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As before all calculations are based on thermodynamically fi
2020-01-16
As before [3], [4], all calculations are based on thermodynamically first- and second-order hydropathic (amino acid) scales [6], [7], linearly scaled to a common center and a common range for each of the 20 amino acids. These are then converted to a triangular matrix , where is the length of a sli
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A second advance came with the discovery that conformational
2020-01-16
A second advance came with the discovery that conformationally-flexible benzamide analogs having an N-phenylpiperazine moiety possessed good affinity and modest selectivity for D3 versus D2 receptors [3,[14], [15], [16]]. This observation spawned a significant effort by medicinal chemists to develop
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We used two different VSMCs
2020-01-16
We used two different VSMCs cell lines, KSB and CSD (isolated from two different thoracic aortas). Rat aortic VSMCs were isolated from medial segments from thoracic rate 4-ap from Wistar-Kyoto rats (six to eight weeks old, Charles River Wiga GmbH) and cultured over several passages as described . Q
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br Material and methods br Results br Discussion br Conclusi
2020-01-16
Material and methods Results Discussion Conclusions To conclude, although CPT2 and CPT1 must have co-evolved to establish the carnitine shuttling, these enzymes are the most distantly related carnitine transferases, split early in evolution, during which a switch occurred in their locati
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muscarinic receptors br Roles of ERR in Physiology and
2020-01-15
Roles of ERRγ in Physiology and Disease Concluding Remarks and Future Perspectives Over the last decade, the generation of tissue-specific ERRγ transgenic or knockout mice and the use of synthetic ligands have rapidly advanced our understanding of the roles of ERRγ in cellular functions, altho
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EP is the major receptor to mediate PGE induced inflammatory
2020-01-15
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by bace inhibitors in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16], [26]. Ho
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br Oxysterols as Key Players in Metabolic
2020-01-15
Oxysterols as Key Players in Metabolic Syndrome? Obesity and sedentary lifestyle are on the rise and pose serious threats to people\'s health and wellbeing. Obesity is often associated with other pathologies and is one of the criteria included in the definition of metabolic syndrome (MetS) (see G
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Dysfunction of the ubiquitin proteasome
2020-01-15
Dysfunction of the ubiquitin-proteasome system causes abnormal organelle morphology and impairs sperm formation and maturation steps resulting in male infertility [[7], [8], [9]]; this indicates that ubiquitination is essential for spermatogenesis and sperm function during fertilization. β-catenin i
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br Materials and methods br Results br Discussion
2020-01-15
Materials and methods Results Discussion The first DGAT1 gene was described in the mouse in 1998 [28], and a few years later DGAT2 was identified from the oleaginous fungus Mortierella ramanniana[29]. Although both of them are known as the primary enzymes for de novo TAG biosynthesis, they
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Herein we designed a strategy utilizing the target protectio
2020-01-15
Herein, we designed a strategy utilizing the target-protection method to produce a signal in a system involving fluorescence CuNPs stabilized by dumbbell template DNA (DT DNA) through a locked circle consisting of two poly T loops and a poly (ATTA) stem. In the presence of MTase, DT DNA was modified
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Classical DHFR inhibitors such as methotrexate MTX bind
2020-01-15
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Azaserine residues as well as hydrophobic
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br Materials and methods br Results
2020-01-15
Materials and methods Results Discussion Although no increase in DAPK activity was detected at early time points associated with neuronal apoptosis, it is possible that the spread of apoptosis through the Sulforaphane following HI is not synchronized enough to yield a large, consistent flu
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br Cyclin dependent kinases control more than
2020-01-15
Cyclin-dependent kinases control more than cell cycle CDKs’ roles conducting the concert of Rivaroxaban was first revealed in the context of the tumor suppressor Rb, phosphorylation of which by CDK4 or CDK6 inactivates it loosing the transcription factor E2F [1], [12], [15]. Discovery of other c
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These contrasting results observed with intra BNST combined
2020-01-15
These contrasting results observed with intra-BNST combined injections of NOC-9 and CP 376395 on freezing (in the novel arena) versus anxiety-related behavior (in the EPM) suggest that CRF neurotransmission within this forebrain limbic site could be mainly involved in the modulation of more subtle a
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Previously we have shown that
2020-01-15
Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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