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While the direct effects of ARI lead to a dramatic
2022-12-12
While the direct effects of 5-ARI lead to a dramatic PYR-41 mg in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laboratory range
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In our studies of leucine
2022-12-12
In our studies of leucine and BCH in pancreatic islets and clonal insulin cell lines, we noticed that leucine was a slightly stronger stimulant of insulin release. Previous studies showed that leucine can be metabolized to CO2[11], [12], [13], [14] and can increase acetoacetate in pancreatic islets
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How does the ATM to
2022-12-12
How does the ATM-to-ATR switch occur at DSBs? The progressive attenuation of ATM activation could be attributed to the loss of DNA structures that activate ATM, or to the generation of DNA structures that interfere with ATM activation. Our finding that SSOs do not directly affect the binding of puri
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br Author contributions br Acknowledgments TJC KW and
2022-12-12
Author contributions Acknowledgments TJC, KW, and VG are supported by awards made to MJN: a Consolidator Grant from the European Research Council under Grant no. 311336; a University Research Fellowship from the Royal Society, and a Career Development Award from the Human Frontiers Science Pro
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Arginase deficiency is a rare urea cycle
2022-12-12
Arginase deficiency is a rare urea cycle disorder with hyperargininemia and profound neurological impairment as hallmark features. Arginase-1-deficient mouse models have been created, and they exhibit a profound lethal phenotype approximately 2 weeks after birth in the global knockout (KO) mice or a
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Here we found that AMPK directly phosphorylates
2022-12-12
Here we found that AMPK directly phosphorylates EZH2 at Thr311 to disrupt its interaction with SUZ12 and to inhibit PRC2 enzymatic activity, which is supported by the increased expression of PRC2-repressed genes. Furthermore, the T311E-EZH2 mutant that mimics AMPK-mediated phosphorylation status sup
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In this report we introduce a new
2022-12-12
In this report, we introduce a new method for identifying aminopeptidases. Because single substrates can be insufficient for enzyme identification, we used an entire library of substrates to obtain more information about enzyme activity and to directly detect aminopeptidases. Moreover, substrates ca
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Lorlatinib is an orally active brain penetrant cyclic aminop
2022-12-12
Lorlatinib is an orally active brain penetrant cyclic 2-aminopyridine derivative that is a type I½ B ALK inhibitor (Fig. 5F) [61]. This medicinal is an effective antagonist against the more common L1196M and G1269A crizotinib-resistant mutations as well as the less common T1151Ins, L1152R, C1156Y, F
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br Introduction The traditional Chinese medicine TCM Ganoder
2022-12-12
Introduction The traditional Chinese medicine (TCM), Ganoderma (G.) lucidum Karst is a well-known mushroom which has been used clinically in some Asian countries. It is termed “Lingzhi” in China, “Reishi” in Japan and “Yeongji” in Korea. It has long been used in TCM for the promotion of longevity
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Pregnane X receptor PXR is a
2022-12-12
Pregnane X receptor (PXR) is a nuclear receptor that plays an important role in regulation of metabolism and disposition of structurally diverse xenobiotics as well as endogenous steroids and bile acids (Bertilsson et al., 1998, Kliewer et al., 1998, Lehmann et al., 1998). PXR regulates the metaboli
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The rank order of agonist potency in turkey cardiac
2022-12-12
The rank order of agonist potency in turkey cardiac chambers demonstrated the predominant presence of the β-adrenergic receptor subtype, in line with the receptor classification by . However, a previous radioligand binding study in the left ventricles of 7-week old turkeys reported the existence of
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NLX a k a F or befiradol
2022-12-12
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in LBH589 synthesis to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally,
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AMPK is an essential player in
2022-12-12
AMPK is an essential player in adiponectin signaling pathway that regulates energy metabolism. The fact that suppression of AMPK activity by compound C largely diminished candesartan-mediated inhibition of NFκB via blocking AT1 also suggests that the AT1-mediated effect is at least partly resulted f
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br Experimental procedure br Funding The present study was s
2022-12-12
Experimental procedure Funding The present study was supported by the Grant Russian Foundation for basic research (project no. 16-04-01517). Introduction 5-HT, a monoaminergic neurotransmitter, is synthesised from l-tryptophan catalysed by the enzymes tryptophan hydroxylase (Tph) and aroma
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Structure activity relationships biochemical metabolic and m
2022-12-12
Structure–activity relationships [23], [24], [25], [26], biochemical [24], [25], [26], [27], [28], [29], [30], [31], metabolic [19], [27], [28], [29], [30], [31], and molecular [32] investigations have demonstrated that the substrate specificity, as well as other characteristics of T. gondii adenosi
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