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br Results br Discussion Many tumor cells
2023-12-06
Results Discussion Many tumor BVT 2733 rely on EAAs to provide fundamental building blocks for macromolecular biosynthesis because they cannot synthesize EAAs de novo (Hattori et al., 2017; Sheen et al., 2011). Therefore, they must use highly effective transporters to maximize EAA uptake from
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In contrast to the beneficial treatment of skin inflammation
2023-12-06
In contrast to the beneficial treatment of skin-inflammation with PAH containing coal tar, epidemiology showed that environmental pollution, containing AHR-activating PAH, lead to more eczema [80]. Of note, other epidemiological data suggested that Th17 cell polarization may be enhanced air pollutio
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The central problem in amnesia developing following impairme
2023-12-06
The central problem in amnesia developing following impairment of long-term memory consolidation or reconsolidation is a question of the underlying mechanisms, whether it is caused by impairment of retrieval or memory storage mechanisms [3,8,9,[15], [16], [17], [18]]. To answer this question, severa
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AVE-1625 In previous research we determined that blocking mA
2023-12-06
In previous research, we determined that blocking mAC during heparin-induced capacitation result in sperm having a lesser oxygen consumption, suggesting that cAMP produced by this enzyme would be linked to mitochondrial activity and, therefore, with the regulation of sperm metabolism (Fernández and
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Interestingly as observed with Treg cells adenosine can regu
2023-12-06
Interestingly, as observed with Treg cells, adenosine can regulate the function of Breg cells, a subset of immunosuppressive cells that support immunological tolerance [115]. In particular, Bregs were able to regulate both their own function and T cell activity via an adenosine signaling originating
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In the late s Solvay Pharmaceuticals discontinued the Phase
2023-12-06
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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Toxicity is the main reason for the failure
2023-12-06
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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Vortioxetine is a multimodal antidepressant that acts as an
2023-12-06
Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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Whereas more research is needed to identify the precise
2023-12-06
Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the Swainsonine that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reversed the be
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The benzimidazole group seems to
2023-12-06
The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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Introduction Aldose reductase ALR is the first enzyme of
2023-12-05
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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An important observation in our study is the
2023-12-05
An important observation in our study is the lack of effect of paroxetine pretreatment alone on β2AR membrane expression, which suggests that paroxetine, and pharmacologic inhibition of GRK2 in general, does not directly induce changes in receptor dynamics. Rather, the decreased ligand-induced β-arr
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br Materials and methods br Results The
2023-12-05
Materials and methods Results The average body weights for each group of mice over the course of the study are shown in Fig. 2A. The average body weights of the mice in the saline control group and PACAP group increased slightly during the study. In contrast, starting at day 17, the body weigh
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br Conclusions and clinical relevance Astrogliosis and an in
2023-12-05
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic W146 is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of A1R agonists or ADK inhibitor
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The cytoplasmic domain of muscle
2023-12-05
The cytoplasmic domain of muscle AChR is not accessible to GSK2879552 australia in vivo. Theoretically, therapy with the cytoplasmic domains should be safe. Safety is demonstrated by the facts that: (1) rats repeatedly immunized with the cytoplasmic domains in TiterMax adjuvant do not develop EAMG,
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