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Negative regulation of AR expression by
2023-12-11

Negative regulation of AR expression by NFκB was also correlated with the ‘age-dependent desensitisation’ of androgen action in the rat liver (Supakar et al., 1995). In this case the binding site was mapped upstream of the gene to sequences −555 to −565 bp, that binds heterodimers of p65 and p50, as
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PF is orally bioavailable and has
2023-12-11

PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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AMG-458 br Acknowledgments The authors thank
2023-12-11

Acknowledgments The authors thank Claudia Wittrock for her excellent technical assistance. The work was supported by grants of the Deutsche Forschungsgemeinschaft (SFB974 TP B05) and of the Anton-Betz-Stiftung to N.K. A.M. is an associate member of the iBrain graduate school at the University of
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Although the effects of adenosine
2023-12-08

Although the effects of adenosine receptor signaling in acute renal IRI have been attributed to the generation of high concentrations of adenosine, we have recently reported an increase in kidney levels of both AMP and adenosine, with a concomitant fall in ATP and ADP. We have also previously demons
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Though we have proved that VA could
2023-12-08

Though, we have proved that VA could suppress hepatic gluconeogenesis, the mechanisms of VA on gluconeogenesis in vivo and in vitro remain unclear. AMP-activated protein kinase (AMPK), which is called an energy receptor enzyme, is widely expressed in liver and other tissues [23]. AMPK has become ano
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br Introduction ACK or Activated Cdc Associated
2023-12-08

Introduction ACK1, or Activated Cdc42-Associated Kinase, located on chromosome 3q, is a ubiquitously expressed non-receptor tyrosine kinase cloned from a human ISCK03 cDNA library (Manser et al., 1993). It was first identified to bind to activated Cdc42, a small Ras GTPase via its CRIB domain (M
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br Regulation and pharmacology of
2023-12-08

Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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Here we show that the co activation of RTKs and
2023-12-08

Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC 5'-Iodoresiniferatoxin and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhib
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br Materials and methods br Results and discussion
2023-12-08

Materials and methods Results and discussion In our previous studies (Matarneh et al., 2017), mitochondria were mechanically disrupted and separated into supernatant and pellet fractions by centrifugation. The causative agent for enhnced glycolytic flux was shown to be a protein that resides i
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br Conflicts of interest br Introduction Phosphatidic acid
2023-12-08

Conflicts of interest Introduction Phosphatidic cotransport phosphatase (PAP) enzymes are responsible for catalyzing the reaction that dephosphorylates phosphatidic acid (PA), which in turn produces diacylglycerol (DAG) and a phosphate group during phospholipid regulation (Fig. 1A) [1]. Subse
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br Aromatase the key enzyme for estrogen
2023-12-08

Aromatase: the key enzyme for estrogen formation in adipose tissue Estrogens are synthesized from androgens by aromatase, a member of the cytochrome P450 superfamily, which is the rate-limiting enzyme in estrogen biosynthesis (Santen et al, 2009, Simpson et al, 1994). At the cellular level, aroma
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Apoptosis a major process of programmed cell death and
2023-12-08

Apoptosis, a major process of programmed cell death, and in response to many chemopreventive agents (Jeyamohan et al., 2016). In general, two major signaling pathways control apoptosis, namely, a pathway mediated by cell death receptor and a pathway mediated by mitochondrion, and possible drug targe
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In this study we have generated
2023-12-08

In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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PGC mediated mitochondrial biogenesis in brown fat
2023-12-08

PGC-1α-mediated mitochondrial biogenesis in brown fat and endothelial Demethoxycurcumin is in part regulated by eNOS and NO [28], [29]. Recent studies indicate that H2S not only augments NO bioavailability and signaling [11], [17], but provides protection against cardiac injury in an eNOS-dependent
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br Role of AMPK in inflammation
2023-12-08

Role of AMPK in inflammation signaling Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), activate Ikβ kinase (IKKβ), which phosphorylates IκBα, triggering the degradation of proteasomal IκB. This liberates active nuclear factor kB (NF-kB) to translocate i
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