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Here we investigate the structural and biochemical
2022-03-28

Here we investigate the structural and biochemical properties of the N-GTPase domain of p190RhoGAP-A. We determine the crystal structure and find that N-GTPase adopts an extended GTPase-like fold with six unique inserts that seem to preclude its ability to bind typical GAP, GEF, or Azithromycin Dihy
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br Materials and methods br Results br
2022-03-28

Materials and methods Results Discussion According to the literature, zaprinast is a high-affinity agonist of GPR35 (Berlinguer-Palmini et al., 2013, Divorty et al., 2015, Taniguchi et al., 2006, Zhao et al., 2010). GPR35 WEHI-539 synthesis has been identified within discrete regions of th
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LPC OMe LPC LPC and OMe LPC were shown
2022-03-28

LPC 14:0, 2-OMe-LPC 14:0, LPC 16:0 and 2-OMe-LPC 16:0 were shown to be most potent stimulators of intracellular calcium flux in the β cell model, which is one of key processes leading to insulin exocytosis. Yet, species with myristoyl residue initiate calcium influx through voltage-gated Liproxstati
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Based on these findings we set out to identify
2022-03-28

Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun
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In three groups independently proposed two different mechani
2022-03-28

In 2001, three groups independently proposed two different mechanisms for the catalytic reaction of GlxI [5], [6], [7]. Richter and Krauss (RK) used HF/4–31G calculations of the active site, coupled with a frozen effective fragment potential description [8], [9] of eleven residues in the binding sit
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Netarsudil receptor First class II fusion proteins are known
2022-03-28

First, class II fusion proteins are known to transition from a (homo- or hetero-) pre-fusion dimer to a post-fusion trimer [57], [58], [59], [60], [61], [62] through a monomeric intermediate [63], [64], and a crystalline structure of a monomer of Rift Valley fever virus (a phlebovirus, member of the
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It is becoming increasingly apparent that membrane lipids
2022-03-28

It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene
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At the second step blind docking simulation of independent r
2022-03-26

At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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Recently several dual GLP GIP
2022-03-26

Recently, several dual GLP-1/GIP receptor agonists have been developed as a treatment of type II diabetes. These peptides can activate both the GLP-1 and the GIP receptor. Such dual receptor agonists are superior compared to single GLP-1 analogues such as liraglutide (Finan et al., 2013). Previously
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There is increasing evidence that Cxs in astrocytes may
2022-03-26

There is increasing evidence that Cxs in astrocytes may play a role in several models of brain pathologies. Interestingly their roles are at the moment more considered through their hemichannel function (Bennett et al., 2012; Bosch and Kielian, 2014; Davidson et al., 2013; Orellana et al., 2016; Kim
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br Involvement of gap junctions and Panx in spinal cord
2022-03-26

Involvement of gap junctions and Panx1 in spinal cord processing of pain information Several studies indicated that GJs in the CNS contribute to pain. A common finding in such studies is that intrathecal administration of GJ blocker attenuates pain behavior. For example, intrathecal CBX attenuate
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Of note the intracellular egg compartment exhibiting SA gal
2022-03-26

Of note, the intracellular egg compartment exhibiting SA-β-gal activity also exhibits lipofuscin auto-fluorescence (Fig. 6B), and it is co-stained with the lipid-specific dye SBB (Supplemental Fig. 5). On the one hand, these findings reflect the fact that the pool of yolk protein contains lipoprotei
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Many neutral and acidophilic galactosidases have been
2022-03-26

Many neutral and acidophilic β-galactosidases have been purified from microorganisms [14], while only a few alkalophilic β-galactosidases have been reported [19]. An alkalophilic β-galactosidase, BGal_375, was obtained and researched for the characterization of its hydrolytic activity. BGal_375 show
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At this point it needs
2022-03-26

At this point it needs, however, to be mentioned that most in vivo studies regarding the herein discussed nuclear receptors were performed in rodents, especially in mice. Due to the significant differences in metabolism in mice and humans, not all results are translatable between these species and h
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FBPase deficiency is a very rare inborn error of fructose
2022-03-26

FBPase deficiency is a very rare inborn error of fructose Roxithromycin of autosomal recessive inheritance. This disorder usually occurs in the first year of life through ketotic hypoglycemia and lactic acidosis triggered by catabolic episodes such as prolonged fasting or febrile infections (Steinm
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