stokłsa, Tomasz
    Gołąb, Jakub
    Powiązania:
    https://bibliotekanauki.pl/articles/1041406.pdf
    Data publikacji:
    2005
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    missense mutations
    cancer
    p53
    stress response
    small molecule inhibitors
    tumor suppressor
    Opis:
    The p53 tumor suppressor plays the role of a cellular hub which gathers stress signals such as damage to DNA or hypoxia and translates them into a complex response. p53 exerts its action mainly as a potent transcription factor. The two major outcomes of p53 activity are highlighted: cell cycle arrest and apoptosis. During malignant transformation p53 or p53-pathway related molecules are disabled extremely often. Mutations in p53 gene are present in every second human tumor. A mutant form of p53 may not only negate the wild type p53 function but may play additional role in tumor progression. Therefore p53 represents a relatively unique and specific target for anticancer drug design. Current approaches include several different molecules able to restore p53 wild-type conformation and activity. Such small molecule drugs hold great promise in treating human tumors with dysfunction of p53 pathway in the near future.
    Źródło:
    Acta Biochimica Polonica; 2005, 52, 2; 321-328
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Interaction of diatomic molecules with nickel ions inside the channels of high silica zeolites : an EPR and DFT study
    Autorzy:
    Mazur, T.
    Podolska, K.
    Pietrzyk, P.
    Sojka, Z.
    Powiązania:
    https://bibliotekanauki.pl/articles/147105.pdf
    Data publikacji:
    2013
    Wydawca:
    Instytut Chemii i Techniki Jądrowej
    Tematy:
    electron paramagnetic resonance (EPR) spectroscopy
    g-tensor
    nickel
    zeolite
    small molecule activation
    Opis:
    Interaction of CO, NO, and O2 diatomics with NiII and NiI ions dispersed in ZSM-5 zeolite was investigated by electron paramagnetic resonance (EPR) spectroscopy and density functional theory (DFT) modelling. The resulting adducts NiI-CO, NiII-NO, and NiI-O2 were identified based on g-tensor parameters, obtained by computer fitting of the powder EPR spectra, and next ascertained by parallel relativistic DFT calculations of the corresponding g-tensor values. The structures of the NiI-CO, NiII-NO, and NiI-O2 complexes were obtained by geometry optimization with the Kohn- -Sham method. Binding of the diatomics was discussed in terms of the spin-pairing and electron density transfer events. Interaction of CO with NiI cations led to the pronounced change in the coordination and electronic structure of the NiI center, however, no redox processes were observed in agreement with the “innocent” nature of CO as a ligand. On the contrary, strong electron and spin density redistribution was observed upon NO and O2 interaction (“non-innocent ligands”) leading to the formation of the bound nitrosonium NOδ+ and superoxo O2 – species, respectively.
    Źródło:
    Nukleonika; 2013, 58, 3; 351-357
    0029-5922
    1508-5791
    Pojawia się w:
    Nukleonika
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Exploring Baltic Sea cyanobacteria for small-molecule inhibitors of microRNA function: a project description
    Autorzy:
    Brzuzan, P.
    Mazur-Marzec, H.
    Stefaniak, F.
    Woźny, M.
    Florczyk, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/363294.pdf
    Data publikacji:
    2018
    Wydawca:
    Uniwersytet Warmińsko-Mazurski w Olsztynie
    Tematy:
    cyanobacteria
    luciferase reporter cell line
    microRNA
    small-molecule inhibitor
    cyjanobakteria
    inhibitor
    Morze Bałtyckie
    Opis:
    Cyanobacteria constitute a rich source of biologically active and structurally diverse compounds. The pharmacological potential of these compounds resides among others in their ability to control the proliferation and growth of cancer cell lines and potent disease-causing microbial agents. Despite recent scientific advances, the way these compounds interact with the body’s molecular structure are still unclear and science still has to discover how the cyanobacterial metabolites interact with cell structures and how cells react to them. In this project, we will study yet unexamined cyanobacterial metabolites, especially the compounds which act as chemical ligands for microRNA (miRNA) -binding sites, making them promising regulators (inhibitors) of gene networks that are involved in various diseases. We will first develop a stable cell line that constitutively expresses a unique miRNA reporter system. Then, we will conduct a screen on chemical compounds discovered in Baltic cyanobacteria to identify small molecules with inhibitory activity and specificity to MIR92b-3p, which has a significant impact on liver cell behavior in humans. We assume that a successful MIR92b-3p inhibitor will bind to the precursors of MIR92b-3p miRNA, disabling the action of either of the two processing enzymes involved in the biogenesis of any miRNA in a cell (Drosha or Dicer), thus affecting the MIR92b function. The discoveries made with these inhibitory chemical molecules could provide insight into the role of the MIR92 pathway in liver diseases and cancer, and possibly, if promising results appear, they may facilitate a strategy for treating some human diseases in the future.
    Źródło:
    Environmental Biotechnology; 2018, 14, 1; 1-4
    1734-4964
    Pojawia się w:
    Environmental Biotechnology
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Design of small molecule inhibitors of type III secretion system ATPase EscN from enteropathogenic Escherichia coli
    Autorzy:
    Bzdzion, Lukasz
    Krezel, Hanna
    Wrzeszcz, Karol
    Grzegorek, Irmina
    Nowinska, Katarzyna
    Chodaczek, Grzegorz
    Swietnicki, Wieslaw
    Powiązania:
    https://bibliotekanauki.pl/articles/1038684.pdf
    Data publikacji:
    2017
    Wydawca:
    Polskie Towarzystwo Biochemiczne
    Tematy:
    Escherichia coli (E. coli)
    type III secretion system (T3SS)
    enzyme inhibitor
    small molecule
    Opis:
    Enteropathogenic E. coli (EPEC) is a human pathogen using type III secretion system for delivery of proteins directly into the human host. The system contains a single ATPase, EscN, which is essential for uncoupling of proteins from their complexes with chaperones before the delivery. The structure of EscN ATPase (PDB code: 2obm) was used to screen computationally for small molecule inhibitors blocking its active site. Two lead candidates were examined but only one, Compound 54, was selected for further optimization. After extended QSAR optimization, two derivatives were found to be competitive inhibitors of EscN capable of blocking ATPase activity with a Ki below 50 µM. One candidate, WEN05-03, with a Ki=16±2 µM, was also minimally toxic to mammalian cells as determined by other assays. In the cell infection model of HeLa cells with EPEC, Compound WEN05-03 completely blocked actin cluster formation at 100 µM concentration, when analyzed by confocal microscopy. The second best inhibitor of EscN ATPase activity was WEN04-34 with a Ki=46±2 µM. However, the compound was highly toxic to the BALB/3T3 cell line. In summary, the work identifies a compound blocking bacterial ATPase in its active site without causing cellular toxicity to the host cells. It is the first report showing feasibility of using bacterial virulence system ATPase as a target for safe, non-toxic compounds and offering a proof-of-concept for non-antibiotic alternatives.
    Źródło:
    Acta Biochimica Polonica; 2017, 64, 1; 49-63
    0001-527X
    Pojawia się w:
    Acta Biochimica Polonica
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
    Tytuł:
    Animal Dicer and plant Dicer-like proteins
    Autorzy:
    Tworak, A.
    Urbanowicz, A.
    Podkowinski, J.
    Figlerowicz, M.
    Powiązania:
    https://bibliotekanauki.pl/articles/80710.pdf
    Data publikacji:
    2013
    Wydawca:
    Polska Akademia Nauk. Czytelnia Czasopism PAN
    Tematy:
    eukaryotic organism
    RNA molecule
    double stranded RNA
    Dicer-like protein
    biogenesis
    Drosophila melanogaster
    microRNA
    small interfering RNA
    Źródło:
    BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology; 2013, 94, 1
    0860-7796
    Pojawia się w:
    BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
    Dostawca treści:
    Biblioteka Nauki
    Artykuł
      Wyświetlanie 1-6 z 6

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