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Additionally regulation of GPCR heteromerization by specific
2023-04-19

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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A selected set of these new derivatives
2023-04-19

A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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tmn br Conflict of interest br
2023-04-19

Conflict of interest Acknowledgments This work was supported by research grant [PR26/20326] from Santander Bank/UCM. The authors would like to thank Miguel Capo, Professor of Toxicology from the Universidad Complutense de Madrid, for his counseling during the preparation of the present work.
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There is also a literature
2023-04-19

There is also a literature on the impact of commodity (consumption) taxation under imperfect competition. Besley (1989) applies a Cournot model, in which production takes place under IRS and in which free entry leads to an excessive number of firms in the market. Introducing a distortive specific co
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Many ruthenium complexes were tested as potential anticancer
2023-04-18

Many ruthenium complexes were tested as potential anticancer agents and two complexes, namely NAMI-A (trans-[imH] [RuCl4(dmso-S)(im)]; im, imidazole) and KP1019 (trans-[indH][RuCl4(ind)2]; ind, indazole) have successfully entered clinical trials [27], [28]. NAMI-A is selectively active against metas
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Thus phosphorylation of p was used to measure
2023-04-18

Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc GSK2126458 expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]. Re
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To circumvent these issues multiple approaches have been dev
2023-04-18

To circumvent these issues, multiple approaches have been developed that target small fractions of the genome, thus reducing the sequencing burden (Dostie et al., 2006; Fullwood et al., 2009; Mumbach et al., 2016). Application of one such approach, chromosome conformation capture carbon copy (5C), w
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Although the interactions of PhLP with G and its
2023-04-18

Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls FTI 277 HCl signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its interacting partners
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br AR signals and chemosensitivity
2023-04-17

AR signals and chemosensitivity in urothelial cancer A significant amount of patients with urothelial cancer fail to respond to cisplatin-based systemic chemotherapy, although it remains the mainstay of successful management of advanced disease. However, underlying mechanisms for chemoresistance
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br Concluding remarks The past decade has
2023-04-17

Concluding remarks The past decade has seen rapid advances in our understanding of the metabolic reprogramming that occurs during tumorigenesis. Strategies to target specific nodes of cancer cell amino PF-477736 metabolism have progressed from preclinical studies to clinical trials, and are show
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The cavity volume of the binding pocket
2023-04-17

The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino Posaconazole substitution within a binding pocket may result in a change in the cavity volume. This, in turn, may a
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Young et al described the role of adenine
2023-04-17

Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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AMPK is an essential player in adiponectin signaling pathway
2023-04-17

AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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It has been suggested that the suppression of LOX could
2023-04-17

It has been suggested that the suppression of 5-LOX could promote apoptotic signaling pathways in cancers [6]. However, the role of 5-LOX in modulating apoptotic factors and neutrophil activation during ANP has not yet been evaluated. In this study, we aimed to evaluate the expression of 5-LOX in pa
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The anorexic effect observed when
2023-04-17

The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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