• br STAR Methods br Acknowledgments Funding for

  2022-03-23

  

  STAR★Methods Acknowledgments Funding for this work was provided by grants from the US National Institute of Allergy and Infectious Diseases (NIAID) (R01-AI095068 and UM1-AI068613 to S.H.E. and U24-AI118633 to H.B.L.) and grant OPP1155863 from the Bill and Melinda Gates Foundation to S.J.E. Ad

• Here we show that Jmjd a zebrafish JmjC domain

  2022-03-23

  

  Here, we show that Jmjd3, a zebrafish JmjC domain-containing protein, possesses H3K27 histone demethylase activity in vivo, and down-regulation of jmjd3 leads to significant reduction of primitive and definitive myelopoiesis. Importantly, we have demonstrated that jmjd3 directly upregulates spi1 exp

• Histamine H and H receptors are

  2022-03-23

  

  Histamine H1 and H2 receptors are considered as low affinity receptors (pKi of 4.2 and 4.3 respectively), whereas histamine H3 and H4 receptors as a high affinity receptors (pKi of 8 and 8.2 respectively) (Schreeb et al., 2013). Therefore it might well be that other histamine receptors might be invo

• Treatment with histamine had no effect on histamine

  2022-03-23

  

  Treatment with histamine had no effect on histamine H1 receptor expression in HepG2 GW3965 (Fig. 1), while knockdown of histamine H1 receptor expression prevented histamine from repressing apo A-I gene expression (Fig. 2). Overexpression of the histamine H1 receptor regulated apo A-I promoter activi

• Aberrant expression of HKII may be a required feature

  2022-03-23

  

  Aberrant expression of HKII may be a required feature for cancer development and progression. Overexpression of HKII has been reported in tumor tissues of cancer patients with liver [9], ovary [8], [24] and larynx [25]. The clinical significance of HKII in cancer was noted as overexpression of HKII

• Although HK localizes mainly to either the

  2022-03-23

  

  Although HK localizes mainly to either the cytosol or mitochondria [29], [30], [31] and cardioprotection is associated with increased mitochondrial HK binding, some studies have identified a component of HK located in intracellular vesicles within the cardiomyocyte [48], [61], supporting older data

• The rationale for developing HDACi as anticancer

  2022-03-23

  

  The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and XCT790 arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematological

• Several classes of small molecules that modulate CDK activit

  2022-03-23

  

  Several classes of small molecules that modulate CDK8 activity have been reported in the patent literature (Fig. 1). A quinazoline derivative, Senexin B (SNX2-1–165, 1), showed CDK8 enzyme inhibitory activity with an IC50 value of 24–50 nM in different assay, and displayed potent, selective enzymati

• Toc and Toc are GTPases

  2022-03-23

  

  Toc34 and Toc159 are GTPases that regulate initial steps of preprotein import [3,4,26]. It was shown that GTP hydrolysis of at least one receptor is necessary to initiate the translocation process [23,27]. As reported for other small G-proteins, Toc34 and Toc159 bind their cargo in a nucleotide-depe

• In the H NMR spectrum two pairs of doublet resonances

  2022-03-23

  

  In the 1H NMR spectrum two pairs of doublet resonances arising from the protons in the aromatic moiety of the two diastereoisomers can be readily observed around 7.5–7.6 ppm. These resonances can be used to detect and quantify the two diastereoisomers. From the results presented in Fig. 1A it can be

• Given the involvement of dysregulated S nitrosylation in mul

  2022-03-23

  

  Given the involvement of dysregulated S-nitrosylation in multiple pathological conditions, a number of approaches to regulate S-nitrosylation therapeutically are being tried in multiple indications [18]. In the lung, GSNO releasing compounds and GSNOR inhibitors are being considered as potential the

• GW9662 A number of in vivo studies have

  2022-03-23

  

  A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g

• Previous studies have demonstrated that cannabinoid potentia

  2022-03-22

  

  Previous studies have demonstrated that cannabinoid potentiation of GlyR α3 subunits contributes to cannabinoid-induced analgesia. For instance, Dehydroxylcannabidiol (DH-CBD), a chemically modified cannabinoid, can alleviate acute pain and chronic inflammatory pain by targeting spinal α3 GlyRs (Xio

• br In vivo actions of

  2022-03-22

  

  In vivo actions of GLP-1/GLP-1R agonists on the vascular endothelium Using contrast-enhanced ultrasound, male Sprague Dawley rats receiving an intravenous infusion of native GLP-1 (30 pmol/kg/min) for 2 h demonstrated significant improvements in both microvascular blood volume and microvascular b

• The eradication of agonist activity in

  2022-03-22

  

  The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary focal adhesion kinase as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also

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