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Immunohistochemistry in tissue samples showed the expression
2025-02-25
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of ion channels tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted i
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br Role of AMPK in inflammation signaling Pro
2025-02-25
Role of AMPK in inflammation signaling Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), activate Ikβ kinase (IKKβ), which phosphorylates IκBα, triggering the degradation of proteasomal IκB. This liberates active nuclear factor kB (NF-kB) to translocate i
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br Material and methods br Results br Discussion Aminopeptid
2025-02-25
Material and methods Results Discussion Aminopeptidase N is a transmembrane protease present in a wide variety of human tissues and cell types (endothelial, epithelial, fibroblast, leukocyte). APN expression is dysregulated in inflammatory diseases as well as in solid and hematologic tumors
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br Materials and methods br Results br Discussion We
2025-02-25
Materials and methods Results Discussion We have in this study used semi-nested degenerative PCR to identify the lipoxygenases expressed in the lung tissue from M. fascicularis and report on the identification of 5- and 12/15-LO transcripts from this tissue. Although we did not find transcr
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Gemcitabine Lorlatinib is an orally active brain penetrant c
2025-02-25
Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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The G R mutation is located
2025-02-25
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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In large biopsies series from ALK NSCLC treated
2025-02-25
In large biopsies series from ALK+ NSCLC treated patients, the number of detected mutations increased after second generation ALKi (Gainor et al., 2016) and in one study were present in 56% of the entire cohort (Shaw et al., 2013b). For example, the rate of G1202R mutations increases from 2% in post
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Similar to V the temporal neocortex of mammals including
2025-02-25
Similar to V1, the temporal neocortex of mammals, including the primary auditory cortex (A1), is densely innervated by 5-HT fibers originating mainly in the dorsal raphe nucleus (Campbell et al., 1987, Harding and Paxinos, 2004, Törk, 1990), and the major atomoxetine hcl of 5-HTRs are expressed thro
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br Perspectives and challenges Previously the main
2025-02-25
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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We further analyzed selected hit
2025-02-25
We further analyzed selected hit compounds for their ability to inhibit human AdK in intact cells. Human 1321N1 astrocytoma Agarose GPG/LMP low melt were utilized which were found to express AdK. The whole cell assay was performed using a 96-well format. The standard AdK inhibitor 5-iodotubercidin
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Cy5 water-soluble dye That disassembling actin filaments tra
2025-02-25
That disassembling Cy5 water-soluble dye filaments transport chromosomes towards the spindle in oocytes may be surprising at first sight. On the other hand, it is well established that chromosome movement during anaphase is driven by the depolymerization of microtubules [20]. It will be interesting
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Earlier studies revealed an interaction between
2025-02-25
Earlier studies revealed an interaction between HSP90β and ACK1 [15]. In the proteomic approach, we show that ACK1 associates with HSP90α and HSP90β. Additionally, we confirm the existence of a HSP90-ACK1 complex with co-IP experiments. We further analysed whether an inhibition of HSP90 affected the
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A high throughput small molecule
2025-02-25
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 Biocytin to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was per
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PC is considered as a cancer
2025-02-25
PC is considered as a cancer of the epigenome (Grasso et al., 2012, Robinson et al., 2015). Our results demonstrate that the interaction of AR with ACK1 drives the positive feedback epigenetic circuitry that is ultimately conducive to promote AR transcription. Further, this circuitry subjugates AR t
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br Colabeling evidence for ACh
2025-02-25
Colabeling evidence for ACh and GABA cotransmission Though functional demonstrations of ACh/GABA cotransmission remain largely limited to the retina and our recent analyses of cortex (Lee et al., 2010, Saunders et al., 2015a, Saunders et al., 2015b), evidence suggestive of ACh/GABA cotransmission