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In some cases more than one CYP enzyme
2020-09-25

In some cases, more than one CYP450 enzyme may be involved in the metabolism of a drug, and an Eadie–Hofstee plot is usually more reliable for assessing the involvement of multiple Aurora Kinase Inhibitor III (Bu, 2006). Therefore, we first plotted the Eadie–Hofstee curves and observed their shape t
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HOIP s ability to build linear
2020-09-25

HOIP\'s ability to build linear Ub chains arises from a unique domain that follows directly after the RING2 domain, the linear ubiquitin chain-determining domain (LDD) (Fig. 1). Structures have revealed that the LDD is structurally integrated into RING2, creating a single RING2–LDD unit (Fig. 2D) [4
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br Discussion The regulation of intracellular
2020-09-25

Discussion The regulation of intracellular cholesterol levels is a biological process of vital importance for cellular function and integrity, and involves robust transcriptional and post-transcriptional mechanisms that are sensitive to metabolic feedback control. Amongst post-transcriptional mec
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In conclusion adipose PGD suppressed
2020-09-24

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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The results of bisaryl ether
2020-09-24

The results of bisaryl ether linker study are shown in . It was found that the methylene linker () moderately improved the binding to the DP receptor. The increased binding potency was also diminished in the presence of plasma, possibly due to higher plasma protein binding. Other linkers, such as th
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In the preclinical evaluation of CRF
2020-09-24

In the preclinical evaluation of CRF1 receptor antagonists, effects were mainly focused on the regulation of hyperactivated HPA axis and the modulation of anxiety or depressive-like behaviors in CRF challenge [16], [17], [18] or stress models [16], [19], [20]. However, it remains to be concluded whe
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Although many neurotransmitters e g catecholamines serotonin
2020-09-24

Although many neurotransmitters (e.g., catecholamines, serotonin, and excitatory/inhibitory amino acids) have been implicated in the modulation of anxiety-like responses (Carobrez et al., 2001, Molchanov and Guimaraes, 2002, Vianna et al., 2001), the so-called atypical neurotransmitters, endocannabi
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The COMT gene maps to
2020-09-24

The COMT gene maps to chromosome 22q11.2 (Grossman et al., 1992) and has two protein isoforms. The differences between S-COMT and longer MB-COMT are in the N-termini, which use alternative translation initiation sites and promoters. These two isoforms display different affinity and capacity for COMT
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Although CK phosphorylated Msn as well
2020-09-24

Although CK2 phosphorylated Msn4 as well as Msn2 (Fig. 1A), the two CK2-dependent phosphorylation sites in Msn2 are not conserved in Msn4. Thus, Msn2 and Msn4 might be differently regulated by CK2-dependent phosphorylation. Msn2 and Msn4, which have 41% identity and similarity in size and amino chlo
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In the present study cells were exposed to
2020-09-24

In the present study, cells were exposed to a low level of arsenite and a low cytotoxic concentration of BaP. Thus, γ-H2AX loss correlated with repair of DNA damage in cells co-exposed to arsenite and BaP. These results show that arsenite inhibits repair of BaP-induced DNA damage. In a previous stud
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Case report The patient was
2020-09-23

Case report The patient was referred to the oral and maxillofacial department at the authors’ institution for further evaluation and treatment. The patient underwent tumor resection with left hemi-mandibulectomy with wide bony margins (Fig. 1A), and mandible reconstruction with fibula free flap and
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The third challenge is to understand the mechanisms
2020-09-23

The third challenge is to understand the mechanisms of drug resistance. There are several different mechanisms of ES tumor to develop drug resistance. First, cancer stem cells are capable of proliferate and generate tumor cells with new sets of mutations which may harbor different protein targets [1
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Metal ions are known not to be necessary
2020-09-23

Metal ions are known not to be necessary for catalytic activity of serine proteinases. Nevertheless, Co2+ and Ca2+ ions were found to stabilize glutamyl endopeptidase molecule [1], [7], [19]. In our previous study, we have described significant stimulating effect of Ca2+, Mg2+, and Co2+ on biosynthe
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Radicicol The development of C S mutation
2020-09-23

The development of C797S mutation has been reported in vivo in a small cohort (15 subjects) of EGFR T790M positive patients progressing after Osimertinib: this tertiary mutation was found, using a droplet digital PCR (ddPCR) assay, in 40% of patients after AR to this agent, while 33% of the cases ex
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Doxorubicin HCl An increasing body of evidence
2020-09-22

An increasing body of evidence demonstrates that MXC can cause neurobehavioral and neuropathological alterations [7]. In the brain, there are several steroidogenic enzymes, which are responsible for neurosteroid production. Neurosteroids are subsets of steroids that rapidly change neuronal excitabil
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