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However although in vitro studies in
2024-06-12
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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L 006235 HT modulates cortical and hippocampal pyramidal cel
2024-06-12
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal L 006235 as well as GABAergic interneurons that exert inhibitory control over pyramidal cells (Leiser et al., 201
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Renal Cell Carcinoma RCC is a lethal cancer with
2024-06-12
Renal Cell Carcinoma (RCC) is a lethal cancer with bad prognosis due to development of chemoresistance and recurrence of an aggressive tumor with increased tumor-angiogenesis and metastasis [7]. We have found Axl and Gas6 to be differentially presented in RCC subtypes, and Axl to correlate to tumor
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br Results br Discussion Although they do not have protein
2024-06-12
Results Discussion Although they do not have protein-coding capacity, lncRNAs make up a large part of the transcripts of the genome, and they play fundamental roles in carcinogenesis and osteosarcoma progression through regulation of tumor proliferation and metastasis. These lncRNAs include M
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The synthesis of compounds in which the
2024-06-12
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic UNC 0646 to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave the
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We demonstrate a role for low oxygen to
2024-06-12
We demonstrate a role for low oxygen to regulate ATX mRNA in hepatocyte-derived HuH7 mglur antagonist and human liver slices, consistent with reports of increased ATX expression in a variety of tumours that are frequently hypoxic. Importantly, we show a positive association between elevated ATX mRN
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Over the past decade extensive research
2024-06-12
Over the past decade, extensive research has been directed toward the discovery of Aurora-selective small-molecule inhibitors. As a result, a handful of Aurora inhibitors has been identified. Among them, 1 (VX-680) and 2 (SNS-314) have entered human clinical trials as pan-Aurora kinase inhibitors (F
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br Results and discussion br Conclusion In
2024-06-12
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic GSK 2830371 australia group extending from the C-3 position of the aniline and subst
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In addition to drawing attention to Ser of
2024-06-12
In addition to drawing attention to Ser454 of ACL as a phosphosite that is regulated by both BDK and PPM1K, our phospho-proteomics screen identified several additional sites in other proteins. For example, Ser25, Ser29, and Ser79 of the lipogenic enzyme acetyl-coA carboxylase 1 (ACC1) were found to
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In clinical studies BA has been reported to promote
2024-06-12
In clinical studies, BA has been reported to promote dose-dependent LDL-C lowering effects of up to 30% as monotherapy, and up to an additional 24% when added in combination with stable statin therapy, or approximately 50% when combined with ezetimibe 109, 110, 111, 112. These effects were accompani
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Plasma apelin levels predict the major
2024-06-12
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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Thus far a tight coupling has been
2024-06-12
Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solub
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Salvia the largest genus in the
2024-06-12
Salvia, the largest genus in the family Lamiaceae, comprises over 900 species that are distributed globally [14], [15], [16]. The genus Salvia has been assessed in many studies because it is a rich source of polyphenol compounds, of which more than 160 have been isolated from plants in the genus, so
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br Discussion AhR is a receptor that
2024-06-11
Discussion AhR is a receptor that binds to a great variety of lipophilic compounds, in particular those containing at least one aromatic ring (Abel and Haarmann-Stemmann, 2010, Guyot et al., 2013, Hahn, 2002). The main known function of this receptor is to induce the metabolism of these compounds
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To confirm a role of OCT in corticosterone
2024-06-11
To confirm a role of OCT3 in corticosterone-induced potentiation of cocaine-primed reinstatement, we examined the interaction of corticosterone and cocaine in the reinstatement of cocaine conditioned place preference (CPP) in wild type mice, and transgenic OCT3-deficient mice. These mice express a t
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