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Hedamycin isolated from Streptomyces griseoruber belongs to
2021-03-12
Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of PFTα (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)). Hedamyc
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The compounds were ranked based on
2021-03-12
The compounds were ranked based on the Glide XP Score, as shown in . All 15 compounds were subject to a radiometric assay previously used in our lab to evaluate their ability to inhibit DHFR steady-state activity in recombinant TS-DHFR (A). Compound demonstrated greater than 50% inhibition of DHFR
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Ultimately we decided to investigate the role
2021-03-11
Ultimately, we decided to investigate the role of Cyp3a in obesity because Hepatic P450 Reductase-null (HRN) mice with no P450 activity show hepatic steatosis with increased Cyp2b10 and Cyp3a11 expression, perturbations in liver size, lipid homeostasis, and increased liver polyunsaturated fatty acid
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br Prostaglandin D PGD is derived from
2021-03-11
Prostaglandin D (PGD) is derived from the metabolism of arachidonic ICI 118,551 hydrochloride by cyclooxygenases and downstream PGD synthases. In the immune system, PGD is mainly produced by mast cells but also although at lower levels, by macrophages and Th2 lymphocytes. PGD binds to three diffe
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Immunofluorescence Cells were fixed with paraformaldehyde PF
2021-03-11
Immunofluorescence. Cells were fixed with 4% paraformaldehyde (PFA) in PBS and extracted by 0.5% Triton X-100-PBS, or fixed in cold methanol. The cells were immunostained with mouse monoclonal Cl-Amidine trifluoroacetate salt against α-tubulin (Sigma), γ-tubulin (Sigma), Ran (Upstate), rabbit polyc
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br Study design br Results To explore potential
2021-03-11
Study design Results To explore potential differences in the volume the different swabs absorb, the loss of weight of tubes filled with water after soaking the different swabs under defined conditions was determined. This revealed that the different swabs absorbed between approximately 0.07 an
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br Materials and methods br Results br Discussion In this
2021-03-11
Materials and methods Results Discussion In this study, we confirmed the activation of Akt by udenafil in 3T3-L1 cells. To elucidate the underlying mechanism of udenafil, we focused on the mitochondria. Our findings demonstrated that udenafil improved mitochondrial function and expression o
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ganciclovir receptor To study systemic potential of the sele
2021-03-11
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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Apart from the ET system s role in
2021-03-11
Apart from the ET system's role in regulating blood vessel tone, it is also involved in a variety of cellular processes that are relevant to DR. For example, the ET receptors influence the survival of retinal ganglion kinesin inhibitor (McGrady et al., 2017; Tonari et al., 2012), development of the
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In addition to glutamatergic inputs the RTn integrates choli
2021-03-11
In addition to glutamatergic inputs, the RTn integrates cholinergic, serotonergic and noradrenergic synapses of fibers coming from nuclei located in the brainstem (Asanuma, 1992, Morrison and Foote, 1986, Pare et al., 1988) involved in the alternating firing mode and in the frequency changes of reti
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Common enzyme quantitative methods include enzyme linked imm
2021-03-11
Common enzyme quantitative methods include enzyme-linked immunosorbent assay [,] (ELISA), chemiluminescence (CLIA) [, , ] and immunochromatography []. The advantages of ELISA are cost reduction and automation, but non-specific reaction caused by HOOK effect, false positive caused by cross-contaminat
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Here we investigate in more detail how Dot function contribu
2021-03-11
Here we investigate in more detail how Dot1 function contributes to the regulation of DNA damage tolerance. We find that Dot1 modulates the response to the alkylating agent MMS through its catalytic activity on H3K79. In fact, progressively reduced levels of H3K79 tri-methylation result in graduall
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Given the excellent in vitro pharmacology
2021-03-11
Given the excellent in vitro pharmacology profiles of methyl ester 28 and primary amide 29 efforts were reengaged on neutral analogs of these leads, with a focus on non-amide replacements for the carboxylic Aldicarb functionality of 1. Acetonitrile 49 was found to have a good balance of DGAT-1 inhib
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br Materials and methods br Acknowledgements SD was supporte
2021-03-10
Materials and methods Acknowledgements SD was supported by a pre-doctoral research fellowship from the Flanders Agency for Innovation and Entrepreneurship (VLAIO-Flanders, Belgium). YB is supported by a postdoctoral fellowship from Research Foundation Flanders (FWO, Belgium). We thank Isabelle
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br Chagas disease Chagas disease an NTD
2021-03-10
Chagas disease Chagas disease, an NTD caused by the protozoan Trypanosoma cruzi, affects 8–10 million people globally. More than 10,000 deaths are caused by the disease each year, and nearly 70 million people are susceptible to infection (Manne-Goehler, Umeh, Montgomery, & Wirtz, 2016). Chagas di
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