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So far GnRH receptors have been detected in the
2021-09-16

So far, GnRH receptors have been detected in the human ovary, but their physiological importance is still unclear (). In particular, GnRH receptors as well as GnRH types I and II have been localized in the granulosa merestinib synthesis of pre-ovulatory follicles, but not of follicles from the prim
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In parallel we were also preparing and
2021-09-16

In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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mineralocorticoid receptor We noticed that the spontaneous
2021-09-16

We noticed that the spontaneous openings of the D97R α1 GlyR appeared to be quite similar to those elicited by a maximally-effective glycine concentration on wildtype GlyR; both generated similar open and shut dwell-time histograms, both exhibited openings grouped into clusters with Popen values gre
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To confirm the in vitro
2021-09-16

To confirm the in vitro findings, atorvastatin or pravastatin was given to C57BL6/J mice fed with high fat diet. Doses of atorvastatin were set to be 6 mg/kg and 12 mg/kg, which were within clinical therapeutic doses. The results revealed that treatment of atorvastatin but not pravastatin impaired g
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br Conclusions Temporally controlled disruption
2021-09-16

Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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In accordance with its similarity to classical NLSs Importin
2021-09-16

In accordance with its similarity to classical NLSs, Importin α3 was recently reported as a nuclear transport receptor for Ci (). We therefore superimposed the Gli1 NLS model with the Importin α2 structure (3EFX), which has a structure similar to Drosophila Importin α3 () (Fig. 4.4B). Gli1 NLS fitte
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HG-10-102-01 br Conclusion Our experiments have confirmed th
2021-09-15

Conclusion Our experiments have confirmed the effects of fasting, DIO, and E2 on the expression of Ghsr, Npy, and Agrp in the ARC (Briggs et al., 2013, Briggs et al., 2010, Brown and Clegg, 2010, Coppola et al., 2007, Palou et al., 2009, Roepke et al., 2008, Verhulst et al., 2012). However, gene
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Since the Gardos channel Ca
2021-09-15

Since the Gardos channel Ca2+ sensor have been shown to be constitutively bound calmodulin [16] and the PMCA is activated by association to a calcium–calmodulin complex, it seems probable that the NS309 agonist effect is caused by direct interaction with the Gardos channel, and not by an action on c
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br Electron crystallographic structures of connexins The str
2021-09-15

Electron crystallographic structures of connexins The structures of gap junctions are good targets for electron microscopy because they exhibit the characteristic features of self-assembly. Early studies examined the three-dimensional (3D) structures of native gap junction Dehydroepiandrosterone
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Some but not all GSIs inhibit
2021-09-15

Some, but not all, GSIs inhibit signal peptide peptidases as well, though this has not been systemically studied [36], [41]. When considering biological activities of various GSIs this is an important and understudied caveat that could influence both biological response as well as potential toxiciti
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The present data suggest that the decrease
2021-09-15

The present data suggest that the decrease of liver BAs was mainly due to the decrease of hepatic BAs synthesis because the BA synthetic enzymes Cyp7a1, Cyp7b1 and Cyp8b1 were markedly reduced. The increase may also be due to the increase of hepatic BAs efflux, because the liver BA efflux transporte
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ubiquitin proteasome system Next we conducted subgroup analy
2021-09-15

Next, we conducted subgroup analyses with stratification along interaction variables, namely the PPARG SNP and fasting NEFA. The study population was thus stratified into high and low NEFA (along the median NEFA, 561 μmol/L), and PPARG minor allele (Ala) carriers. This stratification resulted in 4 s
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Results of studies on fish FBPase are somewhat confusing alt
2021-09-15

Results of studies on fish FBPase are somewhat confusing: although fishes skeletal muscles possess relatively high FBPase activity (Knox et al., 1980, Lushchak et al., 2001) and the isozyme present therein has kinetic properties typical to all vertebrates muscle FBPases (Rosenmann et al., 1977), inv
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br Materials and methods br Results br Conclusions In
2021-09-15

Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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Introduction Post translational modifications to the N
2021-09-15

Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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