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Taken together BRP represents a novel chemotype of LT biosyn
2023-09-23

Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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Application of the broad acting HTR antagonist methiothepin
2023-09-23

Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L
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The original Aurora kinase was identified during a
2023-09-23

The original Aurora kinase was identified during a phenotypic screen for defects in mitotic spindles in Drosophila mutants. Aurora mutants were so named because of the morphological defects at the mitotic spindle resembling the Aurora borealis, or the Northern light [4]. The structure of the Auroras
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To test the compounds metabolic stability
2023-09-23

To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structura
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Given the recent discovery of regions of single stranded DNA
2023-09-23

Given the recent discovery of regions of single-stranded DNA in the nuclei of hypoxic cells, the role for ATR in the response to hypoxic stress seems clearer . Zou and Elledge demonstrated that both Ddc 2 (the homolog of ATRIP) and ATRIP have a lower affinity for double-strand breaks than they do f
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Although TP status has been shown to play a role
2023-09-23

Although TP53 status has been shown to play a role in ATR inhibition and platinum resistance [7], [27], [38], in inhibition of ATM and sensitivity to IR [39], and in the activation of Chk1 and Chk2 [3], [4], ATM and ATR signaling can occur through the p38MAPK/MK2 pathway in p53-deficient Etoposide [
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Similar to other MADS box
2023-09-23

Similar to other MADS box proteins, MEF2 factors associate with a variety of transcriptional cofactors to control specific sets of downstream target genes. Some of the cofactors such as MyoD, GATA4, NFAT, TH receptor, p300, 14.3.3 and ERK5 stimulate MEF2 activity, whereas others, such as HDACs4-5-7-
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br Results and discussion The soil fungus
2023-09-23

Results and discussion The soil fungus PSU-RSPG37 (BCC56870) was isolated from soil samples collected from Rajjaprabha Dam, Suratthani Province, Thailand. The fungus was deposited at BIOTEC Culture Collection, National Center for Genetic Engineering and Biotechnology (BIOTEC), Thailand Science Pa
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In the current investigation we studied the
2023-09-23

In the current investigation, we studied the effect of propofol on prostate cancer cells. Propofol is one of the most commonly used drugs in the critical care setting and for the induction of general anesthesia and moderate and deep sedation intraoperatively. Recent studies indicated that propofol e
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The expanding catalog of glutamate receptor
2023-09-23

The expanding catalog of glutamate receptor auxiliary subunits and associated transmembrane proteins underscores the importance and complexity of the receptor complexes. Whereas the interactions described here specifically control AMPARs, distinct auxiliary subunits, Neto-1/2, modulate neuronal kain
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Furthermore to address the concern that the observed positiv
2023-09-23

Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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Although several ARIs have reached various
2023-09-23

Although several ARIs have reached various phases of clinical experimentation however most of them have been withdrawn either due to an insufficient bioavailability, their poor efficacy or adverse side effects. Currently Epalrestat is in clinical use for the treatment of diabetic neuropathy. The sid
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shows the synthesis of imidazole intermediates and The key
2023-09-23

shows the synthesis of imidazole intermediates , , and . The key precursor keto aldehyde – was prepared in situ by SeO mediated oxidation of corresponding carbonyl compounds and or hydrolysis of dibromo ketone . Subsequent treatment with -Boc piperidine-4-carbaldehyde in the presence of aqueous NHOH
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In vivo CA mediate hypoxic nutritional and neurologic stress
2023-09-23

In vivo CA mediate hypoxic, nutritional, and neurologic stress responses. Stimulation of ADRα2A by these hormones to reduce β-cell metabolism has an obvious role in suppressing insulin secretion (Arun, 2004). Since β-cell metabolism and insulin secretion are linked, mechanisms that inhibit metabolis
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Extracellular adenosine acts as a local modulator of
2023-09-22

Extracellular adenosine acts as a local modulator of cell function via four adenosine receptor subtypes (A1Rs A2AR, A2BR, and A3R) that are involved in numerous physiological and pathophysiological processes [31]. Each is encoded by a separate gene and has different functions, although with some ove
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