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In this article we have outlined
2022-12-01

In this article, we have outlined the increasing, as yet still circumstantial evidence that the 6TM domains of bacterial ACs might operate as receptors for as yet unknown ligands. Intriguingly, several architectural arguments are also applicable to the 6TM domains of mammalian membrane-bound ACs (mA
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Despite these efforts to prevent oxidative metabolic degrada
2022-12-01

Despite these efforts to prevent oxidative metabolic degradation, and showed only marginal improvements in metabolic stability and still exhibited high plasma clearances as shown in . High molecular weight as well as relative high log values could be contributing factors to the poor PK profiles of
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br Thymic expression of AChR Both linear
2022-12-01

Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid follic
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br Acknowledgements br Introduction Resistant hypertension R
2022-12-01

Acknowledgements Introduction Resistant hypertension (RH), is defined as blood pressure (BP) > 140/90 mm Hg despite three full doses antihypertensive drugs including a diuretic. Controlled hypertensive patients taking four gsk525762 receptor or more of antihypertensives are also considered re
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br Trauma and ACEs screening
2022-12-01

Trauma and ACEs screening: the past, present, and future Traditionally, allopathy’s biomedical model has utilized an etic perspective; the outsiders’ view of the problem. Development of diagnostic screening tools requires an etic approach, which relies heavily on a completely objective perspectiv
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br Conclusion There have been multiple
2022-12-01

Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi
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Physiology genetics and biochemistry of CYP A br
2022-12-01

Physiology, genetics, and enos inhibitor of CYP17A1 Clinical presentation and diagnosis Treatment Acknowledgements I thank Dr. Hwei-Ming Peng for assistance with preparing Fig. 3. This work was supported by grant R01GM086596 from the National Institutes of Health. Introduction Prostat
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Ryoichi et al modified potent clinical candidate VX
2022-12-01

Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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In HepG cells compound showed inhibition of
2022-12-01

In HepG2 cells, lomitapide showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, compound
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Several MAP kinases are involved
2022-12-01

Several MAP kinases are involved in the signal transduction pathways that lead to the upregulations of inflammatory mediators. Moreover, transcriptional activations of STATs are regulated by MAP kinases, as evidenced by reports that p38 MAPK is necessary for the S727 phosphorylation of STATs (Kovari
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Previous studies have demonstrated that synaptic AMPARs can
2022-12-01

Previous studies have demonstrated that synaptic AMPARs can differ greatly in their mobility; some rapidly and constitutively daunorubicin synthesis in and out of the synaptic membrane, while others remain somewhat stable in the synaptic membrane (Luscher et al., 1999, Luthi et al., 1999). We find
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br Brain cell reactions Brain cells in common
2022-11-30

Brain cell reactions Brain cells in common with all metabolic cells must contain chemically active primary compounds which spontaneously initiate and continue cell reactions under normal conditions of temperature and pressure (NTP). These compounds have been identified as monophosphoric and polyp
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An important observation is that this patient has
2022-11-30

An important observation is that this patient has been on ALK inhibitor for more than 4 years (51 months: 27 months on crizotinib+24 months on alectinib and on-going) and there was no evidence of disease progression in the central nervous system. The other potential driver mutation in this patient’s
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Adenosine is an endogenous nucleoside
2022-11-30

Adenosine is an endogenous nucleoside that plays pivotal roles in different physiological and pathophysiological processes by triggering specific cell-surface receptors both in the Fmoc-Thr(tBu)-OH and in the periphery. The adenosine receptors (ARs) are four different subtypes of G protein-coupled
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A high throughput small molecule ACK biochemical
2022-11-30

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 PD173074 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was per
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