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In recent years there have been further significant developm
2024-08-08
In recent years, there have been further significant developments that enhance an understanding of the role of adenosine in nociception. Thus, novel methods of recruiting adenosine A1Rs have been developed, and the role of adenosine A2A- and A3Rs in nociception has been further elaborated. Furthermo
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sVRPs were more sensitive to ABT than
2024-08-08
sVRPs were more sensitive to ABT-702 than MSRs. This result agrees with previous reports that the activation of A1 receptors more potently inhibits sVRPs than MSRs (Nakamura et al., 1997, Otsuguro et al., 2009). Importantly, sVRPs are thought to reflex C-fiber-evoked nociceptive transmission. Nocice
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A high throughput small molecule
2024-08-08
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found leukotriene receptor antagonists to be both ATP-competitive and reversible. Early structure-activity relatio
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ACh induced changes in respiratory frequency could be
2024-08-08
ACh-induced changes in respiratory frequency could be of interest. They may reveal an important mechanism of respiratory modulation at the caudal NTS level. ACh-induced increases in respiratory frequency within this region have been also reported by Furuya et al. (2014). Changes in respiratory timin
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br Conclusion Growth survival and invasion
2024-08-08
Conclusion Growth, survival, and invasion of most PCs have been shown to be androgen-dependent at the onset of castration therapy [31]. Thus, castration therapy has been central to systemic therapy and remains the standard approach to PC treatment. Even after progression to a castration-resistant
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Screening a selection of analogues from this library
2024-08-08
Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to Sorafenib mg 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrated
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Our data indicate that the
2024-08-08
Our data indicate that the D1 domain only needs to hydrolyze ATP a few times, or perhaps even just once, during the processing of a given substrate molecule, whereas the D2 domain hydrolyzes ATP many times. Consistent with this model, only D2 contains the canonical aromatic pore loop residues implic
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and LO are members of the lipoxygenase
2024-08-08
5- and 12/15-LO are members of the lipoxygenase family that convert arachidonic AKT inhibitor VIII into lipid mediators such as leukotriene B4 (LTB) and 12()-hydroxyeicosatetraenoic acid (HETE) and 15()-HETE, respectively. Evidence from several in vitro and in vivo studies has shown that activation
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Based on its kinetic parameters
2024-08-08
Based on its kinetic parameters and quaternary structure, R. pycnus arginase is a typical ureotelic L-arginase [2]. The Km value of the enzyme was lower than other arginases from other organisms (Table 2), including S. cerevisiae (15.7mM), B. anthracis (10mM), B. caldovelox (3.4mM), human liver (2.3
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Introduction Preeclampsia a serious hypertensive disorder th
2024-08-08
Introduction Preeclampsia, a serious hypertensive disorder that can occur during pregnancy, is a pregnancy-related disease characterized by the onset of fty and proteinuria after the 20 t h week of gestation, and it occurs in about 5% of all pregnancies [1]. If left untreated, preeclampsia can som
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In conclusion our data highlight that
2024-08-08
In conclusion, our data highlight that variable anti-oxidative Sodium ascorbate could be released through peptic hydrolysis of CMP fractions. Although casein hydrolysates produced a larger number of peptides (Table 1) with variable antioxidant capacities, all the peptides from whey hydrolysate exhi
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AP activity is increased by MAP kinase stimulation
2024-08-08
AP-1 activity is increased by MAP kinase stimulation in different cell types (Whitmarsh and Davis, 1996), while MKP-1, the enzyme that catalyzes the dephosphorylation and inactivation of MAP kinases in the nucleus, inhibits AP-1 (Rössler et al., 2008, Rössler and Thiel, 2009, Mayer et al., 2011, Thi
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The current literature clearly states that there are
2024-08-08
The current literature clearly states that there are no widely adopted standardized methods to determine the total antioxidant capacity of foods or biological samples. One should consider the antioxidant reaction mechanism in system to determine the most appropriate methods for the measurement. It h
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We recently identified a G A dependent epigenetic mechanism
2024-08-07
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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For the first series we decided
2024-08-07
For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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