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In summary we have designed and optimized
2021-10-12
In summary, we have designed and optimized a new series of 1,4-dioxycyclohexane GPR119 agonists. SAR studies led to the discovery of the preferred molecule that has potent and efficacious GPR119 activity across species. This lead compound exhibited an excellent ADME and safety profile, and demonstra
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br Materials and methods br Results br Discussion
2021-10-12
Materials and methods Results Discussion ENU mutagenesis is a powerful approach to identify novel genes or allopurinol zyloprim synthesis to dissect the molecular basis of mammalian immune system (Siggs, 2014). T cells are critical components in the host defense against pathogens, and their
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Estrus expression after removal of P insert and
2021-10-12
Estrus GDC-0152 after removal of P4 insert and before TAI is a clear predictor of greater P/AI in protocols that use GnRH [6,8], EB, or ECP [10,18] as ovulation inducers. Therefore, our third hypothesis was that heifers showing estrus behavior would have greater P/AI, which was supported in both tr
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Given that we planned to isolate
2021-10-12
Given that we planned to isolate the GluN1/GluN3A receptor by immunoaffinity chromatography using a Myc epitope tag on GluN3A, we first checked that the tag does not affect the functional properties of the receptor. To do this we co-transfected HEK-293 cells with DNA encoding WT GluN1 and either WT
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br Conclusions br Acknowledgements br Introduction Glucose m
2021-10-12
Conclusions Acknowledgements Introduction Glucose metabolism is vital to prepare uterine epithelium and stroma for embryo implantation and for the differentiation of the functionalis layer to support the developing conceptus [[1], [2], [3], [4]]. Due to its polar nature and hydrophilic cond
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In general fish has a limited
2021-10-12
In general, fish has a limited ability for digestion and metabolism of carbohydrate though carbohydrate is the cheapest dietary energy and carbon source to animals and the best candidate for replacing dietary protein (Enes et al., 2009, Kamalam et al., 2017, Wilson, 1994). Furthermore, the analysis
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Another lever to efficiently eradicate tumors including
2021-10-11
Another lever to efficiently eradicate tumors including ovarian cancer might rely on their high addiction to iron [34]. In fact, ultrasmall silica-based nanoparticles, functionalized with melanoma-targeting peptide, efficiently triggered ferroptosis not only in cell culture but also in tumor bearing
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Cefpodoxime Proxetil The lysine K specific demethylase KDM f
2021-10-11
The lysine (K)-specific demethylase 4 (KDM4) family is comprised of 4 isoforms, KDM4A to -D, also known as JMJD2A to -D. KDM4A, B, and C encode proteins consisting of a JmjC, a JmjN, two PHD, and two Tudor domains. KDM4D is unique within the KDM4 family in that it has neither PHD nor Tudor domains,
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br Acknowledgments Work in SI s laboratory is
2021-10-11
Acknowledgments Work in SI’s laboratory is supported by grant IM 20/4-1 from the Deutsche Forschungsgemeinschaft, Bonn (Germany) and grant EKFS 2012_A309 from the Else Kröner Fresenius Stiftung, Bad Homburg (Germany). FW’s group is supported by the Dr Vaillant Foundation and the Dutch Burns Found
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br Financial support This study was supported
2021-10-11
Financial support This study was supported by Grant PH-102-PP-11, PH-103-PP-11 from the National Health Research Institutes, Taiwan. Conflict of interest Please refer to the accompanying ICMJE disclosure forms for further details. Authors’ contributions Acknowledgements Introduction
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In the inhibitory kinetic studies five different concentrati
2021-10-11
In the inhibitory kinetic studies, five different concentrations of DEL carefully selected from the near-linear region of the dose–response curve (0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM, and 8.0 μM) were used. The Vm values at fixed [CDNB]–varied [GSH] and at fixed [GSH]–varied [CDNB] were 10.4 ± 0.22 U mg−
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Lactate as administered in these models is
2021-10-11
Lactate as administered in these models is metabolized rapidly and it appears that transient engagement of GPR81 with lactate serum concentrations in the range of moderate exercise physiology, as measured here at 3–4 mmol/L, are sufficient to suppress tissue macrophage NF-κB activation in our models
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Disrupting the dialog between microbiota and the host especi
2021-10-11
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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GnRH ant have been designed to obtain pharmacological compou
2021-10-11
GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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Neurotransmitter transporters are rapidly recycled from and
2021-10-11
Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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