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In various models histamine has been shown to induce
2022-08-08
In various models, histamine has been shown to induce chemotaxis. This was first appreciated over 40 years’ ago in studies with eosinophils (Clark et al., 1977). At that time, only histamine H1 and histamine H2 receptors were recognized and studies with ligands to these receptors indicated that neit
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br Recently MST emerged as a
2022-08-08
Recently, MST1 emerged as a critical regulator of leukocyte function and autoimmunity in humans. Five independent groups reported on autosomal recessive nonsense mutations in the gene STK4 (which encodes for MST1) in human patients with a novel primary immunodeficiency disease (PID), now called ST
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br Materials and methods br Results br Discussion Numerous s
2022-08-05
Materials and methods Results Discussion Numerous studies have identified important roles for HIF-1α in cellular function and dysfunction through its transcriptional activity [4]. A few studies have reported that HIF-1α is translocated to the mitochondria in human and mouse cancer cell line
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br Conclusion br Conflict of interest br Introduction
2022-08-05
Conclusion Conflict of interest Introduction The human epithelial receptor 2 (HER2 or erbb2) is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases that act through the EGF signaling cascade [1,2]. Approximately 20% of breast cancers overexpress HER2
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Finally worth of mention are few papers that
2022-08-05
Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a Decoquinate library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first series
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Anti apoptotic Bcl proteins have become attractive targets
2022-08-05
Anti-apoptotic Bcl-2 proteins have become attractive targets for anti-cancer agents development, because they are associated with progression of a wide variety of human cancers., , The small-molecular Bcl-2 inhibitor venetoclax (ABT-199) () has been approved recently for the treatment of patients w
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The endocytic inhibitors MDC and
2022-08-05
The endocytic inhibitors MDC and CPZ and dynamin GTPase blocker (dynamin mutant) have been shown to significantly decrease the intracellular accumulation of cGMP. Moreover, earlier reports suggested that G-protein-coupled receptor (GPCRs) continue to signal by generating cAMP throughout internalizat
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It is extremely difficult to predict a plausible conformer
2022-08-05
It is extremely difficult to predict a plausible conformer of hsGCαβ heterodimer with right orientation of multiple domains. Even though the template identities in case of dimeric domains were not high enough but still we modelled the entire heterodimeric structure of hsGCαβ with a reasonable and ju
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In contrast the sGC activator BAY relaxed the CC in
2022-08-05
In contrast, the sGC activator BAY 58-2667 relaxed the CC in a concentration-dependent manner (Figure 4B), a response that was significantly increased in the CC of sGCβ1ki/ki mice compared with WT mice. The finding that BAY 58-2667 also possessed a corporal relaxing effect in WT mice is suggestive b
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The crystal structures of plant class ADH
2022-08-05
The crystal structures of plant class ADH3/GSNOR from Arabidopsis thaliana (AtGSNOR) and Solanum lycopersicum cv. Amateur (SlGSNOR) with bound substrates and cofactors revealed important differences between plant and human enzyme, namely within the substrate-binding pocket. GSNOR are unusually homod
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Lipid sensing GPCRs as therapeutic targets G protein coupled
2022-08-05
Lipid-sensing GPCRs as therapeutic targets G-protein-coupled receptors (GPCRs) comprise a family of cell-surface receptors that respond to various extracellular stimuli such as light, odorants, neurotransmitters and hormones, and trigger a cascade of intracellular signaling. There are approximately
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Lactate LA the end product of aerobic
2022-08-05
Lactate (LA), the end product of aerobic glycolysis, has been long neglected and seen as a byproduct until recently the findings for its important role in global gene transcription, cancer progression, functional polarisation of immune look at and the sustenance of stem cells [[7], [8], [9]]. Lacta
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br The mode of binding of ligands to GPR
2022-08-05
The mode of binding of ligands to GPR35 As noted above, although kynurenic Sulfamethazine is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Importantly, i
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In addition to these effects
2022-08-05
In addition to these effects on metabolic function in cardiac cells, this study also demonstrates changes in the expression of hypertrophic genes and proteins subsequent to GPR119 activation. Again this occurred in a distinct pattern dependent on palmitate exposure. Of interest SOCS3 mRNAs were decr
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In the present study we aimed to
2022-08-05
In the present study, we aimed to investigate the effect of a common dairy and beef genetic background on the mRNA GSK2636771 of the AdipoQ system and GPR109A in different adipose depots and liver. Materials and Methods Results Comparing fat masses between families (fat-type vs. lean-type co
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