• Binding affinity was measured by a scintillation proximity b

  2020-03-30

  

  Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six

• br Non cyclic nucleotide EPAC regulators Despite the

  2020-03-30

  

  Non-cyclic nucleotide EPAC regulators Despite the success of 007 as a tool molecule, few studies to date have led to the identification of further EPAC-selective agonists. The most studied and controversial group of small-molecule EPAC regulators are the sulfonylurea (SU) family. SUs (Table 1) su

• br CDK Inhibitors for the Treatment of

  2020-03-30

  

  CDK Inhibitors for the Treatment of inflammatory Diseases Several CDKs have been implicated as regulators of inflammatory gene expression. It will thus be very important to determine the relative contributions of the various CDKs and their kinase function on a systematic basis. This work will be

• Synthetic peptides have proven highly valuable in replicatin

  2020-03-30

  

  Synthetic peptides have proven highly valuable in replicating the characteristics of collagen and in defining the sites on collagen essential for binding and studying protein–collagen interactions. There are, however, disadvantages to synthetic collagen-like peptides. First, the thermal stability of

• Nile tilapia Oreochromis niloticus is

  2020-03-30

  

  Nile tilapia (Oreochromis niloticus) is an important species farmed worldwide (Doan et al., 2018). Lipid-rich diets are commonly used in Nile tilapia aquaculture to reduce feed cost, but impair lipid homeostasis (Huang et al., 2016). Therefore, it is important to determine whether forskolin can stim

• mimosine synthesis br Conflict of interest statement br

  2020-03-30

  

  Conflict of interest statement Acknowledgement The research leading to these results has received funding from the European Union Seventh Framework Programme (FP7/2007-2013) under grant agreement n° 278742 (Eurosarc) Introduction Pseudomyogenic hemangioendothelioma/epithelioid sarcoma-like

• When six chemical inhibitors were incubated

  2020-03-27

  

  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

• Intriguingly one E residue may serve

  2020-03-27

  

  Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In

• br As DAPK is dependent on Ca CaM

  2020-03-27

  

  As DAPK1 is dependent on Ca2+/CaM for its activity, its role in induction of autophagy is Ca2+-dependent and will be described in Section 5.1. LRRK1 and 2 were however shown to regulate autophagy in numerous studies where the role of Ca2+ was not investigated, and these mechanisms will be describe

• We have performed our MSP analyses as real

  2020-03-27

  

  We have performed our MSP analyses as real-time PCR using SybrGreen (Fig. 2). The results of the beta-actin PCR vary in each sample group because the amount of DNA for bisulfite treatment was adjusted to a constant volume of serum (500μl) rather than to equal amounts of DNA. Because we expected lowe

• Application of the CPH model relies on

  2020-03-27

  

  Application of the CPH model relies on the assumption that the hazard ratio of two observations is constant over time [2]. This enables us to infer the rate of risk of the treatment. For example, in the study of patients with pulmonary arterial hypertension (PAH) [5], the hazard ratio of a group of

• Although CK phosphorylated Msn as well as Msn Fig A

  2020-03-27

  

  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 Fmoc

• The crystal structure of full length CHK is still unsolved

  2020-03-27

  

  The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence a

• The in vitro enantioselective metabolism of

  2020-03-26

  

  The in vitro enantioselective metabolism of pesticides has been investigated by employing human liver microsomes, which are a reliable resource to perform MCL enantioselective risk assessment in humans (Carrão et al., 2019; de Albuquerque et al., 2018, 2016; Yao et al., 2016). The enantioselective m

• Mitophagy is a selective autophagic process which leads to

  2020-03-26

  

  Mitophagy is a selective autophagic process which leads to the degradation of damaged mitochondria in response to metabolic or environmental stress conditions. In this study, we found that LFS-01 treatment significantly enhances p62 in a time-dependent manner. We found that the upregulation of p62 i

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