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The biology of the A BR is complex and
2024-05-13
The biology of the A2BR is complex and needs to be considered contextually as the expression and effect of receptor engagement varies according to time post hypoxic injury, cell type and downstream signaling pathway. For example, A2BR expression is dynamic - low under basal and increasing under isch
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Although the mechanisms of APP secretion are well characteri
2024-05-13
Although the mechanisms of APP secretion are well characterised (for review see Ref. [1]), production of soluble AChE species is less well understood although we have reported that a metalloproteinase can shed AChE similarly to APP [16], [17]. Recently it has also been demonstrated that cellular pre
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IC values were obtained for an expanded version of
2024-05-13
IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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br Results and discussion br Conclusion A series of
2024-05-13
Results and discussion Conclusion A series of aminobenzothiazole derivatives were investigated as possible Aurora B kinase inhibitors. Bioisosteric replacement of the heterocyclic core of the lead compound was performed regarding the docking analysis. Replacement of the oxygen (-)-epicatechin
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Previous investigations have established that aromatase
2024-05-11
Previous investigations have established that aromatase activity is regulated via two different pathways in a tissue-specific manner. The first is a slower transcription regulatory pathway that involves an alteration in gene transcription and represents what is classically thought of as the way by w
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Introduction Cytochrome P CYP aromatase catalyzes the
2024-05-11
Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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br Material and methods br Results
2024-05-11
Material and methods Results Discussion The present study demonstrates for the first time that Mino selectively induces apoptosis in Jurkat Exemestane via an H2O2 signaling-dependent mechanism. Structurally, Mino is composed of a C10 and C12 phenol group, C12a hydroxyl group, and C1 and C1
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Protein arrays provide a new approach for the
2024-05-11
Protein arrays provide a new approach for the identification of substrates for several protein-modifying enzymes. For example, protein kinase substrate identification, which constitutes an important aspect of pathway mapping because of the prevalence of these substrates in biological pathways. MacB
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Finally terbinafine is generally associated with a low index
2024-05-11
Finally, terbinafine is generally associated with a low index of toxicity and few adverse effects. In humans, only mild GI toxicity and hepatobiliary dysfunction are reported. In red-tailed hawks, oral administration of a high dose of terbinafine (120 mg/kg BW) was furthermore demonstrated to induce
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The radiographic correlate will be similarly
2024-05-11
The radiographic correlate will be similarly important for the success of other non-VEGF TKIs, such as those targeting the epidermal growth factor receptor expressed in 50% of high-grade primary 5-Azacytidine neoplasms. It has been reported that icotinib and gefitinib, epidermal growth factor recep
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br Concluding Remarks Despite major advances in the
2024-05-11
Concluding Remarks Despite major advances in the development of antibody and small-molecule tumor angiogenesis inhibitors, therapy resistance, both innate and acquired, continues to limit further survival improvements for patients with cancer. Preclinical models of localized primary tumors and me
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Recent retrospective cohort studies have supported
2024-05-11
Recent retrospective cohort studies have supported these preclinical findings in animals indicating the correlation of AR activation with the induction of lipid metabolism pathway carcinogenesis. First, men with prostate cancer who underwent androgen deprivation therapy were shown to have a signific
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Although it is not known if
2024-05-11
Although it is not known if CP-AMPAR regulation is required for LTD, our previous characterization of AKAP150ΔPIX knockin mice that are selectively deficient in CaN anchoring, due to disruption of a PxIxIT-type CaN docking motif, provided important insights. We found that AKAP-CaN signaling dephosph
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Recently two distinct small molecule
2024-05-11
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Vicriviroc Malate receptor with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, r
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br Conclusion br Introduction The
2024-05-11
Conclusion Introduction The identification of Alzheimer's disease (AD) biomarkers and their ability to measure pathology antemortem has led to a fundamental reconsideration of the pathogenesis of AD. The importance of biomarkers was already reflected in revised diagnostic criteria proposed by
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