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Introduction hydroxytryptamine HT is found throughout
2024-05-21
Introduction 5-hydroxytryptamine (5-HT) is found throughout the body and influences smooth muscle activity in various tissues including the intestine, vasculature and urinary gaba receptor (Kim and Camilleri, 2000, Klarskov and Horby-Petersen, 1986, Mohammad-Zadeh et al., 2008). The current classi
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Here we show that the
2024-05-21
Here, we show that the co-activation of RTKs and non-RTKs is a common trait in treatment-naïve EGFR-mutation-positive NSCLC AS-605240 and patients, with AXL and CDCP1 being commonly over-expressed. The combination of gefitinib or osimertinib with the Src/FAK/Janus kinase 2 (JAK2) inhibitor TPX-0005
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Five alternatively spliced isoforms of
2024-05-21
Five alternatively-spliced isoforms of ATX have been described and all are catalytically active [16], [17]. The original ATX described in 1992 is termed ATXα, whereas the most abundant isoform is ATXβ and is the same isoform responsible for plasma lysoPLD activity [18]. Full length ATX is synthesize
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The Type A series contains of the confirmed hits
2024-05-21
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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This project was funded by the University of the Philippines
2024-05-21
This project was funded by the University of the Philippines Diliman through the Natural Sciences Research Institute with grant No. CHE-09-2-02. Introduction There is compelling evidence for an anti-inflammatory effect of 12- and 15-lipoxygenases through the generation of lipid mediators involve
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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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