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The class C receptors also share a common agonist
2024-05-21

The class C receptors also share a common agonist-binding mode. In all cases, an agonist induces VFT closure by forming intermolecular bonds with surface residues in both the LB1 and LB2 domains (Geng et al., 2013, Geng et al., 2016, Kunishima et al., 2000, Muto et al., 2007, Nuemket et al., 2017, T
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Eeyarestatin I Sixth significant progress has been made duri
2024-05-21

Sixth, significant progress has been made during the last few years regarding the molecular mechanisms underlying the activation of AMPK and this should aid to develop more potent and specific compounds. Information from crystallographic structures combined with computer-based drug design hold promi
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In the previous study we
2024-05-20

In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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Bioactive peptides contain amino acids with possible bioacti
2024-05-20

Bioactive peptides contain 2–20 amino acids with possible bioactivities including antihypertensive, antioxidant, antimicrobial, anticancer, and opioid activity [9], [10], [11]. There has been a great interest in antihypertensive peptides for their efficiency in lowering blood pressure. The antihyper
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br Conclusion This is the first report to
2024-05-20

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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Licarbazepine APJ receptor expression is altered
2024-05-20

APJ receptor expression is altered in various cardiovascular diseases, and both increases as well as decreases in APJ receptor expression have been reported. A decrease in mRNA and protein levels of APJ receptors was observed in patients with ischemic heart disease or idiopathic dilated cardiomyopat
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The contractility index showed positive inotropic effects of
2024-05-20

The contractility index showed positive inotropic effects of apelin in both doses at min 5 (Fig. 3, Fig. 5). Although the mean arterial pressure did not recover to the baseline, the contractility index increased, the relaxation index (tau) and ±dp/dt max returned back to their baseline, and left ven
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br Antibiotic drug discovery approaches Traditionally novel
2024-05-20

Antibiotic drug discovery approaches Traditionally, novel Necrosulfonamide were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries derived
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br AR expression in breast tissue Although androgenic signal
2024-05-20

AR expression in breast tissue Although androgenic signalling is chiefly associated with the development and maintenance of primary and secondary male characteristics, especially during puberty when the testes are by far the major source of testosterone, the AR also plays important functions in f
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br Concluding Remarks and Future Perspectives
2024-05-20

Concluding Remarks and Future Perspectives The collective evidence from studies detailing the functions of AMPK in the neuromuscular system, combined with those in DMD, SMA, and DM1 surveyed in the present review, strongly suggests that AMPK is a central mediator of neuromuscular determination, m
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In light of several reports of defects in memory related
2024-05-20

In light of several reports of defects in memory-related tasks for the dysbindin-deficient mice (Cox et al., 2009, Takao et al., 2008), it was rather unexpected that an enhancement of CA3–CA1 LTP was observed in our investigation as well as in another independent study (T.T. Tang et al., 2009). The
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Imatinib was first approved for the treatment of Philadelphi
2024-05-18

Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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Thus we presumed that ALDH A might
2024-05-18

Thus, we presumed that ALDH1A3 might play an important role in TMZ-chemoresistance in glioblastoma patients. As we expected, the glioblastoma cell lines and primary glioma Propidium iodide were more sensitive to TMZ treatment when ALDH1A3 was inhibited or depleted. Consistently, it has been shown
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It is reported that Adiponectin is able to suppress
2024-05-18

It is reported that Adiponectin is able to suppress NF-κB pathway, and Bcr-Abl fusion oncoprotein in CML activates NF-κB by stimulating its nuclear translocation and also by enhancing its transactivation function [25], [26]. Therefore, it is tempting to hypothesize that NF-κB pathway might be involv
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br Conclusion The HT receptor family is complex and
2024-05-18

Conclusion The 5-HT receptor family is complex, and one may ask as does Bryan Roth et al. [205] whether this is useless auda (i.e. too much redundancy) or an embarrassment of the riches (i.e. many potential targets to choose from to affect normal or pathological function); molecular biology has
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