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Wyszukujesz frazę "anti-proliferative" wg kryterium: Temat


Wyświetlanie 1-2 z 2
Tytuł:
Plasma membrane homing of tissue nonspecific alkaline phosphatase under the influence of 3-hydrogenkwadaphnin, an antiproliferative agent from Dendrostellera lessertii
Autorzy:
Sadeghirizi, Akram
Yazdanparast, Razieh
Powiązania:
https://bibliotekanauki.pl/articles/1041081.pdf
Data publikacji:
2007
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
alkaline phosphatase
anti-proliferative
Dendrostellera lessertii
Opis:
Several mammalian enzymes are anchored to the outer surface of the plasma membrane by a covalently attached glycosylphosphatidylinositol (GPI) structure. These include acetylcholinesterase, alkaline phosphatase (AP) and 5'-nucleotidase among other enzymes. Recently, it has been reported that these membrane enzymes can be released into the serum by the GPI-dependent phospholipase D under various medical disturbances such as cancer and/or by chemical and physical manipulation of the biological systems. Treatment of MCF-7 cells with two consecutive effective concentrations of 3-hydrogenkwadaphnin (3-HK, 3 nM) for 48 h enhanced membrane AP activity by almost 330% along with a 40% reduction in the AP activity of the cell culture medium. In addition, our data indicate that 3-HK is capable of inducing mainly the tissue-nonspecific alkaline phosphatase (TNAP) isoenzyme, along with enhancing its thermostability. These findings, besides establishing a correlation between the antiproliferative activity of 3-HK and the extent of plasma membrane AP activity, might assist in the development of new diagnostic tools for following cancer medical treatments.
Źródło:
Acta Biochimica Polonica; 2007, 54, 2; 323-329
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
DESIGN, SYNTHESIS AND BIOLOGICAL ESTIMATION OF INNOVATIVE PYRAZOLES AS ANTICANCER AGENTS TARGETING CDK2
Autorzy:
Ibrahim, Diaa A.
Radini, Ibrahim A.
KHIDRE, Rizk E.
Powiązania:
https://bibliotekanauki.pl/articles/895649.pdf
Data publikacji:
2019-06-28
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
Pharmacophore
binding energy
pyrazoles
anti-proliferative activity
CDK2 inhibitors
Docking study
Opis:
CDK2, which exhibits an indispensable role as an organizer of cell growth, is the powerfully studied protein Kinases objective of anticancer suppressors. The present study was dedicated to design (pharmacophore, docking, and binding energy) and to prepare an inspired derivatives of pyrazole and pyrazolo[1,5-d]pyrimidine as promising anticancer agents, which can act by targeting CDK2. The promising compounds were selected according to their fit-value and binding energy scores. The anticancer activity against MCF-7 was tested for the prepared compounds and compounds 2, 3b, and 7b showed expressive activity with IC50 1.75, 0.89 and 1.32 µM respectively. The CDK2 evaluation was carried out to estimate the efficiency of the prepared compounds as promising inhibitors. The results revealed that compound 3b with effective inhibitory activity against tumor growth and with its potent inhibition against the CDK2 enzyme with percent inhibition 86 would be a prospective anticancer agent. The prepared compounds with high biological activity could be used as lead inhibitors for the CDK2 kinase domain.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2019, 76, 3; 453-468
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-2 z 2

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