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Screening a selection of analogues
2024-10-31
Screening a selection of analogues from this library against the panel of 26 kinases (16, 22, and 24 were screened at 30 μM due to poor solubility; 17 tested at 100 μM) generally demonstrated an increase in activity compared to QX 314 chloride 3 (Fig. 3, Fig. 6). The benzamide analogue 16 demonstrat
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Aminoglutethimide first generation aromatase inhibitor
2024-10-30
Aminoglutethimide, first generation aromatase inhibitor, has been tried as an antiepileptic drug in combination with other standard drugs (Aguilar et al., 1961). Letrozole is a third generation reversible non-steroidal aromatase inhibitor, approved by US-FDA, for the treatment of postmenopausal wome
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Despite these conflicting data about COX
2024-10-30
Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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AP plays a pivotal role in transcriptional
2024-10-30
AP-1 plays a pivotal role in transcriptional regulation of MMP expression. The decoy technique allows the neutralization of AP-1 without any transfection reagents for cellular uptake that cause potential side effects or immune reactions. This energy-dependent transport mechanism of “naked” dODN is c
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First the complete canonical brain original RAS Angiotensino
2024-10-30
First, the complete canonical brain original RAS (Angiotensinogen, Renin, Angiotensin I, Angiotensin Converting Enzyme (ACE), Angiotensin II) has not been conclusively identified in any specific cell type within the brain [1]. Validated evidence for the presence of brain Angiotensinogen and ACE was
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Introduction Cardiovascular disease is the principal cause o
2024-10-30
Introduction Cardiovascular disease is the principal cause of morbidity and mortality in patients with elvitegravir receptor (1). Comprehensive management of these patients includes not only adequate glycemic control but also attention to additional recognized risk factors. Hypertension is a cardi
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MD was the recipient of the Intergroupe
2024-10-30
MD was the recipient of the Intergroupe Francophone de Cancérologie Thoracique (IFCT) Alain Depierre Grant in 2014. JP was the recipient of the ARISTOT (Association de Recherche, d’Information Scientifique et Thérapeutique en Oncologie Thoracique) grant in 2016. Conflicts of interest statement
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A rate limiting step in the generation of
2024-10-30
A rate-limiting step in the generation of kynurenine and xanthurenic Carprofen is the oxidation of N-formyl-kynurenine to l-kynurenine via indolamine 2,3-dioxygenase (IDO) or tryptophan dioxygenase (TDO). IDO and/or TDO knockdown decreases and ectopic over-expression increases production of endogen
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br AHR expression in cancer Perhaps the
2024-10-30
AHR expression in cancer Perhaps the earliest indicator that the AHR might play an ongoing role in tumorigenesis, independent of its role in generating mutations, was the demonstration that non-genotoxic 2,3,7,8-tetrachlorodibenzo(p)dioxin (TCDD) is a carcinogen in animals and humans [7]. Althoug
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However there are a lot of
2024-10-30
However, there are a lot of external magnetic field disturbances in urban environments, for example when the AHRS is close to a ferrous or magnetic object, which will disturb the output of magnetometer, then the observational errors cannot satisfy the assumption of Kalman filtering, and so, the atti
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br ABCA and cancer drug response Overall the expression of
2024-10-30
ABCA2 and cancer drug response Overall, the expression of ABC transporters has been linked with multidrug resistance phenotypes through the efflux of drugs via ATP-dependent transport. For example, 13 distinct transporters (ABCA2, ABCB1, ABCB4, ABCB11, ABCC1–6 ABCC10, ABCC11 and ABCG2) have been
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Two cell surface trans membrane receptors have been
2024-10-30
Two cell-surface trans-membrane receptors have been identified for adiponectin, AdipoR1 and AdipoR2 [21], and adiponectin action is known to signal through these receptors and the docking protein APPL1 [22]. In muscle and liver cells, signal transduction involves the phosphorylation and activation o
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[Ala107]-MBP (104-118) br Adenosine receptors and the adapti
2024-10-30
Adenosine receptors and the adaptive immunity T lymphocytes are responsible for the cell-mediated immune response [95]. These cells can be stimulated by the presentation of antigenic moieties by APCs, such as dendritic cells or macrophages [96]. The presentation of antigenic molecules on the APC
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Phosphodiesterase inhibition increases the intracellular lev
2024-10-30
Phosphodiesterase inhibition increases the intracellular levels of cAMP to restore spontaneous contraction (Essayan, 2001, Qi and Kwan, 1996), acting downstream of adenylyl cyclase. Therefore, cardiac arrest induced by decreased intracellular cAMP levels could be reversed by phosphodiesterase inhibi
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Metformin s pluripotent roles are alluded to in terms of
2024-10-30
Metformin's pluripotent roles are alluded to in terms of its antitumorigenic, glucose-lowering, and cardioprotective effects, which are due in part to its upregulation of AMPK activity [39,40]. Metformin's glucose-lowering effect is a result of reduced hepatic gluconeogenesis, whereas improved insul
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