• Gratifyingly compound also demonstrated improved

  2024-10-15

  

  Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and

• The cytoplasmic domain of muscle AChR is

  2024-10-15

  

  The cytoplasmic domain of muscle AChR is not accessible to 3280 synthesis in vivo. Theoretically, therapy with the cytoplasmic domains should be safe. Safety is demonstrated by the facts that: (1) rats repeatedly immunized with the cytoplasmic domains in TiterMax adjuvant do not develop EAMG, altho

• Rapalink-1 LO is a soluble kDa enzyme composed of

  2024-10-15

  

  5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell

• Loss of virulence in ACL mutants may

  2024-10-14

  

  Loss of virulence in ACL mutants may be caused by defect in vegetative growth and conidial germination, and reduced trichothecene production. However, supplement of potassium acetate restored the defects in germination rate and vegetative growth, but not virulence in wheat heads (Table 2, Fig. 2B),

• Of the many different types of

  2024-10-14

  

  Of the many different types of DNA lesions, DNA double strand breaks (DSBs) are amongst the most deleterious. It has been suggested that a single unrepaired DSB may be sufficient to induce cell death (Bennett et al., 1993), whereas misrepaired DSBs can result in loss of genetic information, potentia

• Having demonstrated that Gq coupled mGluR a was necessary

  2024-10-14

  

  Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in

• br Activity and expression of aromatase in the hippocampus

  2024-10-14

  

  Activity and expression of aromatase in the hippocampus The brain, like the adrenals, gonads and the placenta, is a steroidogenic organ. This paradigm emerged from studies carried out as early as the 1980s by Baulieu and co-workers; these studies showed that steroids such as pregnenolone and dehy

• br Author contribution br Acknowledgement br Introduction Si

  2024-10-14

  

  Author contribution Acknowledgement Introduction Since the initial finding of Gould et al. [1], showing the loss of dendritic spines in the hippocampus after ovariectomy and its rescue after treatment of the animals with estradiol, a tremendous number of studies have demonstrated a role of

• Apelin is involved in various physiological functions includ

  2024-10-14

  

  Apelin is involved in various physiological functions, including mdm2 p53 contraction (Ashley et al., 2005), vasodilatation (Jia et al., 2007), feeding control (Valle et al., 2008), and metabolic homeostasis (Higuchi et al., 2007, Dray et al., 2008, Attane et al., 2010). Its plasma level is elevate

• The reasons why antibiotic treatment

  2024-10-14

  

  The reasons why antibiotic treatment may be detrimental are diverse. First, it may result in disruption of multifaceted microbe–microbe, as well as microbe–host, interactions that are key for the maintenance of homeostasis within this ecosystem. This can lead to the expansion of pathogenic microorga

• Under some pathological conditions AT

  2024-10-14

  

  Under some pathological conditions, AT1R internalization is decreased when agonist exposure is prolonged. This weakens or removes the AT1R desensitization effect and leads to AT1R and downstream signal overactivation. AT1R overactivation can result in continued biological effects such as sustained v

• With wide spread use of corticosteroids to combat

  2024-10-14

  

  With wide-spread use of corticosteroids to combat inflammation and allergies, even children are susceptible to corticosteroid-induced muscle wasting. Although non-steroidal SGRMs that spare muscle and bone, but have significant anti-inflammatory effects, have been preclinically developed and tested,

• In mice the Tfm mutation increased the anxiety state assesse

  2024-10-14

  

  In mice, the Tfm mutation increased the anxiety-state assessed in the novel object and in light/dark box tests, whereas no changes were detected in the open field or elevated plus maze tasks (Zuloaga et al., 2008). As for Tfm rats, this seemed to be related to an increased HPA response to stress. Th

• Introduction Induction of long term potentiation LTP the

  2024-10-14

  

  Introduction Induction of long-term potentiation (LTP), the cellular correlate of learning and memory, triggers profound changes in the structure and function of excitatory synapses by increasing dendritic spine size and synaptic strength. Significant progress has been made in understanding the int

• The RAS may have different functions depending on

  2024-10-14

  

  The RAS may have different functions depending on whether we consider the circulatory component or the different local tissue systems (including brain) well described previously [29]. The cardiovascular control and hydroelectrolytic balance (among other functions), are largely the result of the infl

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