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br General features of FGFRs and inhibitors br
2022-08-19

General features of FGFRs and inhibitors Conclusion Given the critical role of FGFRs in the progression of tumors, the co-crystal structures of these kinases in complex with inhibitors are determined in order to clarify the mechanism of actions and explore new efficient inhibitors. This manusc
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Magtanong et al have demonstrated that MUFAs induce a
2022-08-19

Magtanong et al. (2019) have demonstrated that MUFAs induce a ferroptosis-resistant state in cells in an ACSL3 (acyl-CoA synthetase long-chain family member 3) dependent manner. They observed that MUFAs did not increase the expression of GPX4, which opposes ferroptosis. However, they blocked plasma
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The NGS of six Southern Brazil
2022-08-19

The NGS of six Southern Brazil patients revealed three different variants: c.472C > T (p.Arg158Trp); c.958G>A (p.Gly320Arg) and c.986T>C (p.Leu329Pro) (Table 2). The amino acids involved in these substitutions were evolutionarily conserved in different species (Fig. 1B). The amino (+)- Corydaline in
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More specific quantitative assays for DiXaIs are based
2022-08-19

More specific quantitative assays for DiXaIs are based on the inhibition of chromogenic or clotting activity of Factor Xa. During drug development, Kubitza developed an endogenous Anti-Factor Xa assay [45], which is very sensitive to Rivaroxaban drug concentration. This assay was based on Factor Xa
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Introduction Hedgehog HH signaling regulates
2022-08-19

Introduction Hedgehog (HH) signaling regulates development, cell proliferation, and tissue repair [1], [2], [3]. In mammals, HH signaling is activated by 3 ligands: Sonic hedgehog (SHH), Indian hedgehog (IHH), or Desert hedgehog; SHH is the most widely expressed in adult tissues [3]. The primary re
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A two way chi square test was
2022-08-19

A two-way chi-square test was used to determine statistically significant differences between corresponding frequencies of GT results for the 2 testing periods. A p value of Results Distribution of HCV GT results obtained during the 2 study periods are shown in Table 1. While very low frequencies
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Our data indicate that curcumin
2022-08-19

Our data indicate that curcumin reduced MDA and LOOH formation in plasma and kidney induced by gentamicin treatment. The results demonstrate the protective effect of this compound against oxidative damage to these membranes. Moreover, the ability of curcumin to reduce the formation of LOOH induced b
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Bupivacaine is one of the local anesthetics commonly
2022-08-19

Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root PD 151746 (DRG) neurons [5], [6], [7
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We first set out to identify the minimum pharmacophore
2022-08-19

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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The biological activity at GPR
2022-08-19

The biological activity at GPR109a of each of the 4-functionalized-5-alkyl-pyrazole-3-carboxylic acids (–) was measured using a cAMP whole cell Dynamic2 Homogenous Time-Resolved Fluorescence (HTRF) assay (). Twelve compounds were found to exhibit an EC below 1μM, and of these seven exhibited EC valu
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GlyRs are members of the
2022-08-18

GlyRs are members of the superfamily of Cys-loop receptors (CLRs) [3]. They form postsynaptic pentameric receptor complexes of α1 and β subunits anchored via the scaffolding protein gephyrin [4]. GlyRs are composed of several domains with the large N-terminal extracellular domain (ECD) important for
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Neuregulin/Heregulin-1β (NRG-1β/HRG-1β), human recombinant p
2022-08-18

Results indicated that superfusion of orexin alone, glutamate alone or orexin-glutamate co-administration significantly increases the spontaneous discharge rate of LC neurons in both morphine dependent and non-dependent rats (Fig. 2, Fig. 3). However, co-application of orexin and glutamate resulted
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It is well known that GPCR responsiveness desensitizes
2022-08-18

It is well known that GPCR responsiveness desensitizes after prolonged exposure to agonists through several mechanisms such as receptor phosphorylation, arrestin binding and internalization (Dhami and Ferguson, 2006). Therefore, in the present work we decided to study whether group I-mGluR signaling
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daunorubicin According to the aforementioned preclinical and
2022-08-18

According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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In sharp contrast to these genetically altered animals there
2022-08-18

In sharp contrast to these genetically altered animals, there are two types of living fish that appear to lack Band 3 in their red blood cells. These are the Lamprey [45] and the Hagfish [46,47]. While these fish normally occupy their respective niches, the presumed compensatory mechanisms, as with
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