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The isoenzyme hGSTP is an attractive drug
2021-12-30
The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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One important aspect about GSK inhibitors is
2021-12-30
One important aspect about GSK-3 inhibitors is their effect on pluripotency of leuprolide acetate [4]. Many GSK-3 inhibitors are ATP-competitive and suppress both GSK-3alpha and GSK-3beta [476]. BIO was shown to suppress GSK-3 activity and promote Wnt/beta-catenin signaling. This combination of eve
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Human GPR hGPR was originally isolated in as an
2021-12-30
Human GPR55 (hGPR55) was originally isolated in 1999 as an orphan GPCR with high levels of expression in human striatum (Sawzdargo et al., 1999) (Genbank accession # NM_005683.3). hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen,
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Solasodine receptor Based on the precedent with other GlyT i
2021-12-30
Based on the precedent with other GlyT1 inhibitors such as , we evaluated both and for their ability to enhance prepulse inhibition (PPI) of the rodent acoustic startle response, a measure of sensorimotor gating known to be deficient in schizophrenic patients., In this Solasodine receptor study (),
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Glutamate aspartate transporters or excitatory
2021-12-30
Glutamate-aspartate transporters or excitatory amino BTL105 mg transporters (EAATs) are essential for the maintenance of glutamate homeostasis. EAATs are widely distributed in central neurons and glial cells (Danbolt, 2001, Martinez-Lozada et al., 2011). They are driven by Na + and K+ gradients (Ji
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Caffeine decreased EAAT and EAAT expression levels in P
2021-12-30
Caffeine decreased EAAT1 and EAAT2 ibuprofen msds sale levels in P2 fraction, as well as [3H]d-aspartate uptake; however, as soon as caffeine is removed from incubation, [3H]-d-Aspartate uptake is recovered to control levels, eliminating the possibility of caffeine as a cell death inducer. In resu
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In conclusion we provided the
2021-12-30
In conclusion, we provided the first evidence of a modification and regulation of GCK by O-GlcNAc modification that until now was not explored. This discovery provides important clues in the prevention of hyperglycemia and development of novel therapeutic drugs to treat type 2 diabetes. Acknowled
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Analysis of genomic neighborhoods has helped resolve questio
2021-12-30
Analysis of genomic neighborhoods has helped resolve questions concerning the orthology of receptors for peptides similar to glucagon (Ng et al., 2010, Irwin and Prentice, 2011, Wang et al., 2012, Hwang et al., 2013). Using a diverse array of species with available genome sequence (see Fig. 4) the g
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Diclazuril Interestingly transgenic mice that constitutively
2021-12-29
Interestingly, transgenic mice that constitutively express active FXR in the intestine (iVP16FXR) are protected from chemically-induced and genetically-induced cholestasis. This protective effect is attributed to the induction of intestinal FGF15 and repression of hepatic Cyp7a1 expression, downregu
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br Significance Metabolites present in the extracellular env
2021-12-29
Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS). I
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Several bacterial functional pathways were observed
2021-12-29
Several bacterial functional pathways were observed after DON administration, of which signal transduction, metabolism and genetic information processing displayed the highest levels of enrichment. Importantly, these three pathways were reported to be closely associated with DON's toxicity. Many evi
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br Conclusion and future perspectives In
2021-12-29
Conclusion and future perspectives In the setting of myocardial I/R stress, HDAC activity is induced and contributes to myocardial injury. HDAC inhibition appears to protect the PF-8380 from I/R injury by activating a variety of pro-survival molecular pathways. From a clinical relevance standpoi
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Of xenobiotic quinones thymoquinone methyl isopropyl benzoqu
2021-12-29
Of xenobiotic quinones, thymoquinone (2-methyl-5-isopropyl-1,4-benzoquinone; Fig. 1) is one of the most thoroughly studied for its pharmacological properties. It is the most active component of Nigella sativa, commonly called black cumin2, 3, the essential oil of the seeds of which are used for trea
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glucocorticoid receptor antagonist Starting from commerciall
2021-12-29
Starting from commercially available 1,4-dioxaspiro[4.5]decan-8-ol, was prepared by the synthetic sequence illustrated in . Aromatic nucleophilic substitution of 1,4-dioxaspiro[4.5]decan-8-ol, followed by an glucocorticoid receptor antagonist catalyzed deprotection efficiently gave . A - enriched mi
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HQNO sale br Material and methods br
2021-12-29
Material and methods Results Discussion The inhibitory action of a GABA agonist, muscimol, on the level of mRNA encoding GnRH in the POA-hypothalamus [25] of follicular-phase sheep has suggested that at the hypothalamic level GABA may exert a suppressive effect on subsequent steps of the Gn
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