• Initially studies of GPCRs predominantly assessed the signal

  2021-03-15

  

  Initially, studies of GPCRs predominantly assessed the signalling pathways downstream of receptors on the cell surface. There is now an understanding that GPCRs can localize to and signal from various intracellular compartments, such as the nucleus (reviewed in [40]). These intracellular pools of re

• br Non cyclic nucleotide EPAC regulators

  2021-03-15

  

  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

• The endothelin receptor type B EDNRB belongs to

  2021-03-15

  

  The endothelin receptor type B (EDNRB) belongs to the family of G protein-coupled receptors, which functions as a vital regulatory factor in signal transduction in cells, locating on human chromosome 13q22.3 (Ayala-Valdovinos et al., 2016; Bregar et al., 2018; Morimoto et al., 2018; Widowati et al.,

• br Conclusions br Declaration of interest br Acknowledgement

  2021-03-15

  

  Conclusions Declaration of interest Acknowledgements Introduction Uncorrected obesity has been a major health problem and the prevalence of obesity is fast rising reaching an epidemic proportion [[1], [2], [3]]. Ample of clinical and experimental evidence has suggested that obesity leads

• Therefore HNE is an attractive therapeutic target and the

  2021-03-15

  

  Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo

• MI has been detected in wastewater

  2021-03-15

  

  3MI has been detected in wastewater at concentrations of 640–700 μg L−1 (Hwang et al., 1995) and up to 20 mg L−1 in decaying algal water environments (Peller et al., 2014). It is likely that 3MI accumulation in fish might be due to the degradation of endogenous amino acids. The presence of this che

• Similarly in the EAE model Chalmin et al previously

  2021-03-15

  

  Similarly in the EAE model, Chalmin et al. previously demonstrated that EBI2 and CH25H might be responsible for the efficient egress of differentiated Th17 cells from the draining lymph nodes [31]. As discussed above, in active EAE we did not find differences in EAE development and only the transfer

• Currently two approaches can be used

  2021-03-15

  

  Currently, two approaches can be used individually or combinedly to overcome weak immunogenicity of subunit PIK-90 (Bookstaver et al., 2018; Moyle, 2017; Vartak and Sucheck, 2016). The first is to design particulate antigens. Virus-like particles (VLPs), for example—mainly derived from the capsid pr

• Based on the similar activities of

  2021-03-15

  

  Based on the similar activities of Rad6p and Cdc34p (i.e., both are E2 ub-conjugating enzymes) on ubiquitinylation of p33 replication protein, we propose that Rad6p and the plant Ubc2p mono- and bi-ubiquitinate the viral replication proteins in order to facilitate the recruitment of the cellular ESC

• UBA belongs to the non canonical E enzymes

  2021-03-15

  

  UBA5 belongs to the non-canonical E1 enzymes that lack a defined Cys domain but have the active-site Cys within the adenylation domain [24]. Similar to other E1 enzymes, UBA5's adenylation domain comprises an eight-stranded beta sheet that is surrounded by helices [21]. Moreover, like the ancestral

• br The central role of

  2021-03-15

  

  The central role of DNA-PK in the NHEJ NHEJ can be divided in several steps (Fig. 1A): 1) recognition and binding of Ku at each ends of the DSB following by the assembly of the DNA-PK at the break points and bridging; 2) phosphorylation of the DNA ends by DNA-PKcs; 3) ligation of the ends by DNA

• Hedamycin isolated from Streptomyces griseoruber belongs to

  2021-03-15

  

  Hedamycin, isolated from Streptomyces griseoruber, belongs to the highly cytotoxic pluramycin class of MLN2238 (Figure 3(c)). It consists of a planar anthrapyrantrione chromophore attached to two amino sugar rings at one end and a bisepoxide-containing side-chain at the other end (Figure 3(c)). Hed

• Fmoc-His(Trt)-OH receptor HvPap a member of the cathepsin

  2021-03-15

  

  HvPap-1, a member of the cathepsin F-like family, was identified in germinating barley seeds (Sreenivasulu et al., 2008). This enzyme participates in the mobilization of stored proteins (mainly hordeins) during the last phase of grain germination, and its activity is modulated by a propeptide or/and

• Unlike CRM exportins Cse and Xpot

  2021-03-15

  

  Unlike CRM1, exportins Cse1 and Xpot lack a C-extension and instead rely primarily on changes in HEAT-repeat conformation and direct Ran-cargo contacts to ensure low cargo-binding affinity in the cytosol and cooperative assembly of the exportin/Ran/cargo complex in the nucleus (Cook et al., 2005, Co

• The conventional medical therapy for

  2021-03-15

  

  The conventional medical therapy for IBD consists in reducing the inflammatory response using various strategies that exert severe side-effects, a strategy that also decreases the risk of colon carcinoma [13], [14]. During the last decade, the activation of the cholinergic system has been proposed f

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