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Acknowledgements We appreciated the contributions of
2022-06-28

Acknowledgements We appreciated the contributions of Ana Carolina Galha, Selma XSL Pinheiro and Islene Azevedo for technical assistances. In addition, we wish to thank Adilson José de Almeida (in memoriam), Moyra M Portilho, Vanessa A Marques and Letícia P Scalioni, for data analysis during the set
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Substrate affinity and specificity can be enhanced by dockin
2022-06-28

Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of Agarose GPG/ME synthesis bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recog
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Glutathione S transferases constitute a family
2022-06-28

Glutathione-S-transferases constitute a family of enzymes involved in the detoxification of xenobiotics, signalling cascades and serving as ligandins or/and catalyzing the conjugation of various chemicals and drugs [53]. The present finding indicates significant increase in GST activity in the brain
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Interestingly interactions between Smad and RhoA the other s
2022-06-28

Interestingly, interactions between Smad3 and RhoA, the other small GTPase which is highly homologous to RhoB [9], could not be observed suggesting that the Smad3/RhoB interactions require amino GSK343 residues that are unique to RhoB. Combined with our previous observation that the RhoA gene, which
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Chronic exposure of cells to cytotoxic drugs can result
2022-06-28

Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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Among prostaglandins PG PGD remained the most elusive
2022-06-28

Among prostaglandins (PG), PGD2 remained the most elusive species for a long time and was initially regarded as having negligible biological activity [1]. In 1974 its inhibitory effect on platelet aggregation was discovered by Smith et al. [2] and Mills & McFarlain [3], and both pressor and depresso
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There is sufficient evidence to indicate that kisspeptin pla
2022-06-28

There is sufficient evidence to indicate that kisspeptin plays a role in regulating sheep reproduction. However, the molecular mechanism by which kisspeptin regulates GnRH Mdivi 1 and reproduction has remained unclear. Therefore, in this study on GnRH in sheep, the promoter region of GnRH was clone
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Glycogen synthase kinase GSK is currently considered
2022-06-28

Glycogen synthase kinase 3 (GSK3) is currently considered to be a multifunctional serine/threonine kinase involved in a wide spectrum of cellular processes such as glycogen metabolism, cell proliferation, neuronal function, oncogenesis or embryonic development (for recent reviews see: Rayasam et al.
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k j and d were
2022-06-28

15k, 15j and 14d, were then submitted to metabolic stability studies in human and mouse liver microsomes and permeability test with Caco-2 cells (Table 7). 15k, 15j and 14d all retained excellent permeability (Papp value greater than 15.2 × 10−6 cm/s) and displayed modestly improved metabolic stabil
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Axons are the largest component of WM by volume
2022-06-28

Axons are the largest component of WM by volume and are a significant repository of intracellular glutamate that can be releases under ischemic conditions [1,3,4,29,117]. We have recently shown that the principle route by which mature myelinated ABC294640 mg release glutamate during acute ischemia
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Because of its role in the cleavage of A
2022-06-27

Because of its role in the cleavage of Aβ and the fact that many genetic forms of AD are caused by mutations in the enzyme, GS has long been a target for drug development, though previous clinical trials of Semagacestat, a GS inhibitor, have failed due to an increase in skin cancer, and a decrease i
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FFA expression was also noted to be upregulated in
2022-06-27

FFA4 expression was also noted to be upregulated in eight human CRC cell lines. Compared to two normal colon cell lines with relative one-fold expression of FFA4, CRC cell lines HCT116 (3.5-fold higher), Colo205 (3-fold), Caco-2 (2.2-fold), HT-29 (2.3-fold), RKO (2.8-fold), DLD-1 (2.9-fold), SW480 (
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br Results The RAS MEK ERK
2022-06-27

Results The RAS/MEK/ERK pathway is a potential target of FGFR signaling. Indicative for its activation is the presence of double phosphorylated (activated) ERK (dpERK), which is generated in a series of phosphorylation events downstream of FGFR (op. cit. (Lemmon and Schlessinger, 2010)). Followin
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br Declaration of interest br
2022-06-27

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes
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Last we demonstrate that the role of EZH as a
2022-06-27

Last, we demonstrate that the role of EZH2 as a transcriptional activator, with AR being a key target, coexists with its conventional catalytic role in gene repression and plays important oncogenic functions in AR-driven PCa (Figure 7F). Enzymatic EZH2 inhibitors such as EPZ and GSK126, although eff
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