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MLN another selective Aurora A inhibitor is said to
2023-01-31
MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 day
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Several combination studies have been performed using
2023-01-30
Several combination studies have been performed using animal models of mucormycosis, principally involving R. arrhizus. In two investigations using diabetic and/or neutropenic mice, a combination of a polyene with an echinocandin was shown to improve survival compared with monotherapies [25], [34].
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Several combination studies have been performed using
2023-01-30
Several combination studies have been performed using animal models of mucormycosis, principally involving R. arrhizus. In two investigations using diabetic and/or neutropenic mice, a combination of a polyene with an echinocandin was shown to improve survival compared with monotherapies [25], [34].
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Here we found that AMPK directly phosphorylates EZH at Thr
2023-01-30
Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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Bleomycin A5 hydrochloride br Discussion Hepatic dysfunction
2023-01-30
Discussion Hepatic dysfunction in the metabolic syndrome is a driver of negative patient outcomes that requires more therapeutic options. The complexity of liver alterations in this disease – elevated de novo synthesis of fatty acids and cholesterol, reduced clearance of circulating atherogenic L
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pi3k inhibitors Perhaps the discovery of this
2023-01-30
Perhaps the discovery of this linkage has served to catapult much of the work on ABCA1, leaving its family member in need of a relationship with a defined human pathology. In this regard, there is by now a quite mature literature that suggests that ABCA2 may have been overlooked in terms of its impo
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br Experimental procedure br Introduction Migraine
2023-01-30
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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It is worth pointing out that phenotypes of in vivo
2023-01-30
It is worth pointing out that phenotypes of in vivo HSP90β inhibition were not identical to those observed in rapsyn mutant mice (Gautam et al., 1995). Postsynaptically, junctional AChR clusters appeared fragmented, in addition to expected reduction in AChR intensity, in muscles injected with 17-AAG
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On the basis of the above
2023-01-30
On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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The purpose of the present study is to
2023-01-30
The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos
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The nAChR has been considered an interesting potential targe
2023-01-30
The α7 nAChR has been considered an interesting potential target for numerous therapeutic indications over the last two decades, with GTS-21 one of the first candidates proposed for Alzheimer's disease [2], [3], [23]. Unfortunately, although many α7-selective agonists have been developed [21], none
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The c C T mutation identified in subject K was
2023-01-30
The c.286C>T mutation identified in subject K20-1 was also reported in other ethnic groups, including Brazilian, French-Canadian, Italian, and Arabs from the United Arab Emirates [20], [21], [22], whereas c.318A>G mutation in subjects K10-1 was previously reported in Asian and Caucasians [13], [23],
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br Introduction The principal pathways of adrenal
2023-01-30
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 ACL Regulation and Role
2023-01-30
ACL Regulation and Role in Lipid Metabolism ACL is a ubiquitous enzyme at the nexus of nutrient catabolism and synthesis of cholesterol and fatty acids. In mammals, it is highly expressed in lipogenic tissues including adipose, liver, and lactating mammary glands [9]. In the presence of ATP and C
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madecassol receptor br Conclusion br Acknowledgement This st
2023-01-30
Conclusion Acknowledgement This study was supported by NIH/NINDSR01 NS036812-16. Introduction Stroke is the leading cause of disability and the fifth leading cause of death in the United States (Writing Group et al., 2016). On average, every 4 min a human dies of stroke (Lackland et al., 2
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