• In contrast to SQLE HMGCR could be

  2020-06-16

  

  In contrast to SQLE, HMGCR could be efficiently degraded in Ki16198 lacking UBE2J2. However, this was not the case in cells devoid of UBE2G2, as these cells were unable to support 25-hydroxycholesterol (25-HC)-stimulated degradation of HMGCR (Fig. 1C). This finding is consistent with our recently re

• Covalent inhibitors are well suited for

  2020-06-16

  

  Covalent inhibitors are well suited for targeting the E1 mps1 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circulation

• Ubiquitin activating enzyme activates ubiquitin by a three s

  2020-06-16

  

  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

• br Are incretins the only mediators of the anti

  2020-06-16

  

  Are incretins the only mediators of the anti-hyperglycaemic effects of DPP-4 inhibitors? Even though both GLP-1 and GIP were identified as substrates for DPP-4 early on [17], [19], [20], [22], and DPP-4 inhibition in vivo raises levels of the intact endogenous forms of both of them [43], [44], fr

• br Conclusion br Competing interests br Authors contribution

  2020-06-16

  

  Conclusion Competing interests Authors\' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number

• br Acknowledgements br Introduction Lung

  2020-06-16

  

  Acknowledgements Introduction Lung cancer treatment strategies, especially molecular targeted therapy, have progressed rapidly. However, most established treatments are for adenocarcinoma of the lung, not for squamous cell carcinoma (SQCC). SQCC constitutes approximately 30% of lung cancers, w

• Recently Schenck et al identified

  2020-06-16

  

  Recently, Schenck et al. [25] identified an active site asparagine 222 (N222) residue in the Glycine max TyrAp/PDH (GmPDH1) that is responsible for its prephenate substrate specificity. Mutating the single N222 into an acidic residue (i.e. aspartate, D) in the legume TyrAp/PDH shifted from prephenat

• Our western blotting results showed

  2020-06-16

  

  Our western blotting results showed that phospho-DDR1 levels continued to increase after I/R injury, and the overall activation trend between phospho-DDR1 and MMP-9 was the same. We found that phospho-DDR1 expression started to increase significantly at 12h after I/R injury, which may be related to

• thiostrepton Although it is believed that CYP

  2020-06-16

  

  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)

• The notion that a small subset of inducible cellular transcr

  2020-06-16

  

  The notion that a small subset of inducible cellular transcripts, encoding immunological important factors, is translocated across the nuclear envelope by the karyopherin CRM1 is gaining support from various recent studies. For example, experimental evidence has been provided demonstrating that the

• Previously published results on this topic are inconsistent

  2020-06-16

  

  Previously published results on this topic are inconsistent. Stressin1-A, a novel CRF1 receptor agonist, increased anxiety-like behavior in the social interaction and shock-probe tests [51]. Pharmacological blockade of CRF1 (NBI-30775) reversed both CRF-induced increases in startle and CRF-induced d

• Autophagy is a dynamic process that primarily

  2020-06-16

  

  Autophagy is a dynamic process that primarily involves autophagosome formatting and lysosomal degradation, and these processes are controlled by autophagy-related genes (Atg) (Klionsky et al., 2012). The related protein SQSTM1/p62 (sequestosome 1) importantly serves as a signalling director in sever

• Recent pharmacological and clinical studies suggested that e

  2020-06-16

  

  Recent pharmacological and clinical studies suggested that estetrol (E4) should also be considered as an interesting candidate for MHT (Abot et al., 2014; Mawet et al., 2015). E4 is naturally produced from E2 and estriol (E3) via 15α- and 16α-hydroxylase by the human fetal liver during pregnancy and

• The activity of cysteine endopeptidases

  2020-06-15

  

  The activity of cysteine endopeptidases involved in the germination of caryopses is generally regulated at two levels: the hormonal induction of synthesis by gibberellins (Drzymała et al., 2008) and a putative regulation of activity by phytocystatines (Kiyosaki et al., 2007, Martinez et al., 2009),

• br Introduction The ubiquitination status of a target protei

  2020-06-15

  

  Introduction The ubiquitination status of a target protein is achieved via a delicate balance between two opposing forces: ubiquitin E3 ligases and DUBs. It has been postulated that the majority of proteins in a cell are regulated and modified by ubiquitin at some point (Hershko and Ciechanover,

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