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In addition to the above mentioned synaptic mechanisms the
2024-10-08
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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br Effective therapeutic window of AR actions on ROP
2024-10-08
Effective therapeutic window of AR actions on ROP Retinal vasculature undergoes critical developmental changes postnatally: from P7 onward the superficial ion channel start sprouting vertically in retina to form first the deep then the intermediated vascular plexus in the retina of C57BL/6 mice
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br Results and discussion The morphology and
2024-10-08
Results and discussion The morphology and structure of Biotin-azide samples were observed using an SEM, as shown in Fig. 1. The length and thickness of the actin filaments were regulated with ABPs to mimic the various actins observed in cells. We prepared three types of F-actin with or without g
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M344 mg Owing to efficient catalytic character high electrol
2024-10-08
Owing to efficient catalytic character, high electrolyte accessible area, easy fabrication and many other interesting properties, metal oxide nanoparticles are extensively used in a variety of electro-analytical processes [14]. Metal oxide nanoparticles immobilized over a conductive and large area s
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The following are the supplementary data related
2024-10-08
The following are the supplementary data related to this article. Funding Work in Dr. Rosell's laboratory is partially supported by a grant from La Caixa Foundation, and an Instituto de Salud Carlos III grant (RESPONSE, PIE16/00011). Work in Dr. Cao's laboratory is partially supported by the Maj
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In this paper we describe
2024-10-08
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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Elevated expression of Aurora A
2024-10-08
Elevated expression of Aurora-A and -B frequently detected in a wide variety of human cancers strongly indicate that high expression of these kinases play roles in the development of cancer associated phenotypes. While Aurora-A has been shown to function as an oncogene when over expressed in mammali
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To test the compounds metabolic stability we measured the
2024-10-08
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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br Funding This study was supported by
2024-10-08
Funding This study was supported by Grant UM1-CA186690 (NCI-CTEP) and R01CA204173 (CJB). This project used the UPCI Cancer Pharmacokinetics and Pharmacodynamics Facility (CPPF) and was supported in part by award P30-CA47904 and R50CA211241. Introduction Despite the efficacy of platinum based
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In this review we will present the traditional and
2024-10-08
In this review, we will present the traditional and actual strategies to study orphan receptors and identify their ligands. An extensive description of the orphan GPCR field has been published in 2013 by Davenport et al. [22]. Therefore, we will focus on the deorphanizations that were reported since
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Furthermore a study in Drosophila has
2024-10-08
Furthermore, a study in Drosophila has reported that Dpatj can interact directly with Dmpar6 providing another potential mechanism linking the Crb to the Par complex [163]. In contrast, Wang et al. in 2004 [63] have shown that at least in MDCK epithelial cells, PAR6 binding to PALS1 interferes with
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br HIF Signaling in AA Therapy Resistance
2024-10-08
HIF-α Signaling in AA Therapy Resistance An important result emerging from Phase 3 clinical trials testing AA therapies is improvement of progression-free survival (PFS) that is not accompanied by enhanced overall survival (OS) [26]. This dichotomy has been attributed to mechanisms of acquired re
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AdipoR and AdipoR have been reported
2024-10-03
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low caspase 3 levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of APN expre
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Molecular docking simulations were carried out for
2024-10-03
Molecular docking simulations were carried out for ligands – in the ACE crystal structure (1O86) and DPP4 crystal structure (2G5P). Comparison of the binding mode of – () with enalaprilat (a) in ACE shows that the phenethyl group (–, enalaprilat) occupies the S1 pocket and the adjacent carboxylic eg
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br Regulation of V ATPase assembly in response
2024-10-01
Regulation of V-ATPase assembly in response to changes in amino neuraminidase inhibitors levels A central regulator of cell growth and metabolism is mTORC1 [38]. mTORC1 integrates signals from nutrient availability and growth factor receptors to control such processes as protein and lipid synthe
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