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A selected set of these
2025-01-07

A selected set of these new derivatives was then used for functional assays at the human A1AR showing, as expected, an antagonist profile with IC50 values at nanomolar level. The same molecules showed also to be efficacious as nanomolar antagonists in a functional assay aimed at analyzing their abil
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In an AP scenario several inflammatory mediators are produce
2025-01-07

In an AP scenario, several inflammatory mediators are produced locally to orchestrate an immune response. Eicosanoids are among those molecules and represent a class of lipid mediators synthesized from arachidonic 2'3'-cGAMP immune response through the action of cyclooxygenases or lipoxygenases to g
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The earliest appearance of tumors occurred at months
2025-01-06

The earliest appearance of tumors occurred at 12 months and the latest at 24 months, with an average onset at 18 months (Fig. 1B). This would be roughly equivalent to cancer presenting in a patient between 60 and 70 years of age. In transgenic animals, autotaxin Calcein AM was relatively increased
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Phagosomes acquire some hydrolases early during their journe
2025-01-06

Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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Further important evidence for G protein signaling on early
2025-01-06

Further important evidence for G protein signaling on early endosomes has been subsequently obtained for the β2-adrenegic receptor using fluorescently-tagged conformation-sensitive nanobodies selectively recognizing the active receptor and Gs protein [43]. More recently, our group used a combinatio
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Apoptosis signal regulating kinase ASK
2025-01-06

Apoptosis signal-regulating kinase 1 (ASK1, also referred to as MAP3K5)(Ichijo et al., 1997) participates in many different stress responses, including apoptosis (Chang et al., 1998, Chen et al., 1999, Ichijo et al., 1997, Kanamoto et al., 2000, Noguchi et al., 2008, Saitoh et al., 1998, Tobiume et
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Estrogen exerts its genomic action via estrogen nuclear rece
2025-01-06

Estrogen exerts its genomic action via H&E tissue staining nuclear receptor: ERα and ERβ. The distribution of ERα and/or ERβ positive neurons in CNS of different species has been mapped extensively by various methods [41], [42], [43], [44], [45], [46], [47], [48], [49], [50], although there are some
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The radiographic correlate will be similarly important for t
2025-01-06

The radiographic correlate will be similarly important for the success of other non-VEGF TKIs, such as those targeting the epidermal growth factor receptor expressed in 50% of high-grade primary GX-674 neoplasms. It has been reported that icotinib and gefitinib, epidermal growth factor receptor–TKI
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Therefore in the present study we first examined the ATRAP
2025-01-06

Therefore, in the present study, we first examined the ATRAP Herbal laxative in human leukocytes of healthy subjects. We next analyzed possible relevant clinical factors affecting ATRAP expression in leukocytes of patients with NCDs. Furthermore, we examined the possible effect of ATRAP downregulat
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Numerous studies have reported high glutamate levels in the
2025-01-04

Numerous studies have reported high glutamate levels in the brains of patients with depression, indicating that the glutamate system plays a crucial role in depression (Sanacora et al., 2004; Kendell et al., 2005; Hashimoto et al., 2007). Furthermore, several clinically effective antidepressant drug
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Oxidative stress has recently been reported
2025-01-04

Oxidative stress has recently been reported as one of the important mechanisms of toxic effect of Cd2+[43]. The mechanism of Cd2+-induced oxidative stress involves an imbalance between generation and removal of ROS in tissues and cellular components, causing damage to membranes, DNA, and proteins [4
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A high throughput small molecule ACK biochemical inhibition
2025-01-04

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 labetalol hydrochloride to be both ATP-competitive and reversible. Early structure-activity relationship (SA
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Introduction Dementia is a common disease in the elderly and
2025-01-04

Introduction Dementia is a common disease in the elderly, and a significant source of disability, healthcare spending, and long-term care admissions. There is evidence to suggest that testosterone plays a role in cognitive functioning, and lower serum levels correlate with higher amyloid deposits (
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The synthetic route to M developed by
2025-01-04

The synthetic route to M100907 developed by Rice was utilized, however, the chiral resolution was carried out at an earlier stage to provide the possibility of introducing different substituents onto the piperidinyl group. The conditions for this resolution were different from previously reported.
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br Aurora kinases br Wnt
2025-01-04

Aurora kinases Wnt signaling pathway The signal transduction pathway of Wnt/β-catenin signaling pathway plays an important role in embryogenesis to control cell differentiation and tumorigenesis [39]. A recent report indicates that 90% of colorectal cancer occur due to the activation of the Wn
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