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Tytuł:
The role of chitosan in akt kinase regulation activity
Autorzy:
Ignacak, Jan
Wiśniewska-Wrona, Maria
Dulińska-Litewka, Joanna
Pałka, Iwona
Kucharska, Magdalena
Kazimierski, Jan
Powiązania:
https://bibliotekanauki.pl/articles/1034695.pdf
Data publikacji:
2016
Wydawca:
Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Tematy:
Akt kinase (PKB)
M2 pyruvate kinase
cells migration
metalloproteinases
Opis:
A decrease in migration of tumor cells incubated with the investigated chitosan preparations was correlated with a decreased activity of MMP-2 and MMP-9 metalloproteinases, what significantly affected inhibition of tumor cell proliferation. In the investigations of the effects of various chitosan preparations on expression of PCNA, Akt and β-catenin in the normal human 184A1 cells and in breast carcinoma MCF7 cells evaluated at the protein level, significant differences in inhibition of expression of selected genes were noted in the tumor cells. Similarly as in the case of human cells, in mouse cells, the differences in expression of the investigated genes involved solely the Ehrlich carcinoma cells. In the presence of the investigated chitosan preparations, there was observed inhibition of expression of the N-cadherin, β-catenin, Akt and PCNA genes. In case of p21 protein, its level increased, similarly as in the human breast carcinoma cells, what may also be related to phosphorylation of the protein, its capture by the cytosol and prolonging its half-life as compared to the non-phosphorylated form. In case of the normal human 181A1 cells and mouse CRL 1636 cells, no significant alterations were noted in expression of the investigated genes in presence of the employed chitosan preparations.
Źródło:
Progress on Chemistry and Application of Chitin and its Derivatives; 2016, 21; 73-82
1896-5644
Pojawia się w:
Progress on Chemistry and Application of Chitin and its Derivatives
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Tyrosine kinase, Aurora kinase and leucine aminopeptidase as attractive drug targets in anticancer therapy - characterisation of their inhibitors
Autorzy:
Ziemska, J.
Solecka, J.
Powiązania:
https://bibliotekanauki.pl/articles/876592.pdf
Data publikacji:
2016
Wydawca:
Narodowy Instytut Zdrowia Publicznego. Państwowy Zakład Higieny
Tematy:
tyrosine kinase
Aurora kinase
leucine aminopeptidase
drug
anticancer therapy
enzyme inhibitor
Opis:
Cancers are the leading cause of deaths all over the world. Available anticancer agents used in clinics exhibit low therapeutic index and usually high toxicity. Wide spreading drug resistance of cancer cells induce a demanding need to search for new drug targets. Currently, many on-going studies on novel compounds with potent anticancer activity, high selectivity as well as new modes of action are conducted. In this work, we describe in details three enzyme groups, which are at present of extensive interest to medical researchers and pharmaceutical companies. These include receptor tyrosine kinases (e.g. EGFR enzymes) and non-receptor tyrosine kinases (Src enzymes), type A, B and C Aurora kinases and aminopeptidases, especially leucine aminopeptidase. We discuss classification of these enzymes, biochemistry as well as their role in the cell cycle under normal conditions and during cancerogenesis. Further on, the work describes enzyme inhibitors that are under in vitro, preclinical, clinical studies as well as drugs available on the market. Both, chemical structures of discovered inhibitors and the role of chemical moieties in novel drug design are discussed. Described enzymes play essential role in cell cycle, especially in mitosis (Aurora kinases), cell differentiation, growth and apoptosis (tyrosine kinases) as well as G1/S transition (leucine aminopeptidase). In cancer cells, they are overexpressed and only their inhibition may stop tumor progression. This review presents the clinical outcomes of selected inhibitors and argues the safety of drug usage in human volunteers. Clinical studies of EGFR and Src kinase inhibitors in different tumors clearly show the need for molecular selection of patients (to those with mutations in genes coding EGFR and Src) to achieve positive clinical response. Current data indicates the great necessity for new anticancer treatment and actions to limit off-target activity.
Nowotwory stanowią jedną z głównych przyczyn zgonów na świecie. Dostępne w lecznictwie substancje przeciwnowotworowe charakteryzują się niskim indeksem terapeutycznym jak i wysoką toksycznością. Rozwijająca się oporność komórek nowotworowych na dostępne w terapii leki przyczynia się do konieczności poszukiwania nowych punktów uchwytu/miejsc docelowych (z ang. targets) dla potencjalnych substancji przeciwnowotworowych. Obecnie prowadzonych jest również wiele prac nad nowymi związkami przeciwnowotworowymi o wysokim potencjale terapeutycznym, nowym mechanizmie działania i/bądź wyższym indeksie selektywności. W pracy, autorzy skupili uwagę na trzech grupach enzymów, będących obecnie w obszarze zainteresowań współczesnej medycyny. Omówione zostały kinazy tyrozynowe na przykładzie enzymów EGFR i Src, kinazy Aurora typu A, B i C, a także aminopeptydazy na przykładzie aminopeptydazy leucynowej. Scharakteryzowano klasyfikację enzymów, ich rolę w cyklu komórkowym w warunkach fizjologicznych i procesie nowotworowym. Opisano również inhibitory enzymów, substancje będące w trakcie badań in vitro, przedklinicznych i klinicznych jak i leki wprowadzone na rynek farmaceutyczny. Zwrócono uwagę na budowę chemiczną inhibitorów enzymów i tym samym na kierunek poszukiwań nowych leków przeciwnowotworowych. Omówione enzymy w warunkach fizjologicznych odgrywają ważną rolę w cyklu komórkowym, zwłaszcza na etapie podziału mitotycznego. Jednakże w procesie nowotworowym dochodzi do ich nadekspresji. Zjawisko to można zahamować poprzez inhibicję aktywności enzymu. Autorzy omówili wpływ inhibitorów kinaz tyrozynowych, kinaz Aurora czy aminopeptydaz leucynowych na cykl komórkowy i bezpieczeństwo stosowania tych potencjalnych leków u ludzi. Dotychczasowe badania przedkliniczne i kliniczne inhibitorów kinazy tyrozynowej typu EGFR czy Src potwierdziły konieczność selekcji pacjentów, na tych z mutacją w genie kodującym dany enzym. Badania prowadzone na wybranej grupie chorych przynosiły oczekiwany pozytywny wynik. Wiele aspektów dotyczących nowych punktów uchwytu w terapii przeciwnowotworowej wciąż wymaga dalszych prac, aczkolwiek daje również nadzieję na odkrycie skutecznych i selektywnych leków.
Źródło:
Roczniki Państwowego Zakładu Higieny; 2016, 67, 4
0035-7715
Pojawia się w:
Roczniki Państwowego Zakładu Higieny
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Gamma-radiation-induced ATM-dependent signalling in human T-lymphocyte leukemic cells, MOLT-4
Autorzy:
Tichý, Aleš
Záškodová, Darina
Řezáčová, Martina
Vávrová, Jiřina
Vokurková, Doris
Pejchal, Jaroslav
Vilasová, Zdena
Cerman, Jaroslav
Österreicher, Jan
Powiązania:
https://bibliotekanauki.pl/articles/1041075.pdf
Data publikacji:
2007
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
checkpoint kinase-2
ionizing radiation
p53
ATM kinase
Mdm2
Opis:
ATM kinase (ATM) is essential for activation of cell cycle check points and DNA repair in response to ionizing radiation (IR). In this work we studied the molecular mechanisms regulating DNA repair and cell death in human T-lymphocyte leukemic cells, MOLT-4. Apoptosis was evaluated by flow-cytometric detection of annexin V. Early apoptotic cells were determined as sub-G1 cells and late apoptotic cells were determined as APO2.7-positive ones. Proteins involved in ATM signalling pathway were analysed by Western-blotting. We observed a rapid (0.5 h) phosphorylation of ATM declining after 6 h after irradiation by all the doses studied (1.5, 3.0, and 7.5 Gy). Checkpoint kinase-2 (Chk-2) was also phosphorylated after 0.5 h but its phosphorylated form persisted 4, 2, and 1 h after the doses of 1.5, 3.0, and 7.5 Gy, respectively. The amount of p53 protein and its form phosphorylated on Ser-392 increased 1 h after irradiation (1-10 Gy). The lethal dose of 7.5 Gy caused an immediate induction and phosphorylation of p53 after 0.5 h post-irradiation. At the time of phosphorylation of p53, we found simultaneous phosphorylation of the oncoprotein Mdm2 on Ser-166. Neither ATM nor its downstream targets showed a dose-dependent response after 1 h when irradiated by the doses of 1-10 Gy. MOLT-4 cells were very sensitive to the effect of IR. Even low doses, such as 1.5 Gy, induced apoptosis 16 h after irradiation (evaluated according to the cleavage of nuclear lamin B to a 48-kDa fragment). IR-induced molecular signalling after exposure to all the tested doses was triggered by rapid phosphorylation of ATM and Chk-2. Subsequent induction of p53 protein and its phosphorylation was accompanied by concomitant phosphorylation of its negative regulator, oncoprotein Mdm2, and followed by induction of apoptosis.
Źródło:
Acta Biochimica Polonica; 2007, 54, 2; 281-287
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Inhibition of ehrlich ascites tumour (eat) cells proliferation through chitosan-mediated regulation of activity of the akt pathway
Autorzy:
Ignacak, Jan
Wiśniewska-Wrona, Maria
Dulińska-Litewka, Joanna
Pałka, Iwona
Kucharska, Magdalena
Powiązania:
https://bibliotekanauki.pl/articles/1035195.pdf
Data publikacji:
2014
Wydawca:
Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Tematy:
Akt kinase - PKB
EAT cells proliferation
M2 pyruvate kinase
chitosan
Opis:
Isoenzyme M2 pyruvate kinase, which is a marker of cancer transformation, can take both tetramer (cytosol) and dimer (nucleus) forms. The former is responsible for ATP synthesis, and the latter demonstrates histone H1 kinase activity. Regulation of the expression of pyruvate kinase through which Akt controls the expression of genes involved in Ehrlich ascites tumour (EAT) cell proliferation, migration and death, also involves cross-talk with the other signalling pathways, transcription factors and co-regulatory proteins such as β-catenin and c-Myc. Treatment of EAT cells with chitosans significantly reduced their proliferation (by 45-60%), expression of nuclear β-catenin, c-Myc as well as cell migration. After 48–72 hours of treatment of the cell with oligochitosans, lower levels of p-Akt were detected. Simultaneously, decreased expression of isoenzyme M2 PK protein levels was observed. The dimeric form (nucleus) can participate in H1 histone phosphorylation, which contributes to increased EAT cell proliferation.
Źródło:
Progress on Chemistry and Application of Chitin and its Derivatives; 2014, 19; 33-40
1896-5644
Pojawia się w:
Progress on Chemistry and Application of Chitin and its Derivatives
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
The role of oligochitosans in akt kinase regulation
Autorzy:
Ignacak, Jan
Wiśniewska-Wrona, Maria
Dulińska-Litewka, Joanna
Pałka, Iwona
Kucharska, Magdalena
Powiązania:
https://bibliotekanauki.pl/articles/1034912.pdf
Data publikacji:
2015
Wydawca:
Sieć Badawcza Łukasiewicz - Polskie Towarzystwo Chitynowe
Tematy:
Akt kinase – PKB
EAT cells proliferation
HIF-1 factor.
M2 pyruvate kinase
Opis:
Among characteristic properties of cancers, there is their increased glycolytic activity.Contrary to normal cells, neoplastic cells use anaerobic glycolysis, even when a sufficient amount of oxygen is available. The intensity of the process is associated with a considerable demand for energy in the form of ATP. Akt, which - acting through the mTOR pathway - activates the HIF-1 factor, which in turn activates hexokinase that participates in glucose phosphorylation, stimulates the transport of glucose to cells via increasing glucose transporters (GLUT) and activates lactate dehydrogenase (which transforms pyruvate to lactate). Chitosan, as well as products of its degradation - oligochitosans - contribute to inhibiting the activity of the Akt kinase, and thus contribute to inhibiting excessive glycolytic activity of Ehrlich ascites tumor (EAT) cells and to decreasing proliferation of these cells.
Źródło:
Progress on Chemistry and Application of Chitin and its Derivatives; 2015, 20; 73-81
1896-5644
Pojawia się w:
Progress on Chemistry and Application of Chitin and its Derivatives
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Modulation of human deoxycytidine kinase activity as a response to cellular stress induced by NaF.
Autorzy:
Csapó, Zsolt
Sasvári-Székely, Maria
Spasokoukotskaja, Tatjana
Staub, Mária
Powiązania:
https://bibliotekanauki.pl/articles/1044195.pdf
Data publikacji:
2001
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
tonsil
NaF
deoxycytidine kinase
lymphocytes
Opis:
Deoxycytidine kinase (dCK) is one of the key enzymes of deoxynucleoside salvage supplying resting lymphocytes with DNA precursors for synthesis and repair. The level of dCK activity is especially important in chemotherapy with the use of deoxynucleoside analogues like arabinosyl cytosine (Citarabid, ara-C), or 2-chloro-deoxyadenosine (Cladribine, CdA). Previous results showed that Cladribine treatment of human lymphocytes increased several fold the activity of dCK without increasing the amount of dCK protein itself (Sasvári-Székely, et al., 1998, Biochem. Pharmacol. 56, 1175), and a possible post-translational modification was suggested. This theory was further investigated using NaF as an inhibitor of protein phosphatases. It was shown that NaF treatment of cells elevated dCK activity while inhibiting DNA synthesis. The possible mechanism of dCK activation/inactivation induced by exposure of cell cultures to different agents is discussed.
Źródło:
Acta Biochimica Polonica; 2001, 48, 1; 251-256
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Regulatory mechanisms for the expression and activity of platelet-derived growth factor receptor.
Autorzy:
Funa, Keiko
Uramoto, Hidetaka
Powiązania:
https://bibliotekanauki.pl/articles/1043436.pdf
Data publikacji:
2003
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
review
tyrosine kinase
expression
receptor
PDGF
Opis:
PDGF is one of the most potent serum mitogens, and the signalling mechanism by way of its receptor tyrosine-kinase has been extensively studied since its first purification in 1979. The identification of homology between the simian sarcoma virus oncogene, v-sis, and the B-chain of PDGF, as well as the frequent over-expression of both the ligands and receptors in various tumours and stroma led to the proposal of the PDGF-mediated autocrine and paracrine hypothesis. Consistent with the important roles of PDGF in the growth and survival of cells, the expression and activity of PDGF receptors are tightly controlled by both positive and negative feedback mechanisms at different levels. The deregulation of the control system can result in serious pathological conditions such as chronic inflammation and tumours. Understanding the molecular mechanisms for the regulatory system and the signalling pathway of PDGF is essential in order to find effective therapies in the diseases where PDGF is involved.
Źródło:
Acta Biochimica Polonica; 2003, 50, 3; 647-658
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Ganoderma lucidum extract stimulates glucose uptake in L6 rat skeletal muscle cells
Autorzy:
Jung, Kyung
Ha, Eunyoung
Kim, Mi-Ja
Uhm, Yoon
Kim, Hye
Hong, Seung-Jae
Chung, Joo-Ho
Yim, Sung-Vin
Powiązania:
https://bibliotekanauki.pl/articles/1041224.pdf
Data publikacji:
2006
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
Ganoderma lucidum extract
skeletal muscle
phosphatidylinositol 3-kinase
AMP-activated protein kinase
glucose uptake
Opis:
The effect of Ganoderma lucidum extract on glucose uptake was studied in L6 rat skeletal muscle cells. G. lucidum extract increased glucose uptake about 2-fold compared to control. The extract stimulated the activity of phosphatidylinositol (PI) 3-kinase which is a major regulatory molecule in the glucose uptake pathway. About 7-fold increased activity of a PI 3-kinase was observed after treatment with G. lucidum extract, whereas PI 3-kinase inhibitor, LY294002, blocked the G. lucidum extract-stimulated PI 3-kinase activity in L6 skeletal muscle cells. Protein kinase B, a downstream mediator of PI 3-kinase, was also activated by G. lucidum extract. We then assessed the activity of AMP-activated protein kinase (AMPK), another regulatory molecule in the glucose uptake pathway. G. lucidum extract increased the phosphorylation level of both AMPK α1 and α2. Activity of p38 MAPK, a downstream mediator of AMPK, was also increased by G. lucidum extract. Taken together, these results suggest that G. lucidum extract may stimulate glucose uptake, through both PI 3-kinase and AMPK in L6 skeletal muscle cells thereby contributing to glucose homeostasis.
Źródło:
Acta Biochimica Polonica; 2006, 53, 3; 597-601
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Components of defence strategy induced in Solanum species by elicitor from Phytophthora infestans
Autorzy:
Polkowska-Kowalczyk, L.
Olszak, K.
Tarwacka, J.
Szczegielniak, J.
Muszynska, G.
Wielgat, B.
Powiązania:
https://bibliotekanauki.pl/articles/80345.pdf
Data publikacji:
2013
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
conference
Solanum
signal transduction
protein kinase
reactive oxygen species
mitogen-activated protein kinase
calcium-dependent protein kinase
signalling network
gene expression
signalling pathway
nitroblue tetrazolium
elicitor treatment
Phytophthora infestans
Źródło:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology; 2013, 94, 3
0860-7796
Pojawia się w:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Identification, phylogenetic analyses and subcellular localization of protein phosphatases 2c type (PP2Cs) in Populus trichocarpa
Autorzy:
Betlinski, B.
Vashutina, K.
Gawronski, P.
Karpinski, S.
Powiązania:
https://bibliotekanauki.pl/articles/79950.pdf
Data publikacji:
2013
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
conference
protein phosphatase 2C
protein kinase
mitogen-activated protein kinase
subcellular localization
Populus trichocarpa
phylogenetic analysis
identification
Źródło:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology; 2013, 94, 2
0860-7796
Pojawia się w:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Elements of signalling pathways in the response of Solanum species to Phytophthora infestans
Autorzy:
Polkowska-Kowalczyk, L.
Olszak, K.
Tarwacka, J.
Szczegielniak, J.
Muszynska, G.
Wielgat, B.
Powiązania:
https://bibliotekanauki.pl/articles/80244.pdf
Data publikacji:
2013
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
conference
signalling pathway
Solanum species
Phytophthora infestans
reactive oxygen species
mitogen-activated protein kinase
calcium-dependent protein kinase
Źródło:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology; 2013, 94, 2
0860-7796
Pojawia się w:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
PP2A phosphatase interacts with CPK kinase and regulates pathogenesis responses triggered by intracellular ROS signals
Autorzy:
Kangasjarvi, S.
Denessiouk, K.
Trotta, A.
Konert, G.
Rahikainen, M.
Li, S.
Mhamdi, A.
Noctor, G.
Powiązania:
https://bibliotekanauki.pl/articles/80995.pdf
Data publikacji:
2013
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
conference
protein phosphatase 2A
calcium-dependent protein kinase
reactive oxygen species
organelle
protein kinase
plant immunity
Arabidopsis
Źródło:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology; 2013, 94, 2
0860-7796
Pojawia się w:
BioTechnologia. Journal of Biotechnology Computational Biology and Bionanotechnology
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Bidirectional regulation of renal cortical Na+,K+-ATPase by protein kinase C.
Autorzy:
Bełtowski, Jerzy
Marciniak, Andrzej
Jamroz-Wiśniewska, Anna
Borkowska, Ewelina
Wójcicka, Grażyna
Powiązania:
https://bibliotekanauki.pl/articles/1041555.pdf
Data publikacji:
2004
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
phosphatidylinositol-3-kinase
protein kinase C
cytochrome P450-dependent arachidonate metabolites
Na+,K+-ATPase
Opis:
We examined the role of protein kinase C (PKC) in the regulation of Na+,K+- ATPase activity in the renal cortex. Male Wistar rats were anaesthetized and the investigated reagents were infused into the abdominal aorta proximally to the renal arteries. A PKC-activating phorbol ester, phorbol 12,13-dibutyrate (PDBu), had a dose-dependent effect on cortical Na+,K+-ATPase activity. Low dose of PDBu (10-11 mol/kg per min) increased cortical Na+,K+-ATPase activity by 34.2%, whereas high doses (10-9 and 10-8 mol/kg per min) reduced this activity by 22.7% and 35.0%, respectively. PDBu administration caused changes in Na+,K+-ATPase Vmax without affecting K0.5 for Na+, K+ and ATP as well as Ki for ouabain. The effects of PDBu were abolished by PKC inhibitors, staurosporine, GF109203X, and Gö 6976. The inhibitory effect of PDBu was reversed by pretreatment with inhibitors of cytochrome P450-dependent arachidonate metabolism, ethoxyresorufin and 17-octadecynoic acid, inhibitors of phosphatidylinositol 3-kinase (PI3K), wortmannin and LY294002, and by actin depolymerizing agents, cytochalasin D and latrunculin B. These results suggest that PKC may either stimulate or inhibit renal cortical Na+,K+-ATPase. The inhibitory effect is mediated by cytochrome P450-dependent arachidonate metabolites and PI3K, and is caused by redistribution of the sodium pump from the plasma membrane to the inactive intracellular pool.
Źródło:
Acta Biochimica Polonica; 2004, 51, 3; 757-772
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Characterization of dual specificity protein kinase from maize seedlings.
Autorzy:
Trojanek, Joanna
Klimecka, Maria
Fraser, Anna
Dobrowolska, Grażyna
Muszyńska, Grażyna
Powiązania:
https://bibliotekanauki.pl/articles/1041540.pdf
Data publikacji:
2004
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
dual specificity kinase
tyrosine phosphorylation
maize
Opis:
A protein kinase of 57 kDa, able to phosphorylate tyrosine in synthetic substrates pol(Glu4,Tyr1) and a fragment of Src tyrosine kinase, was isolated and partly purified from maize seedlings (Zea mays). The protein kinase was able to phosphorylate exogenous proteins: enolase, caseins, histones and myelin basic protein. Amino acid analysis of phosphorylated casein and enolase, as well as of phosphorylated endogenous proteins, showed that both Tyr and Ser residues were phosphorylated. Phosphotyrosine was also immunodetected in the 57 kDa protein fraction. In the protein fraction there are present 57 kDa protein kinase and enolase. This co-purification suggests that enolase can be an endogenous substrate of the kinase. The two proteins could be resolved by two-dimensional electrophoresis. Specific inhibitors of typical protein-tyrosine kinases had essentially no effect on the activity of the maize enzyme. Staurosporine, a nonspecific inhibitor of protein kinases, effectively inhibited the 57 kDa protein kinase. Also, poly L-lysine and heparin inhibited tyrosine phosphorylation by 57 kDa maize protein kinase. The substrate and inhibitor specificities of the 57 kDa maize protein kinase phosphorylating tyrosine indicate that it is a novel plant dual-specificity protein kinase.
Źródło:
Acta Biochimica Polonica; 2004, 51, 3; 635-647
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Design, Synthesis and Biological Evaluation of Novel Benzo[4,5]thiazolo[2,3-c][1,2,4]triazole Derivatives as Potential Anticancer Agents
Autorzy:
Abdelazeem, Ahmed H.
Gouda, Ahmed M.
Omar, Hany A.
Alrobaian, Majed
Powiązania:
https://bibliotekanauki.pl/articles/895393.pdf
Data publikacji:
2018-06-30
Wydawca:
Polskie Towarzystwo Farmaceutyczne
Tematy:
apoptosis
anticancer
S-benzothiazolotriazole
Kinase
caspase3/7
Opis:
In the present study, we have designed and synthesized a novel series of benzothiazolotriazole derivatives as potential anticancer agents. The anticancer activity of the newly synthesized compounds was evaluated against three cancerous cell lines; A549 (human lung adenocarcinoma), MCF-7 (human breast carcinoma) and Hep3B (human hepatocellular carcinoma) using MTT assay. Among this series, compounds 15 and 16 showed the most promising anticancer activity with IC50 values between 11.1 to 21.5 μM. Kinase profiling was performed for the most potent compounds 15 and 16 and it revealed weak inhibitory activity against 10 various kinases, where the highest inhibition was against CDK2/Cyclin A1 by compound 15. Furthermore, caspase-3/7 assay also indicated that the same compound 15 has the ability to induce apoptosis through the activation of effector caspase-3/7 family. Therefore, it could be deduced that the S-benzo[4,5]thiazolo[2,3-c][1,2,4]triazole is a promising novel anticancer scaffold with antiproliferative and apoptosis-inducing activities deserves to be taken up as a lead for further structural optimization.
Źródło:
Acta Poloniae Pharmaceutica - Drug Research; 2018, 75, 3
0001-6837
2353-5288
Pojawia się w:
Acta Poloniae Pharmaceutica - Drug Research
Dostawca treści:
Biblioteka Nauki
Artykuł

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