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The neotropical fish Prochilodus lineatus
2022-06-30
The neotropical fish Prochilodus lineatus has been widely used in experimental designs for being sensitive to variations in water quality and tolerant to laboratory conditions (Camargo and Martinez, 2006, Cazenave et al., 2014, da Silva and Martinez, 2014, Vieira et al., 2016). Concern and reports
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A repertoire of cytotoxic payloads is
2022-06-30
A repertoire of cytotoxic payloads is increasing; among those, MMAE has been utilized for the highly effective ADC brentuximab vedotin. However, the ADCs which utilized MMAE to target GCC in solid tumors have shown a poor efficacy suggesting that various tumor types respond differently to a given to
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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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