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Many PIM inhibitors have been reported
2020-03-16

Many PIM inhibitors have been reported to date [7], [8], [9] however, none of them has been marketed so far. SGI-1776 is a representative first-generation PIM inhibitor, which had been under clinical trials for leukemia and prostate cancer [10]. While most of the first-generation PIM inhibitors are
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Several TERRA binding proteins have also been
2020-03-16

Several TERRA-binding proteins have also been discovered, especially telomeric duplex DNA binding proteins TRF1 and TRF2, pointing to a significant role of TERRA in more general chromosome biology [14], [20], [21]. TRF2 is a key component of Shelterin that protect chromosome termini [22]. Telomeres
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Other studies have investigated the role of HDAC inhibitors
2020-03-16

Other studies have investigated the role of HDAC inhibitors in particular signaling pathways mediated by EWS–FLI1 (Matsumoto et al., 2001). A recent investigation, showed a physical association of EWS–FLI1 and HDAC1 that helps mediate a disruption in the p53 activation of downstream targets (Li et a
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Pridinol Methanesulfonate br Results and discussion br Concl
2020-03-16

Results and discussion Conclusions In conclusion, we have developed rational strategies that allowed us to successfully identify a series of novel analogs structurally related to to modulate the activity of estrogen-related receptors (ERRγ and ERRβ), which are constitutively active. All of th
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An Ubl modification requires several steps that are catalyze
2020-03-16

An Ubl modification requires several steps that are catalyzed by three enzymes, referred to as E1 (activating enzyme), E2 (conjugation enzyme), and E3 (ligase). The SUMO E1 is a heterodimer of SAE1 and Uba2 (also known as SAE2). In brief, an Ubl is first activated by E1 through ATP hydrolysis and fo
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For immobilization of enzymes natural polymers depict severa
2020-03-16

For immobilization of enzymes, natural polymers depict several outstanding features as support. These materials are inert, non-toxic, biodegradable and biocompatible. As well as, they can be treated with different functional groups easily by chemical reactions that occur under gentle conditions in a
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Nrf and HO are key factors in the regulation
2020-03-16

Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin
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MK-8745 br Materials and methods br Results and
2020-03-16

Materials and methods Results and discussion Conclusions Codon-optimized MGSK-Lys-C was expressed at a high level in an optimized expression system as inclusion bodies. The Lys-C activity reached its maximum with about 9340 nkat/Lculture under standard (chemical) refolding conditions. The r
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Advances in the total chemical synthesis of
2020-03-13

Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio
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We also observed reduced insulinotropic effects after intrav
2020-03-13

We also observed reduced insulinotropic effects after intravenous administration of both GLP-1 and GIP with atropine, whereas no inhibition was observed by atropine of the direct effects of GLP-1 and GIP action on beta-cells in the islet experiments. This suggests that the reduction in circulating i
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br Conclusion br Conflict of interest br Acknowledgment The
2020-03-13

Conclusion Conflict of interest Acknowledgment The authors acknowledge the grant support of the Tehran University of Medical Sciences (94-02-49-29647). Introduction Earlier in vitro observations have also established that the human 5-HT2A, while very similar to the rat isoform, exhibits
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The ribosomal synthesis of D proteins is not currently feasi
2020-03-13

The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi
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In the context of food allergy it
2020-03-13

In the context of food allergy it is hypothesized that intestinal barrier dysfunction might contribute to both antigen sensitization and the IgE/mast cell mediated effector phase of allergic disease, however no concluding data has been published to date [5]. An understanding of the mechanism of prim
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br A brief history of RBR E s RBR
2020-03-13

A brief history of RBR E3s RBR E3s were originally defined based on sequence alignments that predicted a tripartite motif of three zinc (Zn)-binding domains: two RING domains (RING1 and RING2) connected via an in-between-RING (IBR) domain [28], [29]. The prediction together with initial observati
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Ubiquitin activating enzyme activates ubiquitin
2020-03-13

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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