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br Conclusions and perspectives In view of the evidences sup
2024-01-02
Conclusions and perspectives In view of the evidences supporting that Ecdysterone MAS receptors mediate the effects of AT1 antagonists (Iwai et al., 2012, Ohshima et al., 2014, Pernomian et al., 2015, Schuchard et al., 2015), the prime targets from the perspectives on future directions in the in
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Perhaps the first evidence of AMPKs
2024-01-02
Perhaps the first evidence of AMPKs therapeutic ability in DM1 came from Thomas Cooper’s laboratory where they demonstrated that insulin-independent glucose uptake was unaffected in human DM1 muscle AG-1024 treated with MET, an AMPK activator and first-line therapy for type 2 diabetes mellitus [76]
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First investigation of numerous membered
2024-01-02
First, investigation of numerous 12-14-membered ether-linked macrocycles revealed that smaller motifs were most lipophilic efficient. Compound (3) (12-membered macrocycle) exhibited good cellular potencies (ALK IC50 = 1.0 nM; ALK-L1196 M IC50 = 20 nM) and the highest LipE (4.4) with picomolar bindi
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In addition to plasma membrane sites OCT was also
2024-01-02
In addition to plasma membrane sites, OCT3 was also observed associated with endomembranes, including mitochondrial membranes, with particularly strong expression in the outer nuclear membranes of both neurons and astrocytes (Gasser et al., 2017), indicating that, in addition to regulating extracell
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Norepinephrine and epinephrine are catecholamines CA
2024-01-02
Norepinephrine and epinephrine are catecholamines (CA) released from synaptic nerves and the adrenal gland that mediate systemic responses to nutritional stressors (Cannon and De la Paz, 1911). CA mobilize plasma glucose by suppressing insulin secretion from the pancreatic β-cell (Katada and Ui, 198
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Napabucasin mg In summary the role of
2024-01-02
In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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br Introduction Epilepsy is characterized by spontaneous
2024-01-02
Introduction Epilepsy is characterized by spontaneous recurrent seizures and represents one of the most frequent neurological diseases affecting about 60 million people worldwide (McNamara, 1999). It is estimated that up to 50% of all cases are triggered by “initial precipitating injuries”, such
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Because LTs are proved to mediate multiple biological
2023-12-30
Because LTs are proved to mediate multiple biological and pathological responses in various disease states, the 5-LO biosynthetic pathway producing LTs from AA have been the target of drug discovery efforts for over two decades. As observed from literature, a pile of research efforts has been direct
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Drug resistance development often involves structurally un
2023-12-30
Drug resistance development often involves structurally un-related drugs and, specifically both conventional and targeted agents. IGROV-1/Pt1 Scriptaid are characterized by resistance to cisplatin and reduced sensitivity to inhibitors of EGF-R and MEK, the up-stream activator of ERK1/2, associated
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Docking studies were performed on the selected compounds to
2023-12-30
Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-83
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Ryoichi et al modified potent clinical candidate VX with cya
2023-12-30
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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br Conflicts of interest br Financial support This
2023-12-30
Conflicts of interest Financial support This work was supported by grants from the Fondazione Cariplo [Grant number 2011-0463] (Carini); and by Funds for Original Research of the Università del Piemonte Orientale (2016, Project: Carini-Boldorini). The sponsors had no involvement in study desig
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br Summary and future br Introduction Androgen
2023-12-29
Summary and future Introduction Androgen activity is critical for a wide range of developmental and physiological responses and is especially important in male sexual differentiation and maturation. The biological activity of androgens occurs through binding to the androgen receptor (AR) and t
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Kim et al found that hydroxydopamine OHDA
2023-12-29
Kim et al. (2013) found that 6-hydroxydopamine (6-OHDA) promoted the atrophy of dopaminergic neurons associated with the activation of poly (ADP-ribose) polymerase (PARP), the translocation of apoptosis inductor factor (AIF) and the depletion of ATP. An increase in p-AMPK and pS6K (upstream kinase o
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icilin The control group participants of the current study
2023-12-29
The control group participants of the current study were very similar in age to those of Puertas et al. There was no significant correlation between age and enzyme activity over the short age span studied although age-related changes in the activity of ApA and aspartyl aminopeptidase, typically incr
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