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br Introduction The signaling molecule nitric oxide NO
2022-06-10

Introduction The signaling molecule nitric oxide (NO) plays an essential role in vessel homeostasis by initiating vasodilation [1], [2], [3]. After biosynthesis in endothelial cells, NO diffuses into the subjacent smooth muscle layer to reach its target enzyme, soluble guanylyl cyclase (sGC, EC 4
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Protein structures determined in high
2022-06-10

Protein structures determined in high resolution by X-ray crystallography and NMR techniques provide wealth of structural information on intra-domain and inter-domain protein interactions of small sized proteins. In addition, cryo-EM often provides low resolution structures of multi-component protei
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Mice with GSTP knock out show increased risk of
2022-06-10

Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino Sodium Aescinate residue
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Chronic exposure of cells to cytotoxic
2022-06-10

Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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Here we demonstrate an anti inflammatory and anticancer func
2022-06-09

Here we demonstrate an anti-inflammatory and anticancer function for Gpr109a in colon. Gpr109a signaling imposed anti-inflammatory properties in colonic antigen-presenting cells, which in turn induced differentiation of Treg hydrazone and IL-10-producing T cells. Gpr109a was also required for the e
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Molecular properties as well as metabolic
2022-06-09

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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EAATs can transport glutamate aspartate cysteic
2022-06-09

EAATs can transport glutamate, aspartate, cysteic acid, and serine-o-sulfate (Bjorn-Yoshimoto and Underhill, 2016). All EAATs work as symporters co-transporting 2 or 3 molecules of Na+ and a proton with each molecule of glutamate (or aspartate). In addition, a K+ ion is counter-transported ending in
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The EEGs of these six patients
2022-06-09

The EEGs of these six patients interestingly showed focal, multi-focal and generalized spikes, which was an exclusion criteria in our study as we selected our cohort to exclusively represent focal epilepsy. Remarkably all of these cases were diagnosed with paroxysmal exercise-induced dyskinesia (PED
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Extensive pharmacological and structural analysis shows
2022-06-09

Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in Fosmidomycin sodium salt 14, 17, 20. Functionally identical to REMD-
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PP121 australia Cartilage and subchondral bone synovial tiss
2022-06-09

Cartilage and subchondral bone/synovial tissue interactions are well-recognized features of joint failure and osteoarthritis[17](seeFig. 1A, B). The intimate mechanical and biological interactions between these tissues are likely to alter the structural organization and function of either tissue. Ho
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Notwithstanding the functioning of galaninergic system
2022-06-09

Notwithstanding, the functioning of galaninergic system may be even more complex (Fuxe et al., 2012). Some studies present evidence that GAL2 receptors might form heteroreceptor complexes with neuropeptide Y1 receptors in Zalcitabine of amygdala (Narváez et al., 2015a), DRN (Díaz-Cabiale et al., 201
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There are additional implications of subunit alterations
2022-06-09

There are additional implications of α2-subunit alterations in the hippocampus. P has anticonvulsant activity (Herzog, 1995, Herzog et al., 1997, Herzog et al., 2012, Reddy et al., 2001, Reddy, 2010). These actions result from the metabolic conversion of P to GABA-A receptor-modulating, antiseizure
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br Novel mechanisms of fipronil resistance in
2022-06-09

Novel mechanisms of fipronil resistance in planthoppers Conclusion Conflict of interest Introduction Methamphetamine, a widely abused drug, is mainly used as a psychostimulant although it is occasionally used at low doses for medical purposes, such as in attention deficit or hyperactivit
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Knock out mice of FXR showed enhancing cholesterol
2022-06-09

Knock-out mice of FXR showed enhancing cholesterol metabolism in vivo and reducing serum levels of total cholesterol. Additionally, the results of FXR-deficiency mice revealed potential effects on the improvement of obesity and diabetes.19, 20 As a natural FXR ligand, guggulsterone possesses antagon
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One effective approach to fine tuning the
2022-06-09

One effective approach to fine-tuning the lipophilicity profile of FFA1 agonists is to ‘decorate’ the 3-phenylpropahoic Tanespimycin scaffold with polar heterocyclic moieties. Alternatively, this scaffold could be replaced with heterocyclic isosteres (as in Takeda’s compounds 1,2 and 3 as well as A
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