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Adenosine receptors activate a number of signalling pathways
2024-02-09
Adenosine receptors activate a number of signalling pathways involved in tissue survival including several mitogen-activated protein kinases (Fredholm et al., 2001). The common feature of all adenosine receptors is the positive coupling to ERK1/2, whilst A2B and A3 receptors can also activate the s
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An alternative to the agonist
2024-02-09
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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The structures of these compounds were confirmed
2024-02-09
The structures of these compounds were confirmed from their spectral and micro analytical data. Based on [M + H] 367, molecular formula of was established as CHON. The IR spectrum of showed glut 1 due to CO stretching at 1700 Cm & OH stretching at 3188 Cm indicating that compound contains one car
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Fencilli et al reported derivatives of PHA which demonstrate
2024-02-09
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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In liver the essential organ
2024-02-09
In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic lumiracoxib to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge betwee
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Mechanistically it was soon realized that in
2024-02-07
Mechanistically, it was soon realized that in undead cells, Dronc promotes the activation of Jun-N-terminal kinase (JNK) signaling as the major inducer of AiP [25], [28] (Fig. 2B,C). However, it has been unknown for a long time how active Dronc promotes JNK signaling. Recently, it was reported that
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In humans the superior safety profile of lipid associated fo
2024-02-07
In humans, the superior safety profile of lipid-associated formulations is characterized by decreased acute infusion-related reactions and dose-related nephrotoxicity, allowing the administration of larger doses and therefore similar efficacy with fewer administrations. In vitro studies and human cl
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Immunohistochemistry in tissue samples showed the
2024-02-07
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of Vidofludimus tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted i
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Detailed analysis of the dose dependence of A
2024-02-07
Detailed analysis of the dose dependence of Aβ effects revealed that at low amounts, Aβ can also act as a positive regulator of presynaptic activity, enhancing the neurotransmitter release probability and increasing the neuronal excitability [2]. The facilitator effects of low Aβ dose on excitatory
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To guide our attempts at achieving AKT potency and selectivi
2024-02-07
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AKT
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Last decade has provided a number of studies indicating
2024-02-07
Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider
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egfr inhibitor It is already established in the literature t
2024-02-06
It is already established in the literature that products synthesized by 5-LO, such as lipoxin A4, can activate PPARγ in a setting of experimental stroke [43]. Interestingly, experiments using 5-LO knockout mice in an endotoxemia model to mimic septic conditions, demonstrated reduced multiple organ
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purinergic receptors The LOX hydroxide metabolites are conve
2024-02-05
The 15-LOX hydroxide metabolites are converted to secondary lipid mediators such as lipoxin A4 from 15-HETE and protectin D1/resolvin D1 from 17-HDoHE [45] (Fig. S3). Importantly, all of these secondary lipid mediators have anti-inflammatory and pro-resolving properties [46], [47], [48]. Lipoxin A4
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Chromatin proteins play important roles in gene expression a
2024-02-05
Chromatin proteins play important roles in gene expression and DNA repair. The importance of chromatin composition on gene expression is exemplified by X-inactivation, where one of the two X chromosomes in female mammalian Saikosaponin A is transcriptionally silenced by heterochromatin , , , . In t
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br Introduction In the past two decades graphene
2024-02-05
Introduction In the past two decades, graphene and graphene based nanomaterials with unique physicochemical properties have attracted great attentions in many fields including biomedicine and biotechnology. Graphene oxide (GO) and its derivatives have shown promising potential as biological and c
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