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br Acknowledgements This work was supported by the grants fr
2022-06-05
Acknowledgements This work was supported by the grants from National key Basic Research Program of China (2012CB124702), 948 Program (2015-Z33), National Natural Science Foundation of China (31172093, 31301947), the National Science Foundation for Fostering Talents in Basic Research (J1103510), S
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The HH signaling has also been implicated in the
2022-06-05
The HH signaling has also been implicated in the regulation of cancer stem CCG-1423 sale (CSC) by promoting their self-renewal [53]. Activated HH signaling has been identified in CSCs of many solid tumors, such as glioblastoma, breast, colon, pancreatic cancer, melanoma, and hematological malignanc
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The fine interplay among post translational
2022-06-05
The fine interplay among post-translational modifications and intersection with other pathways, such as PI3K–AKT, has a crucial role in the regulation of GLI activity and in the generation of their repressor forms 40, 41, 42. In addition to β-TrCP, for example, other E3 ligases belonging to the real
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Hydantoin in region F bridging the
2022-06-05
Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,
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To discriminate the peripheral and central involvement of FA
2022-06-02
To discriminate the peripheral and central involvement of FAAH in paracetamol action, we proposed a pharmacological strategy challenging the analgesic action of paracetamol observed in an inflammatory context with either a peripherally-restricted FAAH inhibitor (URB937, Clapper et al., 2010, Moreno-
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br Results br Discussion Previous studies have shown that al
2022-06-02
Results Discussion Previous studies have shown that all the components of ET system are expressed by various neuronal and non-neuronal structures throughout the CNS (McCumber et al., 1990; Giaid et al., 1991). In effect, endothelin-converting enzyme activity, mRNA, ET-1 and ET-3 immunoreactivi
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br Material and methods br Results br Discussion It
2022-06-02
Material and methods Results Discussion It is challenging to discriminate between HIV monoinfection and HIV-1/2 dual infection in settings where both viruses co-exist, due to cross-reactivity in serological tests. Thus, the gold standard for detection of HIV-1/2 dual infection is through NA
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Treatment with histamine had no effect on histamine
2022-06-02
Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 Bazedoxifene HCl (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo A-I prom
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Based on the aforementioned findings variations of the
2022-06-02
Based on the aforementioned findings, variations of the imidazole heterocycle present in the endogenous ligand histamine (1) led to 2-(thiazol-2-yl)ethanamine (2-TEA, 2) and later to 2-(3-bromophenyl)histamine or 2-(3-(trifluoromethyl)phenyl)histamine (3) (Fig. 3). Interestingly, 2-TEA demonstrated
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HOs can be found in
2022-06-02
HOs can be found in both plants and animals and they are evolutionarily conserved proteins [8]. There are two HO isoenzymes: inducible heme oxygenase-1 (HO-1) and constitutive heme oxygenase-2 (HO-2) encoded by different genes [9,10]. Biosynthesis of a stress-inducible HO-1 can be triggered by a var
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The Y H D A
2022-06-02
The Y56H/D168A variant was resistant to all tested PIs, and the inhibitor binding mode determined the molecular mechanism of resistance. Prior to the development of grazoprevir, PIs typically contained large heterocyclic P2 moieties that strongly interacted with S2-subsite residues (Ali et al., 2013
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br Soluble guanylyl cyclase nitric oxide and
2022-06-02
Soluble guanylyl cyclase, nitric oxide and nitric oxide synthase The primary and best-studied endogenous activator of soluble guanylyl cyclase (sGC) is nitric oxide (NO), which was originally describe as endothelium-derived relaxing factor for its potent ability to relax blood vessels in response
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In addition to their functional activation
2022-06-02
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic SB 747651A dihydrochloride to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manne
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learn this here now br Glucose metabolism and diet
2022-06-01
Glucose metabolism and diet Glucokinase is essential for sensing blood glucose levels, thus controls metabolism (Iynedjian, 1993, Iynedjian, 2009, Postic et al., 2001, Agius, 2008). Loss of glucokinase activity in humans and mice leads to diabetes (Printz et al., 1993b, Postic et al., 2001, Agius
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Human GS is a multi subunit complex consisting of four
2022-06-01
Human GS is a multi-subunit complex consisting of four components: presenilin 1 (PS1), presenilin enhancer 2 (PEN-2), anterior pharynx-defective 1A (APH-1A) and nicastrin (NCT) (Fig. 1a) [5,6]. PS1 comprise nine transmembrane helices (TM 1–9) and contains the catalytic aspartate residues in its TM6
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