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br Materials and methods br Results Metabolic stability
2021-08-12

Materials and methods Results Metabolic stability of compounds was studied by incubation with pooled human liver microsomes. Piperine was the metabolically most stable compound, with a t1/2 of 141min (Fig. 2, and Table 1). SCT-29 and LAU 397 showed t1/2 of approx. 45min, whereas a t1/2 of only
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Since free testosterone diffuses into a target organ
2021-08-12

Since free testosterone diffuses into a target organ [1], a remarkable increase in free testosterone in plasma is expected to enhance androgen response in target organs including the prostate. In fact, the results of the present study showed testosterone and DHT levels, and mRNA expression levels of
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Although it is believed that
2021-08-12

Although it is believed that CYP induction is regulated in humans in principle in the same fashion as in animals, some species differences in CYP3A enzymes induction were observed. Rifampicin is known to be a potent inducer of CYP3A4 in human hepatocytes, whereas pregnenolone-16α-carbonitrile (PCN)
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In conclusion adipose PGD suppressed the lipolysis by decrea
2021-08-11

In conclusion, adipose PGD2 suppressed the lipolysis by decreasing the intracellular cAMP level through DP2R. Therefore, PGD2 enhanced adipocyte differentiation (lipid accumulation) through both repression of the lipolysis via DP2R and activation of the lipogenesis via PPARγ. Thus, L-PGDS and DP2R a
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While showing that deletion of EP maintains
2021-08-11

While showing that deletion of EP1 maintains femur bone volume fraction and trabecular bone parameters during aging, perhaps more importantly we have also demonstrated that increased initial BV/TV in EP1 is protective against OVX-induced bone loss. That is, while mice lose an approximately equal pe
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Central to the mechanism of cold
2021-08-11

Central to the mechanism of cold I/R-associated liver injury is the activation of the pro-inflammatory cascade resulting in the release of pro-inflammatory cytokines. In agreement with the present study, serum and hepatic mRNA levels of TNF-α, IL-6, and ICAM-1 were all significantly up-regulated ear
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The generation of ROS in addition to eliciting oxidative
2021-08-11

The generation of ROS, in addition to eliciting oxidative stress, is an important proapoptotic signal (Ott et al., 2007). Apoptosis is clearly associated with the production of ROS, since ROS generation occurs in the mitochondrial respiratory chain and disturbs mitochondrial homeostasis, which plays
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br Experimental Procedures br Author Contributions br Acknow
2021-08-11

Experimental Procedures Author Contributions Acknowledgments Introduction Breast cancer is one of the most common malignancies for women worldwide, representing approximately 22% of women’s malignancies that pose a threat to women’s health [[1], [2], [3], [4]]. The morbidity rate of brea
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Collectively our results indicate that GSK A functions as a
2021-08-11

Collectively, our results indicate that GSK682753A functions as a competitive antagonist and binds to the receptor in the same region as 7α,25-OHC. First, we observe linearity in the Schild plot analysis (Fig. 2B). Second, GSK682753A is highly dependent on F111 at position III:08/3.32 in TM-III (Fig
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br Materials and methods br Results and discussion br
2021-08-11

Materials and methods Results and discussion Conflict of interest Acknowledgments This work was supported by grants from National 973 Project (2015CB755700) and the Doctoral Starting up Foundation of Henan University of Science and Technology (13480033). Introduction Progression thro
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br Regulation of p via the
2021-08-11

Regulation of p53 via the ubiquitin-proteasome pathway Studies into regulation of p53 via PTM processes that involve phosphorylation, acetylation, ubiquitination, SUMOylation, neddylation, and methylation are being increasingly reported [23], [24]. Phosphorylation and acetylation of p53 stimulate
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Taken together this study gives first insights
2021-08-11

Taken together, this study gives first insights into the complex effect of DNMT inhibition on pattern separation. Acute administration of RG108 enhanced pattern separation performance measured with the OPS task and increased Bdnf1 expression. However, this effect was only acute, and was not present
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Rifaximin Like compound substitution on compound contains am
2021-08-11

Like compound substitution on compound () contains amino and carboxamide groups attached to adjacent ring positions. These groups have similar interactions as compound with the protein backbone and Glu114. The triazole core is coordinated with Lys291. The triazole ring core π-stacks with Tyr226.
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LPA is known to regulate the
2021-08-11

LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a
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br Introduction Acylglycerol acyltransferases AGATs are
2021-08-11

Introduction Acylglycerol acyltransferases (AGATs) are predominantly responsible for triglyceride synthesis in the body, via two major pathways: the glycerol phosphate (GP) pathway (Kennedy, 1957) and the monoacylglycerol (MG) pathway (see Coleman and Lee, 2004, Yen et al., 2008). The final step
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