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Unlike many interacting proteins NRG was
2022-03-30

Unlike many interacting proteins, NRG1 was the only one observed to undergo cleavage by NS3/4A. NRG1 is one of four proteins in the neuregulin family that act on the ErbB member of the EGFR (EGF receptor) family. NRG1 has several isoforms produced by alternative splicing of pro-NRG1, which allows it
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Recently anti tumor or antiviral strategies using RNAi for
2022-03-30

Recently, anti-tumor or antiviral strategies using RNAi for both gene silencing and innate-receptor activation were designed; one mechanism of these strategies is activating the intracellular retinoic acid–inducible gene I protein (RIG-I). 5′-Triphosphate RNA (3p-small interfering RNA [siRNA]) is th
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Excessive adiposity is also a key pathogenic
2022-03-29

Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP
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In order to elucidate the mechanisms behind the observed cha
2022-03-29

In order to elucidate the mechanisms behind the observed changes in metabolic activity in the cardiomyoblasts we investigated changes in gene and protein expression subsequent to treatment with PSN632408 with or without concurrent exposure to palmitate. Activating GPR119 in basal and high palmitate
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T lymphocytes play an important
2022-03-29

T lymphocytes play an important role in cellular and humoral immunity and immune responses (Shin and Iwasaki, 2013; Schenkel and Masopust, 2014). T CGP 35348 mature after complex selection and differentiation in the thymus. They can express various membrane proteins, such as CD3, CD4, and CD8 molecu
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br Methods and materials br Acknowledgements The
2022-03-29

Methods and materials Acknowledgements The authors thank the NIH AIDS Reagent Program for providing the materials and reagents. The HIV-1 1084i envelope gene was a generous gift from Dr. Charles Wood. This work was supported in part by grants to S.-H. X. from the Bill and Melinda Gates Foundat
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br Transporter based brain targeting nano DDS Drug delivery
2022-03-29

Transporter-based brain-targeting nano-DDS Drug delivery to the central nervous system (CNS) is still challenging due to the bloodbrain barrier (BBB)53., 54.. The BBB is a natural defense barrier protecting the glucagon receptor antagonist from harmful substances. Since only selected, neutral, l
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Which is the preferred dimer configuration the one correspon
2022-03-29

Which is the preferred dimer configuration, the one corresponding to the active state or the one corresponding to the desensitized state? Umbrella sampling simulations of a pair of GluA2 LBDs, using distances at the top (proximal to the ATD) and the bottom (proximal to the TMD), indicate that the de
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br Functional organization of postsynaptic glutamate recepto
2022-03-29

Functional organization of postsynaptic glutamate receptors Downstream effects of glutamate receptor positioning Mechanisms underlying the subsynaptic positioning of glutamate receptors Conclusions and future prospects The molecular organization of synapses is undoubtedly a critical dete
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To confirm that these were bona
2022-03-29

To confirm that these were bona fide interactions, we investigated whether the potassium channel subunits or Tmem263 formed complexes with GLT-1 or DAT after immunoprecipitation. Lysates of HEK-293 cells previously cotransfected with HA-GLT-1 or HA-DAT, and either YFP-Kv7.3, YFP-Kv7.2 or YFP-Kv7.5 w
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Since we were able to reach low micromolar to sub
2022-03-29

Since we were able to reach low micromolar to sub-micromolar potency in both compound series (6 and 7), we were also keen on assessing the preliminary ADME profile (particularly with respect to plasma and liver microsomal stability) of the most active compounds from these series. As it is evident fr
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br Conclusions GPCRs are versatile signaling
2022-03-29

Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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Although exhibited high inhibitory activity
2022-03-28

Although exhibited high inhibitory activity, was found to be metabolically unstable due to the hydrolysis of the phosphate group (data not shown), which prompted us to modify the phosphate moiety of . Comparison of the activities between three compounds bearing no or different spacer groups (, , and
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The above inferences concluded that histidine is enhancing t
2022-03-28

The above inferences concluded that histidine is enhancing the overall stability and rigidity of the protein which further might be restraining the protein during the transition from inactive to active state and vice-versa present in the SANT domain. Since the SANT domain binds with histone via elec
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br Materials and methods br Results and discussion
2022-03-28

Materials and methods Results and discussion To analyze the dependence of lysosomal exocytosis on Cu we exposed HeLa m-Chlorophenylbiguanide hydrochloride to fresh buffer containing normal levels of free Ca (1mM) and measured β-hex levels in the extracellular medium, followed by measuring β-h
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