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To further investigate if GPR
2022-04-12
To further investigate if GPR40 was the functional target of these phenylpropiolic filgotinib analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40
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Sumoylation of transcription factors has been generally link
2022-04-11
Sumoylation of transcription factors has been generally linked to transcriptional repression and, in a few cases, to transcriptional activation [60] Accumulating evidence implies that corepressor complex subunits, including CoREST, CtBP, Daxx, NCoR1, SMRT and histone deacetylase complexes (HDACs), p
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Our results are consistent with
2022-04-11
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral 2801 as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts. A reduced numbe
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Acknowledgments The authors would like to thank members of t
2022-04-11
Acknowledgments The authors would like to thank members of the Department of Discovery Synthesis (DDS) and Biocon-Bristol Myers Squibb Research Center (BBRC) for scaling up key intermediates, analytical team for analytical experiments, lead profiling group for evaluating compounds in an in vitro AD
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chemicals library The mast cell has long been recognized as
2022-04-11
The mast cell has long been recognized as central to the mediation of allergic responses not least because it is the principal repository of histamine in the body. Following activation by allergens, the mast cell can release histamine as well as generate a host of additional mediators such as cystei
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There are five subfamilies of P type ATPases I
2022-04-11
There are five subfamilies of P-type ATPases (I-V), which transport metal ions or phospholipids across membranes (Palmgren and Nissen, 2011). Although our studies indicate that the P-type ATPase domain is important for function, how it contributes to cGMP production is currently unknown. The P-type
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Ning et al showed that LPC appeared to increase insulin
2022-04-11
Ning et al. showed that LPC 18:1 appeared to increase insulin release through both GPR119-dependent and -independent mechanisms (Ning et al., 2008). In our study, we have shown that not only GPR119 but also GPR40 and GPR55 participate in LPC-stimulated insulin secretion (Fig. 4, Fig. 5) and target p
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The pharmacokinetics of was obtained
2022-04-11
The pharmacokinetics of was obtained in mouse, rat and dog to determine if it had a suitable profile to investigate the effects of the GPR120 mechanism (). had an adequate half-life, low clearance in all 3 species, and high blood levels and bioavailability. The low volume of distribution (V) indi
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The calculations for the R substrate showed
2022-04-11
The calculations for the R substrate showed that, like the S substrate, the coordination shell of the Zn 5 of 17000 mg is more symmetric than in the HIC-SG crystal structure. This symmetry indicates that the enzyme could use the same reaction mechanisms as for the S substrate, but with exchanged ro
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Lamina II SG spinal cord neurons play an important role
2022-04-11
Lamina II (SG) spinal cord neurons play an important role in regulating nociceptive input from the periphery [20,21]. Moreover, lamina II neurons are concentrated with glycinergic or GABAergic inhibitory interneurons. Therefore, it is possible that β-alanine might modulate nociceptive transmission i
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br Author s contributions br Conflict of interest br
2022-04-11
Author's contributions Conflict of interest Acknowledgements This work was supported in part by a grant from Department of Biotechnology (DBT), Government of India (Sanction Order No.: BT/563/NE/U-Excel/2016). MC, PDG and SKM acknowledge the Ministry of Human Resource and Development (MHRD)
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Taking into account abovementioned vitamin D deficiency effe
2022-04-11
Taking into account abovementioned, vitamin D3 deficiency effects on synaptic neurotransmission can be considered as targeting both Ca2+-independent and Ca2+-dependent processes. Ca2+-independent action of vitamin D3 deficiency is associated with a decrease in the expression of glutamate and GABA tr
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Apoptosis a form of programmed cell
2022-04-09
Apoptosis, a form of programmed cell death, is a critical component in maintaining homeostasis and growth in all tissues and plays a significant role in immunity and cytotoxicity [54,55]. Although GR are expressed in all immune cells, the physiological outcomes of GR activation are highly cell type-
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In the course of our
2022-04-09
In the course of our synthetic studies, we also discovered an unprecedented application of Burgess reagent. Instead of generating an olefin by an intramolecular syn-elimination, the product resulting from the treatment of spirocyclic alcohols 11 and 12 with Burgess reagent led to the expansion of th
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br Acknowledgments We would like to acknowledge Jenna Hall
2022-04-09
Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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