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Although pharmacological studies from the
2022-07-14
Although pharmacological studies from the end of the 20th century suggested that β1-AR induces a cAMP-dependent apoptosis [30], more recently it has been demonstrated that cAMP, acting through PKA, may be a crucial anti-apoptotic factor in cardiac myocytes [31]. cAMP can also stimulate PI3K, and the
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The lack of biological activity http www apexbt
2022-07-14
The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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Much is known about FPPS structure and function with over
2022-07-14
Much is known about FPPS structure and function, with over 120 FPPS crystal structures being currently available. This wealth of information is largely the consequence of human FPPS serving as a drug target for the treatment and/or prevention of pathologies such as osteoporosis, hypercalcemia and P
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Microglia after activation can show prominently
2022-07-14
Microglia after activation can show prominently pro-inflammatory but also anti-inflammatory characteristics [46]. Although the ageing process is not a pathological process, many of the age-associated changes resemble those observed under pathological conditions. An increase number of pro-inflammator
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Histone modification is one of the major epigenetic mechanis
2022-07-14
Histone modification is one of the major epigenetic mechanisms.8, 10 Specific histone modifications confer active or repressive transcriptional states. For instance, the trimethylation of Histone3-Lysine27 (H3K27me3) is a marker of tightly packaged heterochromatin and is associated with gene repress
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In humans mutations in KDM A KDM B and KDM
2022-07-14
In humans, mutations in KDM5A, KDM5B, and KDM5C are found in patients with ID, implicating KDM5-regulated transcription in the development or activity of neuronal tissues (Vallianatos and Iwase, 2015). KDM5D is Y-linked, and its role in cognition remains uncharacterized. Mutations in KDM5C are the m
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individuals with variants in the codon region
2022-07-14
13 individuals with variants in the codon 1031–1159 region had global developmental delay and apparent ID, ranging from speech delay and learning difficulties to markedly impaired basic life functions (Table 2 and Table S3). The last available occipitofrontal-circumference measurements revealed micr
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69 8 receptor br Conclusion Our data allow pharmacological d
2022-07-14
Conclusion Our data allow pharmacological discrimination of diverse of H3 69 8 receptor antagonists that can be linked to their differential efficacy in preclinical and clinical disease settings (Fig. 6). Moreover, we identify the sigma-1 receptor as a common “off target” for H3 antagonists, and
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It is important to mention that the IC of
2022-07-14
It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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br STAR Methods br Acknowledgments
2022-07-14
STAR★Methods Acknowledgments We thank P. Adler, V. Riechmann, N. Tapon, E. Knust, the Vienna Drosophila RNAi Center, the Australian Drosophila Research Support Facility (www.ozdros.com), the Bloomington Drosophila Stock Center, and the Developmental Studies Hybridoma Bank for D. melanogaster s
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br Parkinson disease Idiopathic PD is a hypodopaminergic
2022-07-14
Parkinson disease Idiopathic PD is a hypodopaminergic movement disorder of uncertain etiology that affects 3% of persons over age 65 (Dexter and Jenner, 2013). Cardinal signs of this common neurodegenerative condition include bradykinesia, rigidity, rest tremor and postural instability. Autonomic
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Two kind systems are currently available to
2022-07-13
Two kind systems are currently available to assess the nutritional status of cancer patients, one is largely based on some subjective parameters, the other is totally based on the objective parameters. For score systems largely based on some subjective parameters, like Nutritional Risk Screening Sco
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br The serine threonine kinase haspin ploid
2022-07-13
The serine/threonine kinase haspin (ploid Germ Cell-pecific Nuclear rote Kinase, also known as erm Cell-pecific ene-2; Gsg2) functions in mitosis, where it phosphorylates histone H3 at Thr-3 (H3T3ph). During mitosis, this phosphorylation generates a binding site on H3 for Survivin and thereby posi
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As GSH cellular redox status is critical for various biologi
2022-07-13
As GSH cellular redox status is critical for various biological phenomena including apoptosis and inflammation [34], [35] we hypothesized that inflammation could modulate GSTP1-1 gene expression. Indeed, reactive oxygen species (ROS) are released at inflammation sites and can be eliminated from BW 7
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br Introduction br Mitochondrial dysfunction and cancer br L
2022-07-13
Introduction Mitochondrial dysfunction and cancer Lactate and succinate as oncometabolites Intracellular actions of lactate and succinate as tumor promoters Cell-surface receptors for lactate and succinate and their role in cancer GPR109A as the receptor for butyrate and β-hydroxybu
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