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A high throughput screening campaign of the
2022-02-22

A high-throughput screening campaign of the Lilly corporate compound collection led to the discovery of as potent and selective inhibitor of GlyT1 (IC=45nM, GlyT2 IC>30,000nM). In addition to the characteristic -methyl glycine moiety as acidic head group and the novel ethanolamine linker, also cont
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The life cycle of T cruzi requires
2022-02-22

The life cycle of T. cruzi requires both vertebrate and invertebrate hosts. In the insect (invertebrate) vector, the protozoan undergoes extracellular replication, whereas in the mammalian (vertebrate) host it replicates by obligate intracellular multiplication (Rodrigues et al., 2014). Hence, the p
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br Endogenous lipids as SLC
2022-02-22

Endogenous lipids as SLC6 transporter modulators Lipids constitute part of the environment in which membrane-embedded transporters operate [62]. Endogenous lipids can act as inhibitory ligands [63] or functionally important components of the membrane that impart changes in transporter structure [
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Tetrazole is one of the most commonly used bioisosteres for
2022-02-22

1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive
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Considerable evidence links sustained GCG administration
2022-02-22

Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms
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Insulin de sensitization has been observed in
2022-02-22

Insulin de-sensitization has been observed in the brains of people with AD [51], [52], [53] and we previously demonstrated that the GLP-1 analogue liraglutide was able to reverse this [54]. Importantly, GW788388 insulin de-sensitization correlates well with cognitive decline [15], [55] and with tau
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Beside these studies related to
2022-02-22

Beside these studies related to food, several groups examined the role of ghrelin in the actions of psychostimulants. Modulation of the ghrelin system and food restriction alter locomotor sensitization, DA release in the NAc, and CPP induced by cocaine, amphetamine, and nicotine (Abizaid et al., 201
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Although NCT undergoes complex glycosylation processing for
2022-02-22

Although NCT undergoes complex glycosylation processing for maturation through trafficking from endoplasmic reticulum to Golgi or additional compartments, the effect of NCT glycosylation on γ-secretase activity and substrate specificity is still unknown. The present study focused on glycosylation st
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br Conflict of interest br Introduction Milk and
2022-02-22

Conflict of interest Introduction Milk and dairy products are nutritious foods that provide lactose, calcium, phosphorous, magnesium and proteins, among other nutrients, which have been reported to have a fundamental role in bone development and healthy diets. An adequate consumption of dairy
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Recent studies have elucidated a profound
2022-02-21

Recent studies have elucidated a profound role for FFA4 in modulation of metabolism and energy utilization as well as endocrine and immune function, and as a consequence, have thrust FFA4 to the forefront of drug discovery efforts. For example, activation of FFA4 by fatty Tanshinone I or synthetic
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br Significance Metabolites present in the extracellular env
2022-02-21

Significance Metabolites present in the extracellular environment can potently modulate cellular phenotypes and potentially serve as therapeutics for various diseases. Ferroptosis is a non-apoptotic cell death process characterized by the generation of toxic lipid reactive oxygen species (ROS).
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In accordance with our study the
2022-02-21

In accordance with our study, the blockage of Fas/FasL pathway and overexpression of miR-204-5p was associated with reduced BUN, Scr, and MDA, as well as elevated SOD and GSH-Px. A recent study has reported the ectopic expression of BUN and Scr in RIRI animals, which marked the dysfunction of kidney
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br Materials and methods This is a retrospective case
2022-02-21

Materials and methods This is a retrospective case-controlled study. The cases were selected based on the presence or absence of preeclampsia. Women enrolled in the study delivered singleton pregnancies at our institution from June 2003 to July 2004. Preeclampsia is defined as elevated blood pres
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HCC metastasis is a multistep multifactorial process includi
2022-02-21

HCC metastasis is a multistep, multifactorial process, including adhesion of tumor u0126 to the extracellular matrix (ECM), remodeling and degradation of ECM, invasion through local tissue, intravasation into blood or lymph vessels, and forming new tumors at distant sites [6,7]. Loss of adhesion or
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In a preliminary communication we showed
2022-02-21

In a preliminary communication, we showed that AT and ETB receptors colocalize and coimmunoprecipitate in renal proximal tubule cells, and stimulation of the AT receptor increases ETB receptor expression in Wistar-Kyoto (WKY) rats [abstract; Zeng C,, 26:80A, 2003]. We hypothesize that the ETB recept
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