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Matthew et al synthesized and carried out SAR studies of
2024-02-04
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that Vatalanib 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), E
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Once apoptosis has been initiated the HMGA
2024-02-04
Once apoptosis has been initiated the HMGA proteins themselves undergo marked changes in both the types and extent of their post-translational modifications (PTMs; review in [149,175]), some of which are likely correlated with alterations in chromatin structure. For example, the early stages of apop
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To the best of our knowledge only cases of
2024-02-04
To the best of our knowledge, only 3 cases of an E196K mutation have been described since it was first identified in 2000 [15], [16], [17], although 5 cases, accounting for 1.1% of all genetic TSE cases, were reported with no precise data on the clinical phenotypes in the EUROCJD collaborative surve
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br Summary and future br
2024-02-04
Summary and future Introduction Androgen activity is critical for a wide range of developmental and physiological responses and is especially important in male sexual differentiation and maturation. The biological activity of androgens occurs through binding to the androgen receptor (AR) and t
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br Competing interests br Acknowledgments This research was
2024-02-04
Competing interests Acknowledgments This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science and ICT (NRF-2014R1A4A1071040). Introduction Mitochondria occupy an important position as mediators of
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A disfun o cognitiva p
2024-02-04
A disfunção cognitiva pós‐operatória é uma síndrome perioperatória bem reconhecida, consequência da anestesia e cirurgia cuja causa exata permanece por esclarecer. De que forma l arabinose disfunção cognitiva pós‐operatória e a doença de Alzheimer podem estar ligadas permanece uma questão em estudo.
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In fact serotonin is a
2024-02-02
In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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Subsequently Palvimaki et al corroborated Ni and
2024-02-02
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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br Functional consequences of ADK regulation on
2024-02-02
Functional consequences of ADK regulation on neuronal excitability Adenosine modulates neuronal excitability via activation of the high affinity A1 or A2A, low-affinity A2B, or low abundance A3 adenosine receptors that feed into a multitude of different neuronal and astrocytic pathways (Blum et a
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SR1078 Encouraged by this observation a
2024-02-02
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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The cytoplasmic domain of muscle AChR is not
2024-02-02
The cytoplasmic domain of muscle AChR is not accessible to Kenpaullone 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, although
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As we previously observed in the NSFT Fukumoto
2024-02-02
As we previously observed in the NSFT (Fukumoto et al., 2014), the effect of LY341495 in the FST was also inhibited by a 5-HT1A receptor antagonist, indicating the role of the 5-HT1A receptor in the actions of LY341495. Among the 5-HT1A receptors, which exist both presynaptically and postsynapticall
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br Introduction The principal pathways of adrenal and gonada
2024-02-02
Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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br Conclusions br Acknowledgments br Introduction
2024-02-02
Conclusions Acknowledgments Introduction To die or not to die – that is the question. Christian de Duve created the word “autophagy” in 1960’s for the first time (Klionsky et al., 2016). The word “autophagy” was derived from the Greek roots “auto” (self) and “phagy” (eating) and referred to
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From an historical perspective ligands for GPCRs adrenaline
2024-02-02
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Eeyarestatin I synthesis or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenou
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