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Considering the conformational preferences of the
2021-10-01
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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Hardy et al had demonstrated the role
2021-10-01
Hardy et al. had demonstrated the role of GPR40 in mediating the proliferative effect of the FFA oleate's in breast cancer cells, and found that such effect can be reversed by silencing of GPR40 [14]. Similarly we have observed that inhibition of GPR40 function by its antagonist GW1100 inhibited ce
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Trifluoromethyl ketones and fluorophosphates were the first
2021-10-01
Trifluoromethyl ketones and fluorophosphates were the first generation FAAH inhibitors identified. They showed good in vitro FAAH inhibition potency, but most of them exhibited poor selectivity for FAAH over other serine hydrolases (such as the triacylglycerol hydrolase and the membrane-associated h
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Cux is a cell cycle
2021-10-01
Cux1 is a example dependent transcription repressor that is aberrantly expressed in the Pkd1 null, Pkd1CD, and cpk mouse models of PKD, as well as in human ADPKD cells (Vanden Heuvel et al., 1996; Sharma et al., 2005; Paul et al., 2011; Alcalay et al., 2008). In Pkd1 null mice and in human ADPKD ce
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Poziotinib br Activation of soluble guanylate
2021-10-01
Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple
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PDEs block GUCY C associated
2021-10-01
PDEs block GUCY2C-associated second messenger signaling by degrading cyclic nucleotides, whereas inhibition of PDEs activity prevents cyclic nucleotide degradation (Fig. 1). Several researchers have described the pathophysiological roles of various PDEs in numerous tumor cell types, including CRC pl
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Considering that loss of LAG expression
2021-10-01
Considering that loss of LAG-3 e3 ligases results in increased CD4+ T cell homeostatic expansion, and that the ability of a cell to proliferate is tightly coupled to its metabolic profile, we hypothesized that LAG-3 regulates naive CD4+ T cell metabolism. Our results indicate that, indeed, Lag3-def
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br Competing interests br Introduction An effective
2021-10-01
Competing interests Introduction An effective vaccine against the Human immunodeficiency virus (HIV) is still to be created, even though many strategies have already been tried [1]. Antibodies against a vaccine antigen must be either neutralizing or inducing cellular cytotoxicity [1]. It is kn
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Ion dependence of mGluRs activity has been previously
2021-10-01
Ion dependence of mGluRs activity has been previously reported, notably to Ca2+ and Cl− (Kuang and Hampson, 2006). While mGlu1 and mGlu3 receptors were demonstrated to be sensitive to Ca2+, Cl− modulation was reported for all mGluRs, with a lesser extent for the mGlu2 receptor (DiRaddo et al., 2014;
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In an immunohistochemical analysis of gastric cancer samples
2021-10-01
In an immunohistochemical analysis of 117 gastric cancer samples, reduced Cx43 and E-cadherin expression were shown to contribute to the development of primary gastric cancer; however, increased Cx43 and E-cadherin expression contributed to lymph node metastasis [13]. In primary urothelial GSK 0660
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N1-Methylpseudo-UTP In a recent study Neelaveni
2021-09-30
In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported
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bmn 673 Several studies have indicated that PLD
2021-09-30
Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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rad51 inhibitor Introduction As a compound class
2021-09-30
Introduction As a compound class, histone deacetylase inhibitors (HDIs) have been remarkably successful in the treatment of T-cell lymphoma [1]. Vorinostat (suberanilohydroxamic rad51 inhibitor or SAHA) was approved by the FDA in 2006 for the treatment of cutaneous T-cell lymphoma [2], [3]; romidep
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In addition to SAHA SBHA also showed a strong
2021-09-30
In addition to SAHA, SBHA also showed a strong rescue effect. SAHA is a general inhibitor of HDAC function (Finnin et al., 1999, Kim and Bae, 2011), while SBHA is more specific, and has been shown to inhibit HDAC1 and HDAC3 (Richon et al., 1998). The relative level of suppression was similar in Kis
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The identity of organelles is
2021-09-30
The identity of organelles is defined by a particular set of molecules present on their surface. Most organelles in the endomembrane system (i.e., endoplasmic reticulum, Golgi apparatus, endosomes, and lysosomes) carry Rab GTPases (hereafter referred to as Rabs), which serve as binding platforms for
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