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AK-7 receptor Congenital Gcgr mice exhibit increased hepatic
2022-10-12
Congenital Gcgr mice exhibit increased hepatic Fgf21 expression and circulating FGF21 levels. Previous studies by other investigators demonstrated that neutralization of circulating FGF21 with specific AK-7 receptor impairs glucose control in these mice [6]. In addition, the FGF21 analog LY2405319
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As we showed earlier a to
2022-10-11
As we showed earlier [19], a 20- to 30-min incubation with 2mM t-BHP resulted in erythrocyte swelling, which was less in a Ca2+-containing medium. Given that this effect was abolished in the presence of the Gardos channel inhibitor CLT, as well as in media high in K+, we suggested the contribution f
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The chemical structure of BAs consists of
2022-10-11
The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox
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Much is known about FPPS structure and function
2022-10-11
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and Pa
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In order to estimate the influence of
2022-10-10
In order to estimate the influence of mitochondrial hypo-polarization on generated OMP, IMP was changed from the normal value of Δψi = −140 mV (Fig. 4A, D, G) to Δψi = −100 mV (Fig. 4B, E, H), resulting in lower magnitudes of calculated OMP for hypo-polarized Fructose australia (Fig. 4B). Similarly
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Activation of sGC induces the generation of
2022-10-10
Activation of sGC induces the generation of cyclic guanosine monophosphate (cGMP), phosphorylation of protein kinase G (PKG) and changes in activity of effector proteins such as phosphodiesterases (PDE), ion channels and ion pumps [43]. This pathway eventually leads to dilation of Regorafenib (bronc
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We have shown previously that activation of the
2022-10-10
We have shown previously that activation of the TGFβ/Smad signaling pathway in keratinocytes regulates 5-Formyl-CTP cytoskeleton organization via non-genomic and genomic mechanisms and that RhoB gene is a target of Smad proteins [12,13]. Although the role of RhoB in early non-genomic TGFβ-induced c
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Introduction l Glutamate is a major excitatory
2022-10-09
Introduction l-Glutamate is a major excitatory neurotransmitter in the mammalian central nervous system (CNS) that contributes not only to fast synaptic neurotransmission, but also to complex physiological processes like memory, learning, plasticity, and neuronal cell death [30], [81]. Glutamate is
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br Introduction As is now well known obesity
2022-10-09
Introduction As is now well known, obesity is major risk factor for various diseases such as nonalcoholic fatty liver disease, cardiovascular disease, some cancers (McWilliams and Petersen, 2009), type-2 diabetes mellitus (Jakobsen et al., 2007), and hypertension (Aneja et al., 2004), among other
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Herein we describe the development of second generation GSM
2022-10-09
Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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BRD4770 Moreover intestinal chronic inflammation is a promot
2022-10-08
Moreover, intestinal chronic inflammation is a promoting factor in the development of CRC in patients affected by inflammatory bowel disease (IBD), such as Crohn's disease and ulcerative colitis. We have previously shown that pharmacological FXR activation via its ligand obeticolic BRD4770 countera
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br FXR expression in normal intestine and cancer
2022-10-08
FXR Matrine in normal intestine and cancer Of note, there are several question marks about FXR post-translational modifications (such as acetylation or SUMOylation) and their involvement in the pathogenesis of metabolic and inflammatory disease (Balasubramaniyan et al., 2013, Kemper et al., 2009
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In early a collaborative effort
2022-10-08
In early 2017, a collaborative effort between the group that pioneered the above described evidence of platinum-induced PUFA chemotherapy resistance and a group that has contributed to much of the known molecular pharmacology of FFA4, revealed that the molecular target of 16:4(n-3), which affords ch
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A breakthrough in the understanding of the
2022-10-08
A breakthrough in the understanding of the unique properties of GPX4-downregulation-induced cell death was accomplished when Seiler et al. in 2008 demonstrated the role of 12/15-lipoxygenase (12/15-LOX), a polyunsaturated fatty ep4 metabolizing enzyme [92], in the execution of GPX4-knockout-mediated
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At the molecular level AZ
2022-10-08
At the molecular level AZ scaffold proteins including piccolo and bassoon have been shown to directly or indirectly associate with endocytic and actin-binding proteins such as ABP1 (Fenster et al., 2003), profilin, and GIT (Podufall et al., 2014) (Fig. 2B). ABP1 and profilin, via regulating F-actin,
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