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With this goal in mind we proceeded to explore the
2022-03-01

With this goal in mind, we proceeded to explore the C5-heteroaryl class of pyrazole-acids. Initial efforts, focused on a thiophene replacement, demonstrated little improvement. The 2-thiophene derivative (0.25μM and 0.24μM), a surrogate to the phenyl moiety, demonstrated only a modest boost in activ
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In addition to the role of TGR
2022-03-01

In addition to the role of TGR5, the FXR-FGF15/19 axis has been implicated in other aspects of glucose metabolism and metabolic disorders. In humans, both obesity and type 2 diabetes mellitus (T2DM) are associated with lower plasma FGF19 levels [67,68]. A derivative of the naturally occurring FXR ag
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Although we showed that RBL
2022-02-28

Although we showed that RBL-2H3 Sc98 NKY 80 took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporter family, including SERT for
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br Acknowledgements This work is supported by
2022-02-28

Acknowledgements This work is supported by the Cognitive Sciences and Technologies Council of Iran (CSTC, Grant No. 95P31), the Iran National Science Foundation (INSF) and the Faculty of Medical Sciences, Tarbiat Modares University, Tehran, Iran. The authors wish to thank Dr. Ayat Kaeidi for his
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br Methods br Acknowledgements The authors thank
2022-02-28

Methods Acknowledgements The authors thank the ZLS group members, particularly Li Li and Elijah Roberts, for many helpful discussions. They also wish to thank Nathan Baker for APBS assistance, Jan Jensen for help with PROPKA 2.0, Susan Martinis for experimental interpretations, and John Stone
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Previous reports have showed that the expression and
2022-02-28

Previous reports have showed that the expression and localization of GLUT8 in mouse (Gómez et al., 2006; Kim and Moley, 2007), rat (Ibberson et al., 2002) and human (Schürmann et al., 2002). In this study, GLUT8 protein mainly localized in the spermatocytes, elongated and round spermatids in the adu
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In the small intestine digestion and absorption of the nutri
2022-02-28

In the small intestine, digestion and neuropeptides of the nutrients are the next processes with an impact on the resulting plasma profile. Normally, neither carbohydrate digestion nor absorption are limiting factors, which is illustrated by the rapid and extensive absorption of glucose in conditio
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Extending time action is another strategy to increase in
2022-02-28

Extending time action is another strategy to increase in vivo efficacy. Twice daily administration of the unacylated analogs herein caused greater body weight loss in DIO mice than the equivalent dose administered as a single daily injection, suggesting that protracted time action should yield more
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br Materials and methods br Results br Discussion
2022-02-28

Materials and methods Results Discussion Our study demonstrates that human GIP(3-30)NH2 is a selective GIPR antagonist that inhibits both GIP-mediated cAMP signaling, β-arrestin recruitment, and GIPR internalization. Furthermore, we demonstrate that human GIP(3-30)NH2 binds with high affini
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Though regulation of ghrelin interaction with GHSR has not b
2022-02-28

Though regulation of ghrelin interaction with GHSR has not been described previously, a precedent for a similar regulatory mechanism exists in the form of the interaction between Agouti-Related Protein (AgRP) and melanocortin receptor subtypes MC3R and MC4R (Ollmann, 1997). AgRP is produced by hypot
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br Results br Discussion The inflammasome consists of the
2022-02-28

Results Discussion The inflammasome consists of the sensor molecule nucleotide oligomerization domain (NOD)-like receptors (NLRs), the adaptor protein ASC, and the CI 976 molecule CASP1 (Guo et al., 2015). Among the different types of inflammasome, the NLRP3 inflammasome requires a priming st
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Lentiviruses are associated with immunological impairment in
2022-02-28

Lentiviruses are associated with immunological impairment in their respective hosts, and both human immunodeficiency and feline immunodeficiency viral infections increase the likelihood of secondary bacterial infections [23], [24]. Recently, Kubes et al. [25] demonstrated that feline neutrophils exh
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br Methods and materials br
2022-02-28

Methods and materials Results Discussion In this study we demonstrate that CF epithelial chemokine receptor exhibit features of apoptosis in their basal, unstimulated state including increased caspase (-3 and -8) activation compared to non-CF epithelial cells. Analysis of factors responsibl
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In non Hodgkin lymphoma the catalytic
2022-02-28

In non-Hodgkin lymphoma the catalytic SET domain of the histone methyltransferase EZH2 is subject to recurrent heterozygous missense mutations . These alterations have been observed in ∼20% of patients with diffuse large B cell lymphoma (DLBCL) and ∼10% of patients with follicular lymphoma (FL). The
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br STAR Methods br Acknowledgments Funding for
2022-02-28

STAR★Methods Acknowledgments Funding for this work was provided by grants from the US National Institute of Allergy and Infectious Diseases (NIAID) (R01-AI095068 and UM1-AI068613 to S.H.E. and U24-AI118633 to H.B.L.) and grant OPP1155863 from the Bill and Melinda Gates Foundation to S.J.E. Add
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