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Lorlatinib is an orally active brain penetrant cyclic aminop
2024-05-25
Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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To examine whether the interaction between
2024-05-25
To examine whether the interaction between mGlu7 and α1-adrenergic receptors could be confirmed at a behavioural level, we performed the FST in mice. This test has value in predicting the antidepressant-like effect of drugs or environmental manipulations (Krishnan and Nestler, 2008, Krishnan and Nes
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Constitutive tyrosine kinase activity of BCR
2024-05-25
Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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Extracellular ATP and downstream purinergic signaling have a
2024-05-24
Extracellular ATP and downstream purinergic signaling have also been proposed to contribute to dental pulp tissue healing and dentin regeneration. Mechanical and thermal stimulation of external dentin can induce ATP release in dental pulp through pannexins [13]. Cold stimulation was also reported to
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AdipoRon is an orally active synthetic small molecule that a
2024-05-24
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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There is also a literature on the impact of commodity
2024-05-24
There is also a literature on the impact of commodity (consumption) taxation under imperfect competition. Besley (1989) applies a Cournot model, in which production takes place under IRS and in which free entry leads to an excessive number of firms in the market. Introducing a distortive specific co
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br Acknowledgments br Introduction Hypospadias is a common c
2024-05-24
Acknowledgments Introduction Hypospadias is a common congenital malformation in males, in which the urethral orifice is found on the ventral side of the penis as a result of incomplete fusion of urethral folds. The mean prevalence in per 10,000 live births from 1910 to 2013 were: Europe 19.9,
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Thus one possible target for
2024-05-24
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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br Results and discussion br Conclusion In summary a series
2024-05-24
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic T7 High Yield RNA Synthesis group extending from the C-3 position of the aniline and
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Fig summarizes the oxidative metabolism of arachidonic acid
2024-05-24
Fig. 1 summarizes the oxidative metabolism of arachidonic cyclin dependent kinase by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eo
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br Conclusion This is the first report to show that
2024-05-24
Conclusion This is the first report to show that treatment of lung cancer cell lines, A549 and H1299, with ovatodiolid stimulates intracellular reactive oxygen species generation and induces DNA damage. Subsequently activates ATM/ATR and CHK1/2 signaling pathway, inhibits CDC25C and p21WAF1/CIP1,
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These recommendations may be useful for the
2024-05-24
These recommendations may be useful for the future to avoid misleading reports and pairings. However, the existing literature can also hold back current research on some given orphans. Before entering into drug development or further physiological conceptual framework, these pairings should be thoro
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Antioxidative enzymes such as SOD and CAT play prominent
2024-05-24
Antioxidative enzymes such as SOD and CAT play prominent roles in protecting against oxidative stress and extending food freshness due to their ability in scavenging active oxygen species for maintaining cell membrane integrity. Evidence shows that activities of SOD and CAT are positively affected b
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In a missense mutation at codon of the PRNP gene
2024-05-24
In 1989, a missense mutation at codon 102 of the PRNP gene was first reported to be associated with GSS and, in 1991, the same mutation was also found in affected members of the “H” family (Hsiao et al., 1989; Kretzschmar et al., 1991). By 1995, the pedigree of the “H” family included 221 family mem
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Androgen receptor translocates from the cytoplasm to the nuc
2024-05-24
Androgen receptor translocates from the cytoplasm to the nucleus after binding to its ligands (Quigley et al., 1995). In the current study, although propofol did not significantly affect total androgen receptor protein levels, it significantly decreased nuclear androgen receptor levels. These findin
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