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Recently a G protein coupled receptor GPR
2022-04-14
Recently, a G-protein-coupled receptor, GPR109a, was identified as a molecular target for niacin. Following this breakthrough, our group initiated a drug discovery program focused on the development of a high affinity ‘flush-free’ niacin-like agonist. Previously, we reported on the identification of
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Several studies have shown that regulation of glutamate
2022-04-14
Several studies have shown that regulation of glutamate homeostasis is critical in relapse to many drugs of abuse [84,85]. Glutamate is transported by GLT-1, which accounted for about 90% of glutamate clearance from the synaptic cleft [14,15]. CEF is known to produce its effects through GLT-1 upreg
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br Introduction Most organisms require glucose as
2022-04-14
Introduction Most organisms require glucose as a key metabolite, and it is critical that mammalian cells regulate glucose levels properly to maintain bioenergetic homeostasis. The major transporters responsible for the uptake of glucose from systemic circulation into cells are the GLUTs, members
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Extending time action is another strategy
2022-04-14
Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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Exposure of human and animals
2022-04-14
Exposure of human and animals to MPTP can reproduce all the characteristic motor and non-motor signs of PD, in addition to mimicking the same responses and side effects to drugs used to treat PD [37], [38]. Anatomically, intoxication with MPTP induces the same selective loss of substantia nigra DA n
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Ghrelin is mostly known for
2022-04-14
Ghrelin is mostly known for its orexigenic properties, whereas the role of DAG on feeding is controversial with studies claiming an orexigenic, anorexigenic or no effect (Inhoff et al, 2009, Toshinai et al, 2006). One of these studies was that of Toshinai and colleagues, who found a link between the
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br Introduction Connexins are transmembrane proteins that al
2022-04-14
Introduction Connexins are transmembrane proteins that allow the exchange of molecules with the extracellular environment or adjacent pevonedistat via channels in the plasma membrane. Intercellular communication and exchange of biologically active molecules, salts, and nutrients to the extracell
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br Introduction Stroke is the second cause
2022-04-13
Introduction Stroke is the second cause of death worldwide and the first cause of acquired motor disability in adults [1], [2]. In sub-Saharan Africa, stroke is the first cause of admission in neurology departments [3]. In Cameroon, the in-hospital mortality of stroke is estimated at 26.8% [4]. A
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NVP-LCQ195 Acetylation of histones by histone acetyltransfer
2022-04-13
Acetylation of histones by histone acetyltransferases stimulates gene expression by relaxing NVP-LCQ195 structure, allowing access of transcription factors to DNA, whereas deacetylation of histones by histone deacetylases promotes chromatin condensation and transcriptional repression. Recent studies
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Neuromedin B Studies of early cell fate specification
2022-04-13
Studies of early cell fate specification in the mouse embryo have identified a role for differential Motin localization in controlling Hippo signaling [88]. At the 32-cell stage, mouse blastomeres are subdivided into inner cells, which form the inner cell mass (ICM), and outer cells, which form the
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cudc 907 One of the possibilities of HO
2022-04-13
One of the possibilities of HO-1 targeting is gene therapy. So far, the majority of preclinical studies have focused on recombinant adeno-associated viral (rAAV) vectors as DNA carriers. They not only provide stable, long-term transgene expression in non-dividing cudc 907 but also have very limited
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To solve the atomic structures
2022-04-13
To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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Migratory properties of Treg are extremely important for
2022-04-12
Migratory properties of Treg are extremely important for the potential in vivo application. Therefore, the observed expression of CXCR3 on almost all obtained insulin-specific Treg is crucial for directing Ciclopirox ethanolamine into the inflamed tissue (in this case pancreatic islets). CXCR3 resp
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One difficulty in studying gp is that
2022-04-12
One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how checkpoint pathway respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinociception, AM
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br Membrane transporters as a novel therapeutic target
2022-04-12
Membrane transporters as a novel therapeutic target in pediatric TBI The concept of targeting membrane transporters began with identifying a neuroprotective drug and a corresponding transporter inhibitor. Somewhat serendipitously, we discovered that N-acetylcysteine (NAC), a cysteine donor for GS
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