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PHA-680632 To guide our attempts at achieving AKT potency
2023-03-20
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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The PAS domains of AHR consist
2023-03-20
The PAS domains of AHR consist of two regions, PAS-A and PAS-B, which function as interfaces for dimerization with ARNT and for ligand binding, respectively [14]. Although both the bHLH and the PAS-A domains have been shown to be involved in dimerization with ARNT, a recent report suggests that only
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The geometry of two three four and five acetylcholine neutra
2023-03-17
The geometry of two, three, four and five Epiberberine neutral radical ACh molecule complexes with various electronic configurations, i.e. with various multiplicities equal to 1, 2 and 4 (for ACh trimer) were determined using DFT with the unrestricted B97d/SVP potential/basis set in Gaussian09 progr
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It has been reported that leukotrienes and their
2023-03-17
It has been reported that leukotrienes and their receptors, e.g. the cysteinyl leukotriene receptor 1 (CysLT1) may promote angiotensin ii australia injury (Ding et al., 2007) and that increased 5-LOX expression and activity lead to production of brain-toxic molecules (Khan et al., 2010). However, di
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The ATX LPA signaling axis
2023-03-17
The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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br Concluding remarks Autophagy ensures cell
2023-03-17
Concluding remarks Autophagy ensures cell homeostasis and survival through the continuous degradation/recycling of intracellular components. It can also represent a conserved, cell-intrinsic, defense mechanism against invading pathogens, including viruses. The autophagy process can be activated r
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Elevated expression of Aurora A and
2023-03-17
Elevated expression of Aurora-A and -B frequently detected in a wide variety of human cancers strongly indicate that high expression of these kinases play roles in the development of cancer associated phenotypes. While Aurora-A has been shown to function as an oncogene when over expressed in mammali
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Three questions from the To test the compounds metabol
2023-03-17
To test the compounds metabolic stability, we measured the half-life of compounds and in mouse hepatic microsomes (1mg/mL) and found them to have modest stability, with half-lives of 7.5 and 2.9min respectively, indicating these compounds may be unsuitable for studies. In order to gain structural i
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br STAR Methods br AMPK A Therapeutic
2023-03-17
STAR★Methods AMPK: A Therapeutic Target in the β Cell? Loss of pancreatic β cell function is a hallmark of the transition to a diagnosis of T2DM (see Glossary) 1, 2, 3, 4. AMPK activation has gained attention for the treatment of hyperglycemia in prediabetes as an insulin-sensitizing agent bec
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Introduction Alzheimer s disease AD is a complex
2023-03-17
Introduction Alzheimer's disease (AD) is a complex neurological disorder characterized by a progressive dementia resulting from synapse failure (Selkoe, 2002, Tanzi, 2005). The amyloid hypothesis maintains that the pivotal event in AD is the production of amyloid-β (Aβ) peptides following the prote
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Cancer stem cells CSCs may have been
2023-03-17
Cancer stem cells (CSCs) may have been first identified in teratocarcinomas [11], [12], with its initial clues date back to the 19th century [13]. Kleinsmith and Pierce [12] established the immortal pluripotent teratocarcinoma lines from a single transplanted multi-potent malignant cell, strongly su
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The results also showed that the A receptor
2023-03-17
The results also showed that the A3 receptor agonist increased the phosphorylated levels of Akt, leading to activation of the PI3K/Akt pathway. A3 bicuculline receptor stimulation has protective effects against RGC death following ischemia-reperfusion, glutamate toxicity, and optic nerve transectio
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We aim to evaluate the
2023-03-17
We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of Torin1 injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are highly susceptibl
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Finally one can ask whether
2023-03-16
Finally, one can ask whether these results throw any light on the nature of the target in SNMG patients. Interestingly, the results of the in vitro incubations suggested that SNMG sera might increase AChR expression to a small extent, raising the possibility that SNMG patients, who have thymic chang
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br Conclusion br Conflicts of
2023-03-16
Conclusion Conflicts of Interest/Disclosures Acknowledgement This study was funded by the Ministry of Science of the Republic of Serbia (grant #175083). Introduction Myasthenia gravis (MG) is an antibody-mediated, neuromuscular transmission disorder, where the targets are postsynaptic p
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