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AdipoRon is an orally active synthetic
2022-11-01

AdipoRon is an orally active, synthetic small molecule that activates adiponectin receptor (AdipoR). It mimics the antidiabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively (Fig. 2) [62]. AdipoR activation has r
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Several reports of single cases of MG patients treated with
2022-11-01

Several reports of single cases of MG patients treated with Rituximab have claimed a favourable response (Baek et al., 2007, Gajra et al., 2004, Hain et al., 2006, Thakre et al., 2007, Wylam et al., 2003, Zaja et al., 2000). We report our experience with Rituximab in 6 patients with severe MG, 3 pa
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Jesus et al discovered a new series of
2022-11-01

Jesus et al. discovered a new series of azaindole as Aurora inhibitors through various modification of GSK1070916 (47). They synthesized series from modification of the GSK1070916 and evaluated for in-vitro Aurora-B/INCENP and Aurora-A/TPX2 inhibition assays. Modified Nutlin 3 48 and 49 showed IC50
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Receptor Subtypes and Their Function Critical Appraisal Larg
2022-11-01

Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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In the pituitary of R quelen mRNA
2022-11-01

In the pituitary of R. quelen mRNA levels of cyp19a1b were found to be higher in males than females, suggesting a sex-specific function, and perhaps a local action to regulate gonadotropins or other pituitary hormone secretion (Olivereau and Callard, 1985; Zhang et al., 2014). Interestingly, the hig
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br Concluding remarks It is
2022-11-01

Concluding remarks It is clear that a disordered l-arginine homeostasis by changes in arginase, NOS and ADMA activity and expression, is not only vital in the chronic airway diseases, rotenone and COPD, but also seems to play an important role in many co-morbidities. Unknown, however, is whether
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In addition unconventional mechanisms of internalization can
2022-10-31

In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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An unbiased evaluation of hepatic mRNA was
2022-10-31

An unbiased evaluation of hepatic mRNA was performed to assess the impact of hepatocyte AMPK activation on the transcriptome. The expression of 913 genes were altered in control mice after chronic PF-06409577 treatment, 188 genes were affected by knocking out AMPK in hepatocytes, and expression of 2
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Most intriguingly however there was
2022-10-31

Most intriguingly, however, there was no change in basal glutamatergic neurotransmission despite a loss of about half of the neuronal AMPAR population. Highest levels of ammonia did neither affect the amplitude nor the frequency of AMPAR mediated mEPSCs. As revealed by our recordings from somatic ou
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br A and tau in
2022-10-31

Aβ and tau in Alzheimer's disease The two classical histopathological hallmarks of AD are extracellular insoluble Aβ deposits, known as Aβ plaques, and intracellular accumulations of insoluble microtubule-associated tau protein, known as neurofibrillary tangles [14]. Aβ peptides are produced as a
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a-MSH, amide Although several ARIs have reached various
2022-10-31

Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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The aldehyde reductase AKR A and aldose
2022-10-31

The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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In this study high concentrations mM of
2022-10-31

In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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While A Rs communicate mainly with the
2022-10-31

While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this Epiandrosterone area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neurons [69]. Thi
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The biological characteristics of cancer invasion and metast
2022-10-31

The biological characteristics of cancer invasion and metastasis are mainly attributed to the poor prognosis in cancer. It has been reported that overexpression of Ack1 promoted the migratory and invasive properties of breast cancer androgen receptor inhibitor by sustaining expression of epidermal
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