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CYP A is involved in the metabolism of approximately
2020-12-17

CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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Testosterone is inactivated through hydroxylation and conjug
2020-12-17

Testosterone is inactivated through hydroxylation and conjugation pathways [3], [4]. 6β-Hydroxylation is the main pathway among testosterone hydroxylation processes in the liver microsome. Testosterone 6β-hydroxylation is mainly catalyzed by cytochrome P450 3A (CYP3A) [5], [6], which is expressed in
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Allele specific methylation has been observed in CpG
2020-12-17

Allele-specific methylation has been observed in CpG islands of imprinted genes.27, 32 In the present study, however, methylation of CpG1 was specific to ALL carboxypeptidase and occurred in the leukemia cells of 28% of children with ALL, but it was not found in normal leukocytes from the same patie
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T helper Th cells play
2020-12-17

T helper (Th) Lovastatin play a central role in activation of immune system against infectious agents through secretion of lymphokines or cytokines. African trypanosomes target the Th cells and alter their activation, possibly for their own survival and perpetuity (Namangala, 2011). Trypanosoma bru
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In this report we established
2020-12-17

In this report, we established mouse models suitable for human retinal cell transplantation by introducing phosphodiesterase 6B (Pde6b) mutant allele from retinal degeneration (rd) mouse models into NOG background. Pde6b (rd1) and Pde6b (rd10) mice are well-studied and frequently used animal models
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The development and activation of
2020-12-17

The development and activation of T MRS1523 play an important role in the progression of atherosclerosis. As for activation and differentiation of T cells, TCR signalling pathway is pivotal. ZAP70 plays a crucial role in formulation of TCR–microclusters, initiation of TCR signalling pathway, moreov
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Given the molecular pharmacology and in
2020-12-17

Given the molecular pharmacology and in vitro metabolism data, we proceeded to evaluate the in vivo pharmacokinetics of . Mice (=3) were subsequently administered a subcutaneous dose (5mg/kg) with intermittent plasma collections to measure systemic levels of (). Compound achieved a maximum plasma co
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When six chemical inhibitors were incubated with TRB
2020-12-17

When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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br Author contribution br Acknowledgements We want to thank
2020-12-16

Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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Ubiquitin activating enzyme activates ubiquitin by a
2020-12-16

Ubiquitin-activating enzyme activates ubiquitin by a three-step process with ATP as a cofactor (Chen et al., 2011, Haas and Rose, 1982, Haas et al., 1982). We demonstrated that ATP is required for mRFP-Ub–E1 formation under non-reducing conditions (Fig. 2A). A time course of radioactive ATP producti
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br Introduction Although not fully understood the molecular
2020-12-16

Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen
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We elucidated that the ten
2020-12-16

We elucidated that the ten DGK isozymes have different relative 1-MGK and 2-MGK activities vs DGK activity under the same conditions. However, because the octylglucoside-mixed micellar assay was developed for DGK, it is not known whether the DGKs exhibit maximum 1-MGK and 2-MGK activities in this as
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br Biological roles of DGK br Summary
2020-12-16

Biological roles of DGKϵ Summary and future perspectives The most 2 types of active transport segment of DGKϵ, comprised of residues 20–42, appears to have no role in binding the lipid substrate DAG or in the acyl chain specificity of substrate phosphorylation. Nevertheless, the sequence in t
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The molecular docking data supported the
2020-12-16

The molecular docking data supported the potential interaction of lapachol and the synthetic naphthoquinonolyl compounds with the PfDHODH enzyme as the putative mechanism of action and the inhibition of parasite growth in vitro. In general, compounds fit well into the binding pocket of PfDHODH, the
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Pyocyanin br Conclusions In Summary a multilayer
2020-12-16

Conclusions In Summary, a multilayer screening of xanthones of natural origin (Xanthone-NPs) was undertaken against Pf-DHFR. The Re-rank score of screened compounds was size normalized and interaction profile was generated using experimentally known inhibitors. Three compounds X5, X113A and X164B
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