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Reports of hyperlocomotion after administration of
2021-10-11
Reports of hyperlocomotion after administration of ALX-5407 [27] coupled with the lack of hyperlocomotion after administration of SSR504734, a non-sarcosine, long-residence time, competitive inhibitor [19], suggested that the GlyT1 inhibitor chemotype may impact OP. Furthermore, a compound with a co
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br Discussion Agonist and antagonist action
2021-10-11
Discussion Agonist and antagonist action at the GluN1/GluN3 PF-3758309 is known to be complex [4], [10]. Recombinant GluN1/GluN3 receptors produce only small excitatory currents in response to glycine, likely because of a combination of activation via GluN3 and desensitization via GluN1 [2], [3]
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Regulation of pancreatic and cell mass
2021-10-11
Regulation of pancreatic α and β cell mass has been extensively studied and hotly debated, due to potential therapeutic implications. Early claims of Angptl8 as “betatrophin” and Angptl4 as a regulator of glucagon secretion and α cell proliferation (Yi et al., 2013, Ben-Zvi et al., 2015) have not st
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Naringin has been shown to have significant anti inflammatio
2021-10-11
Naringin has been shown to have significant anti-inflammation, anti-oxidative stress, glucolipid metabolic regulation, and myocardial protection effects (Gopinath et al., 2011, Gopinath and Sudhandiran, 2012), suggesting that it may mitigate ADC by inhibiting P2X7 receptors. In the present study, na
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Moreover intestinal chronic inflammation is a promoting fact
2021-10-09
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 A-1210477 austral
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br Ferroptosis modulators With the recognition that the
2021-10-09
Ferroptosis modulators With the recognition that the small molecule erastin targets system xc- and thereby specifically triggers this form of death and that ferrostatin-1 prevents erastin-induced ferroptosis [2], it has become evident that ferroptosis is a druggable pathway with a number of tract
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Integrin engagement triggers activation of several signaling
2021-10-09
Integrin engagement triggers activation of several signaling pathway including Fak, which is recognized as the key signal transduction factor in the integrin signaling pathway that functions by activating downstream signaling in focal adhesion plaques. Whether changes in integrin-FAK signaling pathw
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A previous study from our
2021-10-09
A previous study from our institution showed moderate correlation between the APTT and Anti-FXa assays, prompting an institution-wide change to an Anti-FXa based monitoring of unfractionated heparin. The current study is a descriptive analysis to evaluate the clinical outcomes in this pediatric coho
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In addition to indoles two additional structural variants we
2021-10-09
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic Meleagrin sale side chain to prepare compound (). The extension of the chain
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1295 This connection is supported by
2021-10-09
This connection is supported by studies in the SIV macaque model of HIV, where treatment with methamphetamine, which greatly enhances CNS dopamine levels (Truong, 2005); increased 1295 viral load. Methamphetamine also increased expression of the HIV co-receptor CCR5 in CNS macrophages, thereby enha
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Hydrochlorothiazide mg In contrast to sGC stimulators sGC ac
2021-10-09
In contrast to sGC stimulators, sGC activators promote enzymatic activity of sGC containing oxidized heme iron (Fe3+) or missing the heme group. A-350619 is one of the oldest activators of sGC to be discovered. A-350619 increased sGC activation in a non-additive manner with respect to YC-1, leading
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As comparators compounds and were made using the
2021-10-09
As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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GPR is present primarily in
2021-10-09
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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FSH and LH are glycoprotein dimers that are comprised of
2021-10-09
FSH and LH, are glycoprotein dimers that are comprised of two subunits, a common α-subunit (αGSU) and a distinct β-subunit (FSHβ or LHβ, respectively), which determines the biological specificity of the gonadotropins (Ciccone and Kaiser, 2009, Gharib et al., 1990). The hiv integrase inhibitor of the
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Although encoded by a single gene GR displays
2021-10-09
Although encoded by a single gene, GR displays considerable heterogeneity through the combined effects of alternative mRNA splicing, alternative translation initiation, and complex post-translational modification. Differential expression of the various GR isoforms may contribute to tissue-specific f
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