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br Family A Receptors as Promiscuous
2022-06-29

Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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While NR upregulation in the spinal cord
2022-06-29

While NR1 upregulation in the spinal cord is known to contribute to pathological pain [7], [22] and furthermore, NR1 expression in the spinal cord has been shown to be reduced by continuous administration of the GlyT1-inhibitor ALX5407 [23], little is known about possible expressional changes of NR1
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Then the seven complexes GLOI indomethacin GLOI zomepirac GL
2022-06-29

Then the seven complexes (GLOI-indomethacin, GLOI-zomepirac, GLOI-fenoprofen, and GLOI-ketoprofen, GLOI-tolmetin GLOI-curcumin, and GLOI-bisdemethoxycurcumin) were energy-minimized to remove unfavorable steric strain relative to the force field adopted. Further MD simulations were carried out based
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Finally the formation of a regular network of fusion
2022-06-29

Finally, the formation of a regular network of fusion glycoproteins in their post-fusion state is not exclusive of vesiculovirus G. More or less regular networks have been also observed with other class III fusion glycoproteins such as pseudorabies gB [85] and several class II fusion glycoproteins [
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In insects structural cuticular proteins CPs play
2022-06-29

In insects, structural cuticular proteins (CPs) play important roles in determining the diverse physical properties of the cuticle, depending on developmental stages, as well as different body regions, as a result of interactions with other CPs and the structural biopolymer chitin [4]. Many studies
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Ubiquitination of GlyRs subunit on plasma membrane has been
2022-06-29

Ubiquitination of GlyRs-α1 subunit on plasma membrane has been shown to initiate the receptor COG 133 and subsequent degradation in lysosomes (Buttner et al., 2001). However, the specific E3 ligase responsible for GlyRs-α1 ubiquitination is largely unknown as yet. Also, the functional consequence of
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Although the overall structures of mGlu and mGlu VFTs
2022-06-29

Although the overall structures of mGlu2 and mGlu3 VFTs are highly similar, two major differences can be observed: (i) the number of functional Cl− binding sites, one in mGlu2 versus two in mGlu3 receptors and (ii) the loop 7 in lobe 2 is longer in mGlu3 than in the mGlu2 receptor. These two particu
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Through the analysis of various synthetic
2022-06-29

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic Vincristine sulfate motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of disc
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br Conclusion In summary a series
2022-06-29

Conclusion In summary, a series of novel GPR40 agonists bearing phenylpropiolic Raloxifene HCl motif with favorable metabolic stability were prepared and evaluated for their activities as GPR40 agonists. Among them, compound 9 was identified as a structurally distinct GPR40 agonist possessing po
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A number of GCK activators
2022-06-29

A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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The HH Gli pathway has been demonstrated
2022-06-29

The HH-Gli pathway has been demonstrated to play an extensive role in skeletal development. India Hedgehog, derived from hypertrophic chondrocytes, and Parathyroid Hormone-like related Protein (PTHrP), derived from peri-articular chondrocytes, form a negative feedback loop to inhibit chondrocyte hyp
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9-Phenanthrol br Clinical trials testing GLP
2022-06-29

Clinical trials testing GLP-1 mimetics in AD or PD patients GIP analogues show good neuroprotective effects in animal models of AD and PD Glucose-dependent insulinotropic polypeptide (GIP) is a 42-amino 9-Phenanthrol incretin growth factor which activates pancreatic islets to enhance insulin
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Gap junction channels exhibit different types
2022-06-29

Gap junction channels exhibit different types of gating properties. One alternative mechanism that should be mentioned is loop gating in which the extracellular loop of connexin assumes a configuration to form a narrow pathway for closure of unopposed hemichannels [53] and docked junction channels [
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Cytokines and hormones influence both gap junctions and endo
2022-06-29

Cytokines and hormones influence both gap junctions [106] and endocrine activity in the pituitary [3]. Long-term treatment (2 h) with the proinflammatory cytokines interleukin-1β (Il-1β) and tumor necrosis factor-α (TNF-α) transiently increases Cx43 expression and cell coupling in TtT/GF fccp [105]
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The conversion of lactose to GOS by gal involves
2022-06-29

The conversion of lactose to GOS by β-gal involves the same transglycosylation mechanism used by most glycoside hydrolases (GHs). This mechanism (Fig. 1) involves an enzyme-bound intermediate and consists of two processes: glycosylation and deglycosylation (Adlercreutz, 2017). The glycosylation proc
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