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FXR agonists represent an attractive class of
2022-06-24
FXR agonists represent an attractive class of drugs for patients with PFIC. Synthetic and semi-synthetic FXR agonists, with higher affinity and potency to activate FXR, have been successfully tested in animal models of cholestasis. In these murine models, the semi-synthetic steroidal FXR ligand obet
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Although our knowledge of how FAs affect
2022-06-24
Although our knowledge of how FAs affect GLP-1-producing L-cells is sparse and incomplete, increased intracellular ceramide [6], ER stress [12], and increased production of ROS [9] are indicated mediators of the lipotoxicity induced by SFA (16:0). However, the role for/interaction between these medi
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Nuclear factor erythroid like NFE L hereafter NRF plays
2022-06-23
Nuclear factor erythroid 2-like-2 (NFE2L2; hereafter NRF2) plays a crucial role in the basal and inducible expressions of multiple cytoprotective genes in response to electrophilic and oxidative stress [23]. The cytosolic actin-binding protein Kelch-like ECH-associated protein 1 (KEAP1) primarily re
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The Hedgehog signaling pathway HH pathway hereafter is
2022-06-23
The Hedgehog signaling pathway (HH pathway hereafter) is vital for development and tissue homeostasis. [4] In recent years, studying the role of the HH pathway in carcinogenesis and cancer stemness has highlighted the HH inhibitors as putative cancer therapeutics [5]. However, clinical application o
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E6 Berbamine sale In an effort to further improve the intrin
2022-06-23
In an effort to further improve the intrinsic potency, we evaluated the effect of the C4-substituent of the triazole (). Replacement of the phenyl group with a cyclohexyl or with a 2-pyridyl substituent led to losses in potency. Increasing the size of the substituent to a bi-phenyl or naphthyl gr
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cfse Apo E is defined as
2022-06-23
Apo E is defined as a polymorphic protein arising from three alleles. The human Apo E gene was widely studied and described to be located on chromosome 19, closely linked to the Apo C-I/C-II gene complex [9]. The three major alleles, termed Epsilon-2, Epsilon-3 and Epsilon-4 have been reported [10].
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Failure of antioxidant defenses to remove exogenous ROS prod
2022-06-23
Failure of antioxidant defenses to remove exogenous ROS produced by redox cycling chemicals either by being inhibited by those compounds or overwhelmed by an excess ROS, will disrupt the balance between antioxidant/prooxidant system within the organisms leading to oxidative damage (Livingstone, 2003
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In addition to changes in the
2022-06-23
In addition to changes in the Rho isoforms, all Rac isoforms, including the constitutively active splice variant of Rac1, Rac1b, are overexpressed in various tumors and accumulating evidence indicates that they play an important role in the metastatic potential of cancer Anhydrotetracycline hydrochl
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We addressed the role of GSNOR mediated
2022-06-23
We addressed the role of GSNOR-mediated T-cell activation in HHcy-accelerated atherosclerosis in vivo by two mouse models. Generated for the first time, GSNOR-/-ApoE-/- double knock-out mice showed decreased atherosclerosis in aortic roots in response to HHcy. The specificity of GSNOR ablation in T
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Apart from the different assays used
2022-06-23
Apart from the different assays used, biased agonism could also explain the inconsistent pharmacology of GPR55. Indeed, one study compared the effect of LPIs and Virodhamine in HEK293 tnf alpha inhibitor stably transfected with human GPR55. They found that the effect of both ligands on intracellula
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As natural ligands of GPR several long
2022-06-23
As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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br GPR is a class A GPCR expressed on pancreatic
2022-06-23
GPR119 is a class A GPCR expressed on pancreatic β-cells and certain enteroendocrine KU14R synthesis which upon activation with an agonist, increases insulin secretion in response to rising glucose levels. Mechanistically, this insulinotropic effect is bifurcated involving both GPR119-mediated β-c
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Introduction Cancer is known as a renegade system
2022-06-23
Introduction Cancer is known as a renegade system of expansion that initiate in human body. It is distinguished, in spite of its category, by one universal characteristic, which is uncontrolled cell division. Cancerous carboxypeptidase have the ability to bypass the normal apoptosis mechanism (Nat
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Experiments conducted on the human parasite
2022-06-23
Experiments conducted on the human parasite Leishmania major has shown that specific parasitic antigens are involved in steering the immune responses to “protective” as opposed to “disease” state (Reiner et al., 1993; Reiner and Locksley, 1995; and Sjölander et al., 1998) and that antigenic composit
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Berberine hydrochloride br Methods and materials br Results
2022-06-23
Methods and materials Results Overall, free glutamate intakes in US children and adults are shown in Table 1. The sample-weighted mean intake of crude free glutamate was 258 mg/d for children and 322 mg/d for adults. Furthermore, the corresponding energy-adjusted value was 136 mg/1000 kcal and
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