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br Conclusion In summary screening a small compound library
2023-05-26
Conclusion In summary, screening a small compound library based on the 3-aminopyridin-2-one motif in a target-blind manner against a 26-kinase panel, representative of the kinome, identified hits that possess good activity and excellent ligand efficiency against MPS1, Aurora A and Aurora B. The b
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The ambiguity surrounding the role played
2023-05-26
The ambiguity surrounding the role played by the 15-LOXs in malignant biological processes stems also from the limitations of current animal models, and especially the usage of its 12/15-LOX murine homolog, which can also catalyze the production of 12-HETE. Indeed, the proinflammatory effect of 12-H
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br Acknowledgements br Introduction Double stranded DNA
2023-05-26
Acknowledgements Introduction Double-stranded DNA breaks (DSBs) are among the most deleterious DNA lesions that threaten genomic integrity. DSBs are generated not only by exogenous DNA-damaging agents but also by normal cellular processes such as V(D)J recombination, meiosis, and DNA replicati
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br Disclosure br Acknowledgments br Introduction Anaplastic
2023-05-25
Disclosure Acknowledgments Introduction Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase, belongs to the insulin receptor kinase subfamily [1]. Oncogenic activation of ALK is associated with the Tobramycin receptor and progression of multiple human cancer types [2,3], including
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In our previous study we
2023-05-25
In our previous study we found that the total activity of aldehyde dehydrogenase in cancer cytidine of RCC is at the same level as in normal renal tissue [10]. These findings are similar to our results in serum patients with renal cancer. There is no significant difference between ALDH activity in
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Corticosterone induced inhibition of OCT mediated transport
2023-05-25
Corticosterone-induced inhibition of OCT-mediated transport is rapid and appears to involve direct interaction of the steroid with the transporter at a specific site. Volk et al. (2003) studied OCT2-mediated transport by measuring substrate-induced currents using patch clamp of Xenopus oocytes exoge
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Does dietary caffeine interfere with antinociception
2023-05-25
(8) Does dietary caffeine interfere with antinociception by other modalities that alter pain (TENS, exercise, joint mobilization, water immersion therapy)? Caffeine and/or A1R antagonists inhibit antinociception by each of these modalities in preclinical studies, such that there is potential for int
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During the year study period of men in the
2023-05-25
During the 4-year study period, 19.9% of men in the dutasteride group developed prostate cancer as compared to 25.1% in the placebo group, which represents an absolute risk PRT062607 Hydrochloride australia of 5.1% for men taking dutasteride (Pe weighed against the prospect of undesirable sexual si
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br Dihydrotestosterone in adult fish and frogs
2023-05-25
Dihydrotestosterone in adult fish and frogs New perspectives and next directions Similar to other androgens, DHT can modulate reproductive endpoints in both fish and amphibians. However, predicting the effects of DHT can be challenging, as reproductive homeostasis is dependent upon the balance
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br Autophagy at the Synapse The synapse is
2023-05-25
Autophagy at the Synapse The synapse is a highly specialized neuronal compartment that forms the basic unit of communication between neurons. Communication relies on electrical signals that are propagated down the axon of the presynaptic neuron, where they trigger the quantal release of neurotran
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Interestingly this situation might be changed by the immunol
2023-05-25
Interestingly, this situation might be changed by the immunological context, in particular by the cytokines encountered during differentiation or activation. LPS-activation of bone marrow-derived DCs differentiated in GM-CSF decreases autophagy, CP2, and subsequent activation of CD4+ T cells (Fig. 2
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To evaluate the ability of both sets of compounds to
2023-05-25
To evaluate the ability of both sets of compounds to inhibit the activity of 15-LOX an initial screen was performed, whose results are shown in . The comparison of inhibition values would seem to indicate that, in the HYD series, an electron donor group at the position increases and an electron at
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Fourth non canonical sites may be targeted Classical benzodi
2023-05-25
Fourth, non-canonical sites may be targeted. Classical benzodiazepines require the presence of a γ subunit for high-affinity binding, which limits their activity to a specific large pool of receptor isoforms, leaving other isoforms unaffected. In particular, δ subunit-containing receptors, as well a
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Several structural classes of ASK inhibitors
2023-05-25
Several structural GW9662 of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revealed
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br APJ expression in metabolic diseases Under physiological
2023-05-25
APJ expression in metabolic diseases Under physiological conditions, APJ is present in humans as well as in mouse tissues with high metabolic activity such as muscle and adipose tissue but not in the liver. Moreover, the presence and regulation of APJ in established adipocyte or muscle cell lines
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