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APJ is mainly coupled to PTX sensitive Gi
2022-10-31
APJ is mainly coupled to PTX-sensitive Gi/o proteins [33], and thus, it is associated with the inhibition of adenylyl cyclase and the activations of PI3K/Akt signaling and MAPKs signaling pathways [23], [54], [55], [56]. In a previous study, apelin stimulations of the PI3K/Akt and/or the MAPK pathwa
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br Antioxidant polymers conjugates Natural
2022-10-31
Antioxidant-polymers conjugates Natural antioxidants are usually used as a substitute for synthetics but some degradation phenomena could influence their applications. For example, ascorbic cathepsin g synthesis as a natural antioxidant undergoes yellowish coloration as a result of oxidation [29
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HMGN proteins are subject to extensive post translational
2022-10-31
HMGN proteins are subject to extensive post-translational modifications which influence both their mode of binding to vorapaxar and their functional activity. Like the other HMG protein families, HMGNs are substrates for many of the same enzymes that modify histone proteins (review in [175]). The h
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In fact serotonin is a
2022-10-27
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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br Experimental procedure br Introduction
2022-10-27
Experimental procedure Introduction Migraine is a debilitating neurovascular disorder characterized by recurring unilateral pulsating headaches of moderate to severe intensity, associated with nausea, photophobia and/or phonophobia, lasting from 4 to 72 h (Headache Classification Committee of
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The potential use of derivatives belonging to this series as
2022-10-27
The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore
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A high throughput small molecule ACK biochemical inhibition
2022-10-27
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found JTC-801 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perf
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This study was funded and supported by Tehran University of
2022-10-27
This study was funded and supported by Tehran University of Medical Sciences and Health Services; and Iran National Science Foundation. Introduction The enzyme acetylcholinesterase (AChE) plays a central role in the signal transduction in the nervous system, hydrolyzing the neurotransmitter acet
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In addition to the above mentioned synaptic mechanisms
2022-10-27
In addition to the above-mentioned synaptic mechanisms, the serotonergic system also has a critical role in the antidepressant effects of mGlu2/3 receptor antagonists. Indeed, we previously reported that mGlu2/3 receptor antagonists increased the firing rate of serotonin neurons in the dorsal raphe
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Pompe disease is accompanied by
2022-10-27
Pompe disease is accompanied by the deficiency of the lysosomal α-1,4-glucosidase that makes the TMP269 synthesis unable to hydrolyze glycogen to glucose, thereby resulting in the accumulation of glycogen in lysosomes, especially in skeletal muscles and cardiac tissues. This accumulation results in
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Unfortunately results of serum plasma AC assessment after fo
2022-10-27
Unfortunately, results of serum/plasma AC assessment after food antioxidant intake are rather controversial: although some papers reported an increase of AC after food antioxidant intake (Khan et al., 2015, Torabian et al., 2009), unexpectedly, in a lot of long-term intervention studies (days, weeks
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br Emerging Vascular Mechanisms of AA Therapy Resistance Exp
2022-10-27
Emerging Vascular Mechanisms of AA Therapy Resistance Experimental and clinical evidence indicates that physiological angiogenesis generates blood vessels capable of restoring perfusion [1], whereas tumoral angiogenesis gives rise to vessels that are structurally and functionally abnormal, therei
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Manumycin A Several ceritinib resistant mutations following
2022-10-26
Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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Among all the compounds the
2022-10-26
Among all the compounds, the novel L-748,337 derivative (23d) showed the potent human β3-AR antagonist activity and high lipolysis inhibitory activity in vitro. The Saikosaponin A 23d displayed 23-fold more potent β3-AR antagonist activity (EC50 = 0.5117 nM) than that of L-748,337 (EC50 = 11.91 nM)
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In the isolated right atrium activation of
2022-10-26
In the isolated right atrium, activation of muscarinic receptors and adenosine receptors may block the generation of action potentials in the sinoatrial node, inducing cardiac arrest (Fig. 1, Fig. 2, Fig. 3, Fig. 4, Fig. 5) (Camara et al., 2015, Campbell et al., 1989). Physiologically, this conditi
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