• Discrepancies in the reported results and conclusions

  2021-10-08

  

  Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately

• When tested in dog at mg kg showed

  2021-10-08

  

  When tested in dog at 20mg/kg, showed a reduction of 56% of Aβ42 in the cerebrospinal fluid (CSF) 8h post doing, comparable to that of (see ). Upon evaluation of BH3I-1 receptor in a one week repeated dose study in dog, at 10 and 20mg/kg/day, no increase in liver enzyme levels (ALT or AST) was o

• The focused set of additional pyrazole

  2021-10-08

  

  The focused set of additional pyrazole analogs allowed the identification of three additional moderately potent γ-secretase modulators, , and which were subsequently screened in a kinetic solubility assay. Unfortunately, neither the architectural changes in analog nor the integration of trifluoro

• Somatostatin analogues are among the first peptide based dru

  2021-10-08

  

  Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B

• To meet the requirement of ferroptosis based therapy a coupl

  2021-10-08

  

  To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous

• The presence of FBP in nuclei seems to accompany the

  2021-10-08

  

  The presence of FBP2 in nuclei seems to accompany the cells' potential to divide as it has been shown that during differentiation of the satellite cells (myogenic progenitor cells) the amount of nuclear FBP2 decreases and in differentiated myotubes, the localisation of FBP2 is restricted to cytoplas

• Importantly each conformational state in the

  2021-10-08

  

  Importantly, each conformational state in the SRP–SR dimer provides a distinct point of regulation at which these GTPases can directly sense and respond to different biological cues in the pathway. For example, assembly of a stable ‘closed’ complex between SRP and SR is intrinsically very slow (kon

• As previously discussed even though

  2021-10-08

  

  As previously discussed, even though glucose is the major fuel of the brain, neuronal cells may use alternative fuels such as ketone bodies in metabolically challenging situations in which glucose availability is limited [6]. Ketogenesis takes place mainly in the liver, although astrocytes can also

• br Acknowledgement The author expresses

  2021-10-08

  

  Acknowledgement The author expresses her sincere appreciation to Brian P. Kenealy, Ph.D. for his contributions to the series of studies described in this article that were conducted during his tenure in the lab, as a graduate student first and then a postdoctoral research fellow. She also thanks

• Over expression of Glo can suppress inflammatory responses M

  2021-10-08

  

  Over-expression of Glo-1 can suppress inflammatory responses. Methylglyoxal mediates vascular inflammation in human endothelial NB-598 Maleate [33], indicating that Glo-1 may attenuate inflammation via eliminating methylglyoxal. Glo-1 knockdown mediated methylglyoxal accumulation provokes collagen e

• Na K ATPase adenosine triphosphate ATP and astrocytic glutam

  2021-10-08

  

  Na+/K+-ATPase, ck1 inhibitor and astrocytic glutamate transporters act together to maintain sodium and potassium gradients and the proper activities of EAAT1 and EAAT2 (Rose et al., 2009; Sheean et al., 2013); nevertheless, in present study, Na+/K+-ATPase activity was shown to be increased as from

• br Materials and methods br Results

  2021-10-08

  

  Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini

• The observed CORT induced increase in Cx phosphorylation at

  2021-10-08

  

  The observed CORT-induced increase in Cx43 phosphorylation at S368 may also contribute to GJIC disruption. Gap junction channel permeability is modulated through connexin phosphorylation (Moreno and Lau, 2007). Specifically, the phosphorylation of Cx43 on S368 has been previously shown to decrease i

• Herein we describe the development of second generation GSM

  2021-10-08

  

  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

• Hydantoin in region F bridging the phenoxybenzene and benzim

  2021-10-07

  

  Hydantoin in region F bridging the phenoxybenzene and benzimidazole moieties was replaced by cyclic building blocks, diketopiperazine (25) and imidazolidinone (26), and linear bonds, amide (27) and urea (28). Analogs 25–28 possessing the linkers other than hydantoin were not tolerated in LBD of FXR,

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