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br Additional CDKs with a role
2021-05-21

Additional CDKs with a role in cancer Small molecule CDK inhibitors The majority of protein kinase inhibitors developed to date are type I inhibitors: they bind at the ATP–binding site, are ATP-competitive and target the kinase in its active state; with the activation loop DFG motif in the ‘in
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br Diseases which have been treated with
2021-05-21

Diseases which have been treated with proteins linked to HSA A number of therapeutic products conjugated to HSA have now been approved for clinical use (Table 2). For example, fatty Caspase Inhibitor Set I derivatives of human insulin bound to HSA have applications in the treatment of diabetes w
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Dihydroartemisinin CPG a metalloenzyme derived from sp was t
2021-05-21

CPG2, a metalloenzyme derived from sp., was the elected enzyme for the first pilot-scale clinical trial of ADEPT. This enzyme has no mammalian homologue and activates glutamic Dihydroartemisinin prodrug derivatives of several nitrogen mustards alkylating agents., , , , , A bond cleavable by CPG2
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The causes of POD are complex and not entirely clear
2021-05-20

The causes of POD are complex, and not entirely clear. Androsova et al, believed that the main molecular mechanism of POD is a central cholinergic deficiency caused by deregulation of cholinergic anti-inflammatory pathways leading to increased inflammation. The cholinergic anti-inflammatory pathway,
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Interestingly increased level of both circulating ET and uri
2021-05-20

Interestingly, increased level of both circulating ET-1 and urinary excretion of ET-1 have been observed in patients treated with nephrotoxic immunosuppressive agents as cyclosporine A and tacrolimus (Slowinski et al., 2002). Other nephrotoxic agents, such as cisplatin, also increase urinary excreti
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In brief while previous studies have
2021-05-20

In brief, while previous studies have evaluated the individual roles of VDR and ER signaling pathways in breast cancer, in the present study we performed an in silico approach for comparative evaluation of these pathways. Considering the complex interaction networks in the context of cancer, such co
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br Effects of estradiol outside the nucleus are
2021-05-20

Effects of estradiol outside the nucleus are often mediated by classical estrogen receptors Today, it is widely accepted that steroid hormones can signal in ways that do not rely on receptors acting in the nucleus, including activation of receptors localized to the cellular membrane. Rapid effec
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We recently employed a functional drug screening approach to
2021-05-20

We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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Importantly a crucial role of transcription factor SP in med
2021-05-20

Importantly, a crucial role of transcription factor SP1 in mediating the anti-lung cancer effect of XJD was found in this study. Our results suggested that the inhibition of SP1 was required to mediate the inhibitory effect of XJD on the growth of NSCLC cells. Nuclear transcription factors SP1 is as
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br Acknowledgements br Introduction Endothelial cells consti
2021-05-20

Acknowledgements Introduction Endothelial capivasertib constitute a unique source of humoral factors that may regulate the functions of other cell types via paracrine or endocrine pathways [1]. Among the many molecules originated from the endothelium, nitric oxide (NO) plays versatile roles i
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In this study we were
2021-05-20

In this study, we were able derive new insights into the biology of DDR2 including the demonstration that cellular tyrosine phosphorylated proteins co-localise with DDR2 and exogenously added collagen I (Fig. 1G). This finding suggests that similar to the focal adhesion complexes associated with int
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Multiple protein species are known to naturally
2021-05-20

Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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br Results br Discussion Oxysterols and EBI have received
2021-05-20

Results Discussion Oxysterols and EBI2 have received growing attention in the field of immunology, with works highlighting an important role for EBI2 in immune cell migration. However, these studies are mainly limited to animal models (Chalmin et al., 2015, Hannedouche et al., 2011, Kelly et a
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Like all other cellular processes ubiquitination is also tig
2021-05-20

Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con
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Here we describe preparation of three stable conjugates
2021-05-20

Here, we describe preparation of three stable conjugates that are linked by either oxyester, disulfide, or isopeptide bonds (Fig. 10.1). Each of these conjugates depends upon the prior purification of E2 and ubiquitin proteins that have been engineered to favor specific linkages. For the oxyester- a
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