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Pimozide receptor All DGKs have at least two
2021-01-11

All DGKs have at least two cysteine-rich regions homologous to the C1A and C1B motifs of PKCs [26]. In theory, these domains may bind DAG, perhaps localizing DGKs to where DAG accumulates. However, no DGK C1 domain has so far been conclusively shown to bind DAG. In fact, structural predictions sugge
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With the recent expanse of technology to evaluate synthetic
2021-01-11

With the recent expanse of technology to evaluate synthetic lethality, new combinations with DHODH inhibitors may be uncovered (O'Neil, Bailey, & Hieter, 2017). Many oncogenic backgrounds share synthetic lethality with DHODH. Cells with mutant PTEN have increased glutamine metabolism and are sensiti
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Currently it is not known if drought induces changes in
2021-01-11

Currently, it is not known if drought induces changes in the cysteine protease AZD3514 australia of soybean nodules. The available annotation of the soybean genome, in Phytozome (www.phytozome.net) has identified 706 C1 cysteine protease sequences and 75 C13 cysteine proteases. We have previously re
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Therefore in this study we determined whether exogenous LTD
2021-01-11

Therefore, in this study we determined whether exogenous LTD, a potent agonist of both CysLT and CysLT receptors , , induces STF-118804 edema and AQP4 expression in mouse brain; if so, which subtype of the receptors is involved in AQP4 expression in mouse brain and the cultured rat astrocytes. Mat
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In summary our findings show that
2021-01-11

In summary, our findings show that LPS can activate CysLT2R on microglial Derquantel to induce microglial inflammation and microglia-dependent neuronal death. Furthermore, pharmacological inhibition or knocking down of CysLT2R expression protects neurons against neurotoxicity via suppression of LPS
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In addition to the blockade of
2021-01-11

In addition to the blockade of airway smooth muscle contractions, CysLT1 receptor antagonists also exerted a potent anti-inflammatory effect at this level. The oral administration of MEN91507, Pranlukast, Montelukast, and Zafirlukast also produced a long-lasting inhibition of leukotriene D4-induced
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Pharmacogenomics is the study of the role of the genome
2021-01-11

Pharmacogenomics is the study of the role of the retinoic acid receptor in drug response. It was reported that the effectiveness of atorvastatin was affected by genetic factors.26, 27 In previous studies, there are many genetic polymorphisms related to the efficacy of atorvastatin. Cerda et al repo
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Soluble receptors have been shown to
2021-01-11

Soluble receptors have been shown to be important and common regulators of many cytokines within the immune system, including IL-1, IL-6, IFNγ, TNF-α, GM-CSF, G-CSF and others (Fernandez-Botran, 1991, Heaney, Golde, 1998). We previously described a novel soluble receptor, sCSF-1R, that to date has o
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Beside the previously reported Topo I inhibition
2021-01-11

Beside the previously reported Topo I inhibition, time and concentration dependent CRM1 inhibitory properties of klavuzon derivatives have been shown as a second mechanism of action in this work. Especially, compounds 3 and 20 are the most effective derivatives and they completely inhibit CRM1 activ
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Unexpectedly CRF receptor agonist and antagonist evoked simi
2021-01-11

Unexpectedly, CRF2 receptor agonist and antagonist evoked similar effects in the fall in tail skin temperature caused by restraint. However, Ucn3 reduced basal values of tail skin temperature, thus indicating that some degree of basal vasoconstriction caused by BNST treatment with Ucn3 may have cont
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br Study design br Results We enrolled subjects
2021-01-11

Study design Results We enrolled 50 subjects awaiting SOT (15 kidney, 14 liver, 1 liver + small bowel, 11 lung, 9 heart) and 50 controls (Table 1) who were similar with respect to median age (subjects 49.1 yrs., controls 48.6 yrs.) gender (64% male subjects and controls), and CMV-seropositivit
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Based on the above we hypothesized that
2021-01-11

Based on the above, we hypothesized that a PROTAC strategy would be effective to induce CK2 protein degradation. Herein reported is an approach for the preparation of novel PROTACs via “click reaction” for degradation of CK2 protein (Fig. 2). Importantly, “click reaction” is a very facile, selective
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Besides the assessment of toxicological effects immediately
2021-01-11

Besides the assessment of toxicological effects immediately after exposure, we also studied the potential recovery of the exposed organisms, through the quantification of ChE activity at specific time intervals after placing organisms in clean test medium. Recovery from chemical challenge, in this c
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However not all inhibitory profiles by metals
2021-01-11

However, not all inhibitory profiles by metals can be a priori considered artifacts of the methodology used to quantify the activity of such enzymes. Metals can indeed interfere with cholinesterases, and the mechanisms are varied. The inhibitory effect of specific metals may derive from their abilit
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As the primary model we selected LDL receptor knockout
2021-01-11

As the primary model we selected LDL-receptor knockout mice because these resemble the human plasma lipoprotein profile more closely. Currently, genetic models with reduced milk cholesterol content, which mimic cholesterol-free formula feeding, are unavailable. Thus, instead of modifying milk choles
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