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A majority of investigations of the GCK PFK FBPase interacti
2022-08-12

A majority of investigations of the GCK-PFK-2/FBPase-2 interaction have taken place within cells. Immunofluorescence studies in several fixed cell lines indicate that GCK colocalizes with PFK-2/FBPase-2 in the cytoplasm following overexpression [[68], [69], [70]]. Live cell imaging conducted on YO-0
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Analysis of the GHSR screening data for inactive library
2022-08-12

Analysis of the GHSR screening data for inactive library members indicated that the prolinol-derived secondary amine and α-substituted phenoxyacetamide moieties described in were critical for activity. As a result, we initiated the synthesis of follow-up libraries utilizing the solid-phase chemistr
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br Voltage dependent anion channel VDAC is a
2022-08-12

Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially
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Herein we describe the development of
2022-08-12

Herein, we describe the development of second generation GSM compounds aimed at improving critical physicochemical properties while maintaining the potent activity of the parent AGSM. Ligand design focused on identifying heterocyclic replacements for the hydrophobic D-ring as a means to improve ADME
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The physicochemical properties of the prodrugs
2022-08-11

The physicochemical properties of the prodrugs provided important clues for understanding a broad range of inhibitory activities in the cell assays (Table 2). Some physicochemical properties are useful in predicting drug absorption. Considering Lipinski’s rules and the polar surface area (PSA),l-ala
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Previously we have isolated liver FBPase from Pelophylax esc
2022-08-11

Previously we have isolated liver FBPase from Pelophylax esculentus (former Rana esculenta, Frost et al., 2006) and characterized its kinetic properties (Dziewulska-Szwajkowska and Dzugaj, 1999) on the contrary the muscle FBPase has never been fully characterized. The primary aim of the present pape
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The PI K AKT pathway
2022-08-11

The PI3K/AKT pathway is known to affect cell cycle, survival, and apoptosis (Yu et al., 2006; Park et al., 2008). After phosphorylation by AKT, the cytoplasmic apoptotic protein bad (bcl-xl/bcl-2) cannot be transferred to the mitochondria and dissociates from the inhibition protein bcl-2 and bcl-xl,
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PKC potentiates insulin release in beta cells however it is
2022-08-11

PKC potentiates insulin release in beta cells; however, it is currently not clear how this is mechanistically accomplished in living 624 [15]. First, we discuss PKC structure, regulation, and activation in beta cells. Then, we address two fundamental questions: (1) what is the specific effect of PK
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br Materials and methods br Results br Discussion mmLDL is
2022-08-11

Materials and methods Results Discussion mmLDL is an important risk factor for cardiovascular disease, but its mechanism is still unclear. Previously, we co-cultured mmLDL with the coronary artery and basilar artery and found that mmLDL could upregulate ETB receptor expression in both [16],
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In mammalian cells Motins have been identified as a
2022-08-11

In mammalian cells, Motins have been identified as a key link between F-actin and Hippo pathway regulation, as knockdown of all three Motins increased Yap activity even in the presence of cytoskeletal disruption [105]. Motins can physically associate with F-actin but this association is blocked by p
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While phosphorylation site motifs are typically described in
2022-08-11

While nigericin site motifs are typically described in terms of residues that promote phosphorylation, negatively selected residues can also be an important component of substrate recognition. Such ‘forbidden’ resides can act as a filter to prevent phosphorylation of a site by the ‘wrong’ kinase, wh
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In diseased blood vessels increased
2022-08-11

In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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Both plant hormones and some second messengers
2022-08-11

Both plant hormones and some second messengers are involved in Fe-deficiency-related responses in plants (Kobayashi and Nishizawa, 2012). Among these second messengers, nitric oxide (NO) accumulation was induced by Fe deficiencies in tomato and Arabidopsis roots, and it acts as the downstream signal
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We have previously established the pharmacokinetic profile a
2022-08-11

We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in Pam3CSK4 Biotin and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The com
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The endocannabinoid system ECS consists
2022-08-11

The endocannabinoid system (ECS) consists of cannabinoid (CB)1 and CB2 receptors, their endogenous ligands anandamide and 2-arachidonylglycerol, and the synthesizing and degrading enzymes for these ligands. Cannabinoids and the ECS are involved in the regulation of GI motility in physiological and p
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