• The experiments reported herein were designed to

  2022-03-15

  

  The experiments reported herein were designed to test whether co-expression of MRP and GSTP1-1 offers a level of protection from certain cytotoxic drugs not achieved by the expression of either protein alone. This was accomplished by stable transfection with expression vectors into MCF7/WT cells, w

• GSK is inhibited by serine phosphorylation at a residue its

  2022-03-15

  

  GSK-3 is inhibited by serine enolase at a residue its N-terminus (Ser 9 in GSK-3β and Ser 21 in GSK-3α) [52], [53], [54]. This raised the possibility that the N-terminal tail may function as a pseudo-substrate by mimicking the pre-phosphorylated substrate. The interaction mode of the pseudo-substrat

• br Introduction br Mitochondrial dysfunction and

  2022-03-15

  

  Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu

• Human GPR hGPR was originally isolated in as an orphan

  2022-03-15

  

  Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,

• Acknowledgements br Introduction The neurotransmitter glycin

  2022-03-15

  

  Acknowledgements Introduction The neurotransmitter glycine acts through two receptors: a strychnine-sensitive glycine receptor (GlyA) and a strychnine-insensitive glycine receptor (GlyB). GlyA is localized to the neuronal membrane post-synaptic to inhibitory glycinergic neurons, whereas GlyB is

• It is increasingly argued that the

  2022-03-14

  

  It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit hydroxypropyl beta cyclodextrin australia of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with th

• The eradication of agonist activity in

  2022-03-14

  

  The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary salidroside as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize

• Subsequently we decided to test whether the orexin pathway w

  2022-03-14

  

  Subsequently, we decided to test whether the orexin pathway was involved (Delhanty et al, 2012, Delhanty et al, 2013, Pei et al, 2014). Orexin neuronal systems are known to control limbic and neocortical structures (Bonnavion, de Lecea, 2010, Sakurai, 2007). Orexin receptors and possibly orexin synt

• Recently they reported an enyne chemotype

  2022-03-14

  

  Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral g418 (tmax=15min) and a decent pharmacokinetic profile, a satisf

• br Clinical development of FGFR inhibitors

  2022-03-14

  

  Clinical development of FGFR inhibitors in breast cancer The rationale to explore the role of FGFR inhibitors in patients with breast cancer comes from a variety of sources. These include genomic aberrations frequently identified in the FGF/FGFR pathway in breast cancer, the increased sensitivit

• In the FARM motifs of GGPPSs hydrophobic amino acids

  2022-03-14

  

  In the FARM motifs of GGPPSs, hydrophobic cholinesterase inhibitors are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesses GGPP

• CDX is also a tumor suppressor gene the ablation

  2022-03-14

  

  CDX1 is also a tumor suppressor gene; the ablation of CDX1 and CDX2 results in a significant increase in tumor formation in the colon. CDX1 is regulated by epigenetic modification; the hypermethylation of the CpG island at the promoter is positively associated with severe clinical phenotypes. In add

• The EZH overexpression group exhibited upregulated CEP expre

  2022-03-14

  

  The EZH2 overexpression group exhibited upregulated CEP55 expression but downregulated methylation, suggesting that changes in EZH2 expression in lung adenocarcinoma result in differences of CEP55 methylation and expression. Moreover, according to TCGA database and GSE27262 chip data, CEP55 expressi

• The present study was designed to clarify the

  2022-03-14

  

  The present study was designed to clarify the distribution and the function of the endothelin receptors in the guinea-pig urinary bladder. We found that endothelin-1 produced a clear tonic contraction via both 5959 subtypes, the endothelin ETA and ETB receptor, and that sarafotoxin S6c also induced

• Much evidence has demonstrated that the differential

  2022-03-14

  

  Much evidence has demonstrated that the differential HER2 level between normal tissue and a tumor helps to define HER2 as an ideal diagnostic and treatment target. Thus, HER2 status can be incorporated into a clinical decision, along with other prognostic factors, such as the Pyridoxal 5 phosphate

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