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AdK as an important upstream regulator of
2024-11-09
AdK as an important upstream regulator of adenosine-based homeostasis represents a promising drug target since it leads to an increase in adenosine concentrations. Taking into account that the adenosine formation is only increased in affected tissues under stress with high adenosine levels, AdK inhi
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In this study we make the first
2024-11-09
In this study, we make the first simultaneous recordings of MMP-2 Inhibitor II release in multiple brain regions at a temporal resolution less than 1 s. One of the most striking findings is that acetylcholine release has a remarkably similar temporal profile in the mPFC and dHPC, suggesting a coord
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Although effects of low concentrations of agonist
2024-11-09
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major KW-6002 α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acetylcholine-esterase-inhibiting
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The cellular mechanism underlying the CGS mediated inhibitio
2024-11-09
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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br Patients and Methods br Results br
2024-11-09
Patients and Methods Results Discussion Gjerdrum et al showed that Axl phosphocreatine is required to maintain the mesenchymal-like invasiveness of metastatic breast carcinoma cells, but Axl knockdown has no effect on the cell proliferation of MDA-MB-231 cells. Mackiewicz et al also showed
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br Involvement of LPA receptors in cancer
2024-11-09
Involvement of LPA receptors in cancer LPA׳s effects are mediated by at least six different G protein-coupled receptors (LPA1–6). Human gastric and ovarian cancers overexpress the mRNA encoding LPA1 and LPA2 compared to healthy tissues [6], [11], [12]. Papillary and follicular thyroid cancers exh
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Here we report discovery of highly
2024-11-09
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Miltefosine bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. T
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Because the V ATPase inhibitors that have been
2024-11-09
Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra
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Cerebral ischemia occurs following the
2024-11-09
Cerebral ischemia occurs following the occlusion of a cerebral artery by a thrombus and causes cell swelling due to cytotoxic edema and BBB disruption with vasogenic edema (Loreto and Reggio, 2010, Nakaji et al., 2006, Shibata et al., 2004). Vasogenic edema is directly linked to alteration of the BB
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Functional implications notwithstanding the intermolecular c
2024-11-09
Functional implications notwithstanding, the intermolecular contact appears to shield the Y361 side chain (Fig. 3) from being accessible for regulation by phosphorylation/dephosphorylation as has been proposed [18,19]. It is, therefore, likely that Src kinase and PTP1B phosphatase bind to an AROM mo
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Overall the expression of both components ligand
2024-11-09
Overall, the expression of both components (ligand and receptor) of the apelin signaling system allows for analysis of the direct role of apelin in CL function, and specifically P4 production. Although the CL secretes many different hormones, P4 is of predominant importance because it is necessary f
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Recent retrospective cohort studies have supported these pre
2024-11-08
Recent retrospective cohort studies have supported these preclinical findings in animals indicating the correlation of AR activation with the induction of HBC carcinogenesis. First, men with prostate cancer who underwent androgen deprivation therapy were shown to have a significantly lower risk of
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We start with a basic description of the
2024-11-08
We start with a basic description of the MT-SGL model. Consider a multi-task learning (MTL) setting with k tasks. Let p be the number of covariates, shared across all the tasks, and n be the number of samples. Let denote the matrix of covariates, be the matrix of responses with each row correspondin
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Neural progenitor cells NPCs are self renewing multipotent
2024-11-08
Neural progenitor cells (NPCs) are self-renewing, multipotent cells that are capable of differentiating into neurons, astrocytes and oligodendrocytes. NPCs are activated in response to a variety of pathological states in neurodegenerative diseases such as Parkinson’s disease and multiple sclerosis,
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gw research ltd synthesis In the late s Solvay Pharmaceutica
2024-11-08
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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