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A high throughput screening campaign
2023-08-25
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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The following are the supplementary data related
2023-08-25
The following are the supplementary data related to this article. Competing interest Ethics approval and consent to participate Authors' contributions Acknowledgements The authors thank Dr. D. R. Kaplan for kind advice and materials derived from NB primary cell lines, Dr. F. D. Miller f
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Aminoglutethimide first generation aromatase inhibitor has b
2023-08-25
Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome
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SB742457 Although the role of apelin and APJ receptor
2023-08-25
Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G
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br APJ expression in metabolic diseases Under physiological
2023-08-25
APJ expression in metabolic diseases Under physiological conditions, APJ is present in humans as well as in mouse tissues with high metabolic activity such as muscle and adipose tissue but not in the liver. Moreover, the presence and regulation of APJ in established adipocyte or muscle cell lines
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The functions of HMGN protein are modulated
2023-08-25
The functions of HMGN1 protein are modulated by various post-translational modifications, including phosphorylation , , , acetylation , and glycosylation . Phosphorylation in HMGN1 may influence its binding affinity to DNA or nucleosome-associated proteins and affect the sub-cellular localization an
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Finally microRNAs miRNA seem to play an
2023-08-25
Finally, microRNAs (miRNA) seem to play an important role in AR signaling in BC. Some authors have described a differential Febuxostat of miRNAs in AR-positive BCs compared to AR-negative ones. VEGF and mTOR pathways were also reported as implicated in miRNA dysregulation, suggesting a common underl
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The molecular mechanisms that mediate the plasticity of
2023-08-25
The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct
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Epidermal growth factor EGF has been shown to increase the
2023-08-25
Epidermal growth factor (EGF) has been shown to increase the 12S-lipoxygenase mRNA level by about two-fold in human epidermoid carcinoma A431 cells [71]. This enzyme was shown to be of the platelet-type and associated with the microsomal fraction of the cells [71], [72]. A requirement for EGF recept
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The fact that Yoda can activate Piezo
2023-08-25
The fact that Yoda1 can activate Piezo1 in the absence of other cellular components other than a cell membrane [2], suggests that it may directly interact with and activate Piezo1. However, this does not preclude Yoda1 from interacting and activating non-Piezo channels, particularly in endothelial c
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br Conclusion br Acknowledgement This work was supported
2023-08-25
Conclusion Acknowledgement This work was supported by JSPS KAKENHI (Grant Number 15K18770). Introduction Neural crest SR3335 are multipotent progenitors in the vertebrate embryo that give rise to a vast array of different cell types including pigment cells, craniofacial skeleton and mesenc
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Regarding the HT B receptors they act as
2023-08-24
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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Notably both circulating adiponectin and adipsin were equall
2023-08-24
Notably, both circulating adiponectin and adipsin were equally diminished by about 50% in Arfrp1 mice consistent with several studies reporting overlapping trafficking routes for their secretion from 3T3-L1 pdk 1 which was strikingly inhibited upon ablation of TfR-positive endosomes [18,26,33]. In
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In this study high concentrations mM
2023-08-24
In this study, high concentrations (0.5–4 mM) of thuringiensin were required to stimulate the basal adenylate cyclase activity Fig. 2, Fig. 3, Fig. 4, but low concentrations of thuringiensin (1–100 μM) were sufficient to inhibit the forskolin-stimulated adenylate cyclase activity in rat cerebral cor
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While A Rs communicate mainly with the
2023-08-24
While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this MLN9708 area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neurons [69]. This inter
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