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It has recently been reported
2024-10-28
It has recently been reported that plasma and synovial fluid levels of autotaxin correlate with severity of knee OA. Synovial fibroblasts isolated from OA patients express significant amounts of autotaxin mRNA, and this increase in autotaxin SB 204070 could lead to increased production of LPA, sugg
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To test the compounds metabolic stability
2024-10-28
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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In HepG cells compound showed inhibition of
2024-10-28
In HepG2 cells, epinastine hydrochloride showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditi
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Although the gene that encodes
2024-10-26
Although the gene that encodes DHFR has been strongly conserved during evolution, subtle differences in the active sites of bacterial, human and parasite IOX4 have been exploited to develop DHFR inhibitors specific to particular pathogens 1, 3. For example, pyrimethamine and cycloguanil bind strong
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Long term blood pressure regulation is linked to renal
2024-10-26
Long term blood pressure regulation is linked to renal function through the mechanisms of pressure natriuresis (Evans et al., 2005), which has been shown to be modulated by the RAS (Hall et al., 1999). Key components of the RAS are expressed throughout the kidney, and are implicated in renal excreto
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There are several reports providing evidences
2024-10-26
There are several reports providing evidences that functional and mechanistic connection between Sirt1 and LKB1/AMPK in metabolic regulation [26], [32], [33]. It has been reported that the deacetylation of LKB1 by Sirt1 is one of the determining factors of the subcellular localization of LKB1. In ag
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src inhibitor br Conflict of interest statement br
2024-10-26
Conflict of interest statement Introduction Tanshinone IIA (Tan IIA) is a major active component of Salvia miltiorrhiza (S. miltiorrhiza), a well-known Chinese traditional medicine that is used for the treatment of cardiovascular and cerebrovascular diseases [1]. Tan IIA exhibits diverse pharm
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In summary our data have shown
2024-10-26
In summary, our data have shown that one mechanism by which glucose may mediate monocyte–endothelial cell interaction in the retinal endothelial cells is via the 12/15-LO pathway Furthermore, our current and previously published data [20,22] indicate a differential role of endothelial 12/15-LO versu
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br Translational Considerations Targeting the AHR Pathway Mo
2024-10-26
Translational Considerations Targeting the AHR Pathway Modulating AHR function offers exciting therapeutic potential in host immunity and inflammation. However, the emerging concept of AHR function in a cell type-specific manner, combined with differences between AHR activation in cell culture in
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In a recent series of
2024-10-26
In a recent series of studies from our laboratory, to characterize the contractile systems within the rat (+)-MK 801 synthesis wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and muscarinic agonist
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Voluminous literature about the neuroendocrine mechanism
2024-10-26
Voluminous literature about the neuroendocrine mechanism of reproduction and energy regulation has emerged from studies involving mammalian species. The avian infundibular nucleus (equivalent structure to the mammalian arcuate nucleus) consists of two neuronal populations, one of which expresses neu
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Despite functional studies demonstrating the role of HT
2024-10-26
Despite functional studies demonstrating the role of 5-HT in ureteral contractility, the source of endogenous 5-HT in the ureter is unclear. Since 5-HT-containing enterochromaffin cells, which are present in the gastrointestinal tract, could not be found in the ureter (Nocito et al., 2007, Ripoche,
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Endogenous adenosine systems have largely been
2024-10-26
Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it Baricitinib phosphate is generally
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GSK2606414 Several tertiary prevention studies are currently
2024-10-26
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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Crohn s disease an inflammatory bowel disease
2024-10-25
Crohn’s disease, an inflammatory bowel disease that affects the gastrointestinal (GI) tract, is characterized by a polymorphism in ULK1 autophagy gene due to the presence of single nucleotide polymorphisms (SNPs). Thus, the autophagic process is impaired during the disease. The mutations in the leuc
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