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Wyszukujesz frazę "nuclear receptor" wg kryterium: Temat


Wyświetlanie 1-8 z 8
Tytuł:
Functionality versus strength - has functional selection taken place in the case of the ecdysteroid receptor response element?
Autorzy:
Grad, Iwona
Kochman, Marian
Ożyhar, Andrzej
Powiązania:
https://bibliotekanauki.pl/articles/1043745.pdf
Data publikacji:
2002
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
ultraspiracle
nuclear receptor
Drosophila
protein-DNA interaction
ecdysteroid receptor
20-hydroxyecdysone
Opis:
Nuclear receptors are ligand-dependent transcription factors responsible for controlling differentiation, growth and development of higher eukaryotes. Three amino acids within the recognition α-helix of the DNA-binding domain of the nuclear receptors constitute the so-called "P-box" which determines response element specificity. In the ultraspiracle (Usp) protein, which together with EcR forms the heterodimeric ecdysone receptor, the P-box residues are E19, G20 and G23. Substitution of E19, the most characteristic amino acid for estrogen receptor-like P-boxes, with alanine showed that the mutation did not appreciably alter the affinity of the wild-type Usp DNA-binding domain (UspDBDWT) for a probe containing natural ecdysone response element (hsp27wt). Since in many cases E19 contacts a G/C base pair in position -4, which is absent in hsp27wt, we analysed the interaction of UspDBDWT, E19A and other P-box region mutants with the hsp27wt derivative which contains a G/C instead of an T/A base pair in position -4. UspDBDWT exhibited higher affinity for this element than for hsp27wt. Moreover, a different interaction pattern of P-box region mutants was also observed. Thus we conclude that the E19 residue of UspDBD is not involved in any hsp27wt sequence-discerning contacts. However, substitution of the hsp27wt T/A base pair in position -4 with G/C generates target sequence with distinct functional characteristics and possibly with a new specificity. These results could serve as a basis for understanding the role of the presence of a T/A or G/C base-pair in the position -4 in the two types of ecdysone response elements found in nature.
Źródło:
Acta Biochimica Polonica; 2002, 49, 3; 747-756
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Recent advances in computational chemistry for identification of ligands for biological receptors: interdisciplinary aspects
Autorzy:
Todorov, M.
Powiązania:
https://bibliotekanauki.pl/articles/1715.pdf
Data publikacji:
2018
Wydawca:
Uniwersytet Opolski. Instytut Nauk o Zdrowiu
Tematy:
computational chemistry
identification
ligand
biological receptor
nuclear receptor
human health
interdisciplinary aspect
QSAR method
Opis:
Background: Computational (in silico) methods, such as quantitative structure-activity relationships (QSARs) are already well recognized and used in many screening programs related to environmental, industrial and medical chemistry. The main idea of the QSAR is that there is a relationship between molecular structure and ultimate biological effect caused by a chemical compound. In this respect the approach could be used successfully for prediction of various biological endpoints caused by chemical compounds including receptor binding affinity. Aim of the study: In the current study the capabilities for structure-activity modelling incorporated in noncommercial software tool have been employed for investigating the binding effect of xenobiotics toward estrogen and human pregnane X receptor. Material and methods: The analysis was performed by making use of the non-commercial software platform QSAR Toolbox. This system allows application of a set of built-in models for different biological effects, and also allows incorporation of new models for other endpoints. Results: Two models have been applied for predicting the binding effect toward estrogen and human pregnane X receptors of a large number of chemicals collected in a single database of high practical concern. The results show that there are many chemicals which are able to bind the investigated receptors. Since those chemicals are encountered in the environment, they could be considered as potential threat for society. Conclusions: The obtained results could be used as initial step for further experimental testing of those chemicals in order to confirm their potential to harm biological systems in the body.
Źródło:
Medical Science Pulse; 2018, 12, 1
2544-1558
2544-1620
Pojawia się w:
Medical Science Pulse
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
In silico study by using ProTox-II webserver for oral acute toxicity, organ toxicity, immunotoxicity, genetic toxicity endpoints, nuclear receptor signalling and stress response pathways of synthetic pyrethroids
Autorzy:
Ghosh, Subhasis
Tripathi, Puja
Talukdar, Partha
Talapatra, Soumendra Nath
Powiązania:
https://bibliotekanauki.pl/articles/1065392.pdf
Data publikacji:
2019
Wydawca:
Przedsiębiorstwo Wydawnictw Naukowych Darwin / Scientific Publishing House DARWIN
Tematy:
In silico study
Molecular mechanism of toxicity
Nuclear receptor signalling and stress response pathways
Predictive toxicology
Synthetic pyrethroids
Opis:
Till date, it is well-known that synthetic pyrethroids are safe to mammal but toxic to non-mammals. The present objective was an in silico study to detect oral acute toxicity, organ toxicity, immunotoxicity, genetic toxicity endpoints, nuclear receptor signalling, and stress response pathways of common synthetic pyrethroids by using ProTox-II webserver. The chemical compounds especially different synthetic pyrethroids such as pyrethrin I, Cinerin I and Jasmolin I (esters of Chrysanthemic acid), Pyrethrin-II, Cinerin II and Jasmolin II (Esters of Pyrethric acid), type I pyrethroids (esters without alpha-cyano group) such as allethrin, resmethrin, permethrin and bifenthrin and type II pyrethroids (esters with alpha-cyano group) such as fenvalerate, cyhalothrin, cypermethrin and deltamethrinwere selected from available literature. ProTox-II webserver was used for toxicological assessment in organism, organs, cell and gene level along with molecular mechanisms of toxicity. The predictive results for the toxicity of common synthetic pyrethroids compounds, Deltamethrin showed highly toxic compound among 14 compounds as fatal if swallowed as class II followed by Cypermethrin, Cyhalothrin, Bifenthrin, Resmethrin, Fenvalerate and Permethrin but hepatotoxic potential was only Deltamethrin and Fenvalerate while immunotoxic was obtained Permethrin. On the other hand, none of the compounds were obtained cytotoxic and carcinogenic but 9 compounds viz. Pyrethrin I, II Cinerin I, II, Jasmolin I, II, Allethrin, Resmethrin and Permethrin were observed mutagenic active. In case of NR signalling pathways, all compounds were inactive but eight compounds such as Pyrethrin I, II, Cinerin I, II, Jasmolin I, II, Allethrin and Resmethrin were obtained nrf2/ARE and HSE active while MMP active compounds were obtained Fenvalerate, Cyhalothrin and Deltamethrin respectively. For p53 and ATAD5 parameters, all fourteen compounds such as were obtained inactive. In conclusion, the present predictive results are suitable for academician, researchers, industries, etc. those who are making drugs and environmental chemicals. This web server helps faster screening of large numbers of compounds within short duration and no animal testing. This present in silico study easily detects toxin(s), which can be validated in future through in vitro and in vivo experimental assay.
Źródło:
World Scientific News; 2019, 132; 35-51
2392-2192
Pojawia się w:
World Scientific News
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Gonadotropin-releasing hormone and kisspeptin-10 regulate nuclear receptor subfamily 5 group a member 1/catenin beta 1/nuclear receptor subfamily 0 group B member 1 activity in female rat anterior pituitary gland
Autorzy:
Zielinska-Gorska, M.
Gorski, K.
Biernacka, K.
Sawosz, E.
Kaminski, T.
Gajewska, A.
Powiązania:
https://bibliotekanauki.pl/articles/69453.pdf
Data publikacji:
2018
Wydawca:
Polskie Towarzystwo Fizjologiczne
Tematy:
gonadotrophin releasing hormone
neuronal network
mRNA expression
kisspeptin-10
nuclear receptor
anterior pituitary gland
ovariectomy
luteinizing hormone
rat
Źródło:
Journal of Physiology and Pharmacology; 2018, 69, 3
0867-5910
Pojawia się w:
Journal of Physiology and Pharmacology
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Nuclear progesterone receptor isoforms and their functions in the female reproductive tract
Autorzy:
Rekawiecki, R.
Kowalik, M.
Kotwica, J.
Powiązania:
https://bibliotekanauki.pl/articles/32231.pdf
Data publikacji:
2011
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
nuclear receptor
female
reproductive tract
progesterone
isoform
function
embryo
corpus luteum
reproductive system
endocrine gland
ovulation
ovarian follicle
hormone
cattle
animal physiology
Opis:
Progesterone (P4), which is produced by the corpus luteum (CL), creates proper conditions for the embryo implantation, its development, and ensures proper conditions for the duration of pregnancy. Besides the non-genomic activity of P4 on target cells, its main physiological effect is caused through genomic action by the progesterone nuclear receptor (PGR). This nuclear progesterone receptor occurs in two specific isoforms, PGRA and PGRB. PGRA isoform acts as an inhibitor of transcriptional action of PGRB. The inactive receptor is connected with chaperone proteins and attachment of P4 causes disconnection of chaperones and unveiling of DNA binding domain (DBD). After receptor dimerization in the cells’ nucleus and interaction with hormone response element (HRE), the receptor coactivators are connected and transcription is initiated. The ratio of these isoforms changes during the estrous cycle and reflects the different levels of P4 effect on the reproductive system. Both isoforms, PGRA and PGRB, also show a different response to the P4 receptor antagonist activity. Connection of the antagonist to PGRA can block PGRB, but acting through the PGRB isoform, P4 receptor antagonist may undergo conversion to a strongly receptor agonist. A third isoform, PGRC, has also been revealed. This isoform is the shortest and does not have transcriptional activity. Alternative splicing and insertion of additional exons may lead to the formation of different PGR isoforms. This paper summarizes the available data on the progesterone receptor isoforms and its regulatory action within the female reproductive system.
Źródło:
Polish Journal of Veterinary Sciences; 2011, 14, 1
1505-1773
Pojawia się w:
Polish Journal of Veterinary Sciences
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Magnolol inhibits Streptococcus suis-induced inflammation and ROS formation via TLR2/MAPK/NF-κB signaling in RAW264.7 cells
Autorzy:
Wang, J.
Sun, Y.
Zhang, L.
Xu, W.
You, J.
Lu, H.
Song, Y.
Wei, J.
Li, L.
Powiązania:
https://bibliotekanauki.pl/articles/2087779.pdf
Data publikacji:
2018
Wydawca:
Polska Akademia Nauk. Czytelnia Czasopism PAN
Tematy:
magnolol
Streptococcus suis
Toll-like receptor2
mitogen-activated protein kinase
nuclear factor Kappa B
Źródło:
Polish Journal of Veterinary Sciences; 2018, 21, 1; 111-118
1505-1773
Pojawia się w:
Polish Journal of Veterinary Sciences
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Side-chain modified vitamin D analogs require activation of both PI 3-K and erk1,2 signal transduction pathways to induce differentiation of human promyelocytic leukemia cells.
Autorzy:
Marcinkowska, Ewa
Kutner, Andrzej
Powiązania:
https://bibliotekanauki.pl/articles/1043768.pdf
Data publikacji:
2002
Wydawca:
Polskie Towarzystwo Biochemiczne
Tematy:
CD11b
cytosolic phospholipase A2
p70S6K
nuclear vitamin D receptor
CD14
analogs
phosphatidylinositol 3-kinase
extracellular-signal regulated kinase
1,25-dihydroxyvitamin D3
HL-60 cells
differentiation
Opis:
Synthetic analogs of vitamin D for potential use in differentiation therapy should selectively regulate genes necessary for differentiation without inducing any perturbations in calcium homeostasis. PRI-1906, an analog of vitamin D2, and PRI-2191, an analog of vitamin D3 bind nuclear vitamin D receptor (nVDR) with substantially lower affinity than 1,25-dihydroxyvitamin D3 (1,25-D3), but have higher differentiation-inducing activity as estimated in HL-60 leukemia cell model. To examine how their increased differentiation-inducing activity is regulated we tested the hypothesis that membrane-mediated events, unrelated to nVDR, take part in the differentiation in response to PRI-1906 and PRI-2191. The induction of leukemia cell differentiation in response to the analogs of vitamin D was inhibited by LY294002 (phosphatidylinositol 3-kinase inhibitor), PD98059 (inhibitor of MEK1,2, an upstream regulator of extracellular-signal regulated kinase) and rapamycin (p70S6K inhibitor) pointing out that activation of signal transduction pathways unrelated to nVDR is necessary for differentiation. On the other hand, inhibition of cytosolic phospholipase A2 accelerated the differentiation of HL-60 cells induced by either 1,25-D3 or by the vitamin D analogs suggesting possible existence of a feedback loop between extracellular-signal regulated kinases and phospholipase A2.
Źródło:
Acta Biochimica Polonica; 2002, 49, 2; 393-406
0001-527X
Pojawia się w:
Acta Biochimica Polonica
Dostawca treści:
Biblioteka Nauki
Artykuł
Tytuł:
Hydrogen sulfide modulates gastric acid secretion in rats via involvement of substance P and nuclear factor-kappaB signaling
Autorzy:
Sun, H.-Z.
Gong, X.-Y.
Wu, L.
Wang, X.-X.
Nie, Y.-N.
Shang, R.
Wang, H.
Li, Y.-C.
Sun, Q.-F.
Gao, P.-F.
Bi, J.-X.
Powiązania:
https://bibliotekanauki.pl/articles/69523.pdf
Data publikacji:
2018
Wydawca:
Polskie Towarzystwo Fizjologiczne
Tematy:
hydrogen sulphide
gastric acid secretion
rat
nuclear factor-kappaB
substance P
transient receptor potential vanilloid type 1
neurokinin-1
Źródło:
Journal of Physiology and Pharmacology; 2018, 69, 3
0867-5910
Pojawia się w:
Journal of Physiology and Pharmacology
Dostawca treści:
Biblioteka Nauki
Artykuł
    Wyświetlanie 1-8 z 8

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