Informacja

Drogi użytkowniku, aplikacja do prawidłowego działania wymaga obsługi JavaScript. Proszę włącz obsługę JavaScript w Twojej przeglądarce.

Wyszukujesz frazę "small molecule" wg kryterium: Wszystkie pola


Wyświetlanie 1-8 z 8
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:
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:
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:
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:
Właściwości antyoksydacyjne części białkowej i niebiałkowej krwi w różnych stanach chorobowych
Antioxidative properties of the protein and small molecule parts of blood serum in various diseases
Autorzy:
Głód, B. K.
Piszcz, P.
Powiązania:
https://bibliotekanauki.pl/articles/92300.pdf
Data publikacji:
2015
Wydawca:
Uniwersytet Przyrodniczo-Humanistyczny w Siedlcach
Tematy:
antyoksydanty
całkowity potencjał antyoksydacyjny
krew
odbiałczanie
antioxidants
total antioxidant potential
blood
deproteinization
Opis:
Wolne rodniki i antyoksydanty odgrywają istotną rolę w prawie każdej jednostce chorobowej. Dlatego tak istotne jest ich oznaczanie. W literaturze opisanych jest wiele metod oznaczania zarówno wolnych rodników jak i antyoksydantów. Często jednak sumaryczne wielkości, stres oksydacyjny i całkowity potencjał antyoksydacyjny (CPA), dostarczają więcej informacji o badanym układzie niż stężenia poszczególnych antyoksydantów i/lub rodników. Obie te wielkości są ze sobą odwrotnie skorelowane. W pracy dokonano przeglądu zmian CPA krwi osób w różnych stanach chorobowych. Opisano też jakie udziały CPA przypadają na białka, antyoksydanty niskocząsteczkowe na wartości CPA, a także udziału różnych związków w całkowitym CPA.
In this paper the possibility of measuring of the total antioxidant potential (TAP) to examination of the antioxidative properties of blood serum and plasma is discussed. Particular attention was paid to the possibility of an independent TAP examination of the protein and small molecules’ parts of the blood serum. The participation of various compounds in the total TAP of serum is also described.
Źródło:
Camera Separatoria; 2015, 7, 2; 129-136
2083-6392
2299-6265
Pojawia się w:
Camera Separatoria
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Znaczenie i przykłady zastosowania banków pseudoatomów asferycznych w krystalografii małych cząsteczek i ich potencjalne wykorzystanie w krystalografii makromolekuł
The importance and examples of application of aspherical pseudoatom databanks in small-molecule crystallography and their potential use in makromolecular crystallography
Autorzy:
Dominiak, P. M.
Powiązania:
https://bibliotekanauki.pl/articles/171730.pdf
Data publikacji:
2014
Wydawca:
Polskie Towarzystwo Chemiczne
Tematy:
asferyczne atomowe czynniki rozpraszania
gęstość elektronowa
rentgenowskie dane dyfrakcyjne
struktura krystaliczna
aspherical atomic scattering factors
electron density
X-ray diffraction data
crystal structure
Opis:
X-rays are diffracted by the electron density of crystals. Thus, the correct analysis of a single crystal X-ray diffraction pattern can provide information about the distribution of the electron density. How precise and accurate the information could be is largely determined by the resolution of the data collected. The majority of X-ray diffraction data is collected at and below the standard resolution, dmin= 0.84 Å. Before the development of pseudoatom databases, such resolution permitted to carry out X-ray refinement only with the use of simple model of electron density called the Independent Atom Model (IAM). In the IAM, individual atoms are represented by the spherically averaged electron density distributions obtained by theoretical methods for isolated atoms in the ground state. The IAM does not take into account changes in the density distribution of individual atoms caused by such phenomena as chemical bond formation, charge transfer, lone electron pairs, etc. Only the geometrical information of the crystal structure is obtained from the IAM refinement. A more physical model has been introduced in which an atom is represented as a finite spherical harmonic expansion of the electron density around each atomic center and is called a pseudoatom. Such definition allows the pseudoatom electron density to be individually adjusted (by changing values of pseudoatom parameters) to account for density departure from spherical and neutral model. However, to refine pseudoatom parameters with experimental data subatomic resolution is required. It has been shown that the values of pseudoatom parameters are almost identical for atoms in similar chemical environments, i.e. atoms having similar local topology of connecting chemical bonds. Therefore it was possible to build a databank of different types of pseudoatoms and to use the bank to generate the Transferable Aspherical Atom Model (TAAM) for any organic molecule, including proteins and nucleic acids. There are three different pseudoatom databanks being developed: ELMAM2, GID and UBDB. They differ by the source of pseudoatom parameters and by the way how atom types are defined. Replacement of the IAM model by the TAAM in the refinement procedure of standard diffraction data leads to more accurate geometrical information and provide access to quantitative estimation of the electron density distribution and properties derived from it (dipole moment, electrostatic potential, etc.) for molecules in a crystalline environment. The review summarizes the research on the verification and application of pseudoatom databases.
Źródło:
Wiadomości Chemiczne; 2014, 68, 5-6; 429-455
0043-5104
2300-0295
Pojawia się w:
Wiadomości Chemiczne
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 1-8 z 8

    Ta witryna wykorzystuje pliki cookies do przechowywania informacji na Twoim komputerze. Pliki cookies stosujemy w celu świadczenia usług na najwyższym poziomie, w tym w sposób dostosowany do indywidualnych potrzeb. Korzystanie z witryny bez zmiany ustawień dotyczących cookies oznacza, że będą one zamieszczane w Twoim komputerze. W każdym momencie możesz dokonać zmiany ustawień dotyczących cookies