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br Structural studies of the cyclase catalytic
2021-12-21
Structural studies of the cyclase catalytic domains Structural determinants for catalytic activity The structure of the active αβGCcat structure has remained elusive. However, several studies have suggested how specific structural elements are involved in αβGCcat transitioning from the open in
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To date no studies have demonstrated any effect of
2021-12-21
To date, no studies have demonstrated any effect of obesity or inflammation on GPR109A expression in adipose tissue. Our findings demonstrate that HFD-induced obesity decreases adipose tissue GPR109A gene expression. Contradictory to our findings in adipose tissue in vivo, Digby et al. report that e
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There is sufficient evidence to indicate that kisspeptin
2021-12-21
There is sufficient evidence to indicate that kisspeptin plays a role in regulating sheep reproduction. However, the molecular mechanism by which kisspeptin regulates GnRH epothilone and reproduction has remained unclear. Therefore, in this study on GnRH in sheep, the promoter region of GnRH was cl
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Throughout the last few decades evidence has accumulated
2021-12-21
Throughout the last few decades, evidence has accumulated indicating that NTTs, whose primary location is the cell surface, are subject to a series of regulatory processes of intracellular traffic to and from the membrane (Robinson and Jackson, 2016; Vaughan and Foster, 2013). In addition, lateral m
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Herein in consider of the
2021-12-21
Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i
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Next the effects of a phenyl group at the
2021-12-21
Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio
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The effects of GHS R a
2021-12-21
The effects of GHS-R1a blockade on alcohol-related outcomes have been examined in numerous preclinical experiments, utilizing various GHS-R1a antagonists (JMV 2959, [D-Lys3]-GHRP-6, BIM 28163) and rodent species (prairie vole, mouse, rat). In spite of methodological differences, the results consiste
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br Materials and methods br
2021-12-21
Materials and methods Results and discussion Conclusion Altogether, our data provide an unexpected insight into Cx26 trafficking pathway and gap junction assembly in the cochlea. Since many of the disease-causing mutations in GJB2 impair the trafficking and delivery of Cx26 to the cell surf
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Some malignant human tumors cells also express FPRs and
2021-12-21
Some malignant human tumors Fmoc-Thr(tBu)-OH receptor also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and resista
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In addition we assessed the viability of tetrahydroquinoline
2021-12-21
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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In conclusion our results showed
2021-12-21
In conclusion, our results showed that FFAR1 can mediate the effect of PIO in attenuating β-cell lipoapoptosis through anti-oxidative stress, which may be related to the activation of the PLCγ-ERK1/2-PPARγ pathway. Our study helps not only to distinguish the role played by FFAR1 in lipotoxicity, but
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The neotropical fish Prochilodus lineatus
2021-12-20
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 a
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Besides the described effects on gross locomotor function
2021-12-20
Besides the described effects on gross locomotor function, impairment of visuo-motor coordination and fine-motor skills like resting tremors, bradykinesia and rigidity were also investigated, reflecting on the symptomatology of Parkinson's disease in humans (Inzelberg et al., 2008). Preclinically, t
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Exendin-4 Corresponding to the different insulinotropic
2021-12-20
Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Exendin-4 on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonis
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In addition we assessed the viability of tetrahydroquinoline
2021-12-20
In addition, we assessed the viability of 1,2,3,4-tetrahydroquinoline (13t) and 1,2,3,4-tetrahydroisoquinoline (13u) as the tail on account of our previous SAR results. To our delight, 13t and 13u each had comparable activity to that of 13c, with 13u being slightly more potent than 13c. Further stru
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