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resazurin receptor In diseased blood vessels increased produ
2022-03-21
In diseased blood vessels, increased production of reactive oxygen species (ROS), such as peroxynitrite, superoxide, and hydrogen peroxide, have been found [[53], [54], [55]]. Peroxynitrite was suggested to alter the redox state of sGC [53] while hydrogen peroxide interfered with the action of NO bu
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br Regulation of gonadotropins by
2022-03-21
Regulation of gonadotropins by GnRH GnRH is released from the hypothalamus, and its release pattern is known to be pulsatile. That is, the pulse frequency and amplitude of GnRH release vary physiologically during reproductive cycles in females, and differentially stimulate the production and rele
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Variants of NEIL were also analysed in
2022-03-21
Variants of NEIL1 were also analysed in Primary sclerosing cholangitis (PSC) and cholangiocarcinoma (CCA) patients by Forsbring et al. to identify effect of variants on these diseases. Four variants were identified i.e., one earlier validated (G83D) and three novel (E181K, H275, R339W). E181K was fo
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In experiments using D to displace binding
2022-03-21
In experiments using D22 to displace binding of specific high-affinity radioligands for DAT, NET, and SERT in mouse 6-Aminonicotinamide tissue, we observed a ranking with D22 displacement efficiency in the order of DAT > SERT > NET (IC50 values being ~ 11 (DAT), 26 (SERT), and 101 (NET) µM; Fig. 1,
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br Conclusions The results of this work showed that glucosid
2022-03-21
Conclusions The results of this work showed that β-glucosidase could be efficiently immobilized onto hydroxyapatite nanoparticles in a single adsorption step. The enzyme adsorption was accomplished by coordination bonds between remaining Ca2+ sites of HA and COO− of amino acids. The immobilizatio
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In contrast with the above results
2022-03-21
In Voriconazole synthesis with the above results, in our GC model system, FPR1-, but not FPR2-knockout, enhanced tumour formation. However, it should be noted that the prominent role of mFPR2 with respect to mFPR1 in the mouse colon might be due to the significantly higher expression of mFPR2 than
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br Results and discussion br Conclusion In
2022-03-21
Results and discussion Conclusion In summary, we designed and discovered a series of novel GPR40 agonists containing 3,5-dimethylisoxazole with improved tPSA and ideal cLog P. Most of these compounds were confirmed as excellent GPR40 agonists in vitro. Especially, compound 11k exhibited robust
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In human cancers it has been identified that FOXC AS
2022-03-18
In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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br Significance Cellular heterogeneity for phenotypic featur
2022-03-18
Significance Cellular heterogeneity for phenotypic features is a key mechanism underlying disease progression and therapeutic resistance, yet its regulation is poorly understood at the molecular level. Our findings demonstrate that endocrine resistance is associated with higher transcriptomic het
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In hypoxic breast cancer cells BNIP mediated autophagy activ
2022-03-18
In hypoxic breast cancer cells, BNIP3-mediated autophagy activation and elevation of amino dynorphin levels were notable. BNIP3, a BCL-2 family protein, is known to be transcriptionally regulated by HIF-1α and to be involved in cancer cell death in hypoxic conditions [51]. As a link to autophagy, h
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Mammals have three known Gli proteins
2022-03-18
Mammals have three known Gli proteins: Gli-1, -2 and -3. Gli-1 does not undergo proteosomal degradation and hence, remains untruncated and always acts as a transcription promoter. Gli-1 is an important target gene for Gli-2. Full-length Gli-2 accumulates when Smo is activated because activated Smo p
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Our data demonstrate that cobas HCV s performance
2022-03-18
Our data demonstrate that cobas HCV’s performance characteristics meet these requirements, making the assay useful in the management of therapy for chronic hepatitis C. We documented that cobas HCV has the requisite LOD, measureable range (15 − 1.0E + 08 IU/mL) and precision allowing for baseline HC
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Having identified initial leads and further lead optimizatio
2022-03-18
Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Sodium 4-Aminosalicylate derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, me
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As disclosed in our preceding paper medicinal chemistry SAR
2022-03-18
As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, BTZ043 Racemate la
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L-690,330 The activation of the ERK pathway participates in
2022-03-18
The activation of the ERK pathway participates in the transmission of pain signaling by sensitizing primary afferents (Ji et al., 2009, Lai et al., 2011). Thus, the blockade of ERK activation in the primary sensory L-690,330 can reduce the mechanical hypersensitivity and the thermal hypersensitivit
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