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To gain insights for further improvement of the agonistic
2022-01-10
To gain insights for further improvement of the agonistic activity, we compared the structural features of the -carbamate piperidine moiety in with that of the spirocyclic moiety in –. Obviously, the substituent corresponding to an isopropyl group on the -carbamate in was lacking in the spirocyclic
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Both GPR A and GPR are located on chromosome
2022-01-10
Both GPR109A and GPR81 are located on chromosome 12q24 [3] and mediate anti-lipolytic effects through coupling to Gi-type G proteins [17]. It is important to note that with the recent deorphanization of these receptors, there has been a recommendation to the International Union of Basic and Clinical
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The life cycle of T
2022-01-10
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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We report here a patient with a
2022-01-07
We report here a patient with a one-base frame-shift deletion in the PURA gene that presented an unusual phenotype including persistent hypoglycorrhachia. We propose a possible link between hypoglycorrhachia and PURA dysfunction postulating PURA as a GLUT1 regulator. We therefore hypothesize that mu
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br Glucocorticoid receptor and metabolic syndrome GCs
2022-01-07
Glucocorticoid receptor and metabolic syndrome GCs acting through the GR regulate key enzymes of glucose metabolism in the liver, skeletal muscle, adipose tissue and the pancreas. In the liver, GCs regulate the expression of major gluconeogenic enzymes such as phosphoenolpyruvate carboxykinase, g
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br Acknowledgements This study was supported by National
2022-01-07
Acknowledgements This study was supported by National Institutes of Health grant (R01GM104037), VA grant (BX002741), and Rutgers Busch grant. Nuclear receptor FXR is the master regulator of bile acids homeostasis The farnesoid X receptor (FXR) belongs to a family of proteins known as nuclear
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Lenvatinib is an orally available multi targeted
2022-01-07
Lenvatinib is an orally available, multi-targeted tyrosine kinase inhibitor against VEGFR1–3, FGFR1–4, PDGFRα, RET, and KIT [11,12]. In a recent phase III trial for patients with previously untreated uHCC (REFLECT study), lenvatinib showed statistical non-inferiority of overall survival compared to
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The feasibility of using the Fas Fas ligand
2022-01-07
The feasibility of using the Fas/Fas ligand (FasL) system to target vascular progenitor 2801 contributing to intimal hyperplasia has been shown in many studies [[18], [19], [20], [21], [22], [23], [24]]. Fas receptor, a member of tissue necrosis factor family, is a death receptor that initiates apop
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A few previous studies have examined Factor Xa
2022-01-07
A few previous studies have examined Factor Xa inhibitors for VTE prophylaxis in hip fracture patients. In a 2001 paper, Eriksson et al. studied 1250 patients with hip fractures that had been randomized to either postoperative Factor Xa inhibitor or enoxaparin [13]. Each patient received bilateral v
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During the activation of the
2022-01-07
During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium bromocriptine mesylate sale on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not dire
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Syt itself does not catalyze lipid
2022-01-07
Syt1 itself does not catalyze lipid mixing and membrane fusion. Rather, the pairing of vesicular and target membrane SNAREs into complexes serves to pull bilayers together to drive fusion; Ca•syt1 accelerates these fusion reactions so that they occur on rapid timescales in a manner that is precisel
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In addition to indoles two additional
2022-01-07
In addition to indoles –, two additional structural variants were synthesized to explore the synthetic flexibility and structure–activity relationships of this system. The first of these was the homologation of the acetic Cyt387 side chain to prepare compound (). The extension of the chain was exp
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br To explore further the functional impact of
2022-01-07
To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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Several mechanisms have been suggested to
2022-01-07
Several mechanisms have been suggested to underline the release of signalling molecules from astrocytes: reverse operation of glutamate transporters, volume-regulated anion channels, gap-junctional hemi channels, diffusional release through purinergic receptors and Ca2+-dependent exocytosis [2], [15
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Mitochondrial binding by HK prevents mortality by
2022-01-07
Mitochondrial binding by HK prevents mortality by inhibiting pro-apoptotic factor (Bcl-2 family)-mediated opening of the mitochondrial permeability transition pore (mPTP) (Arora and Pedersen, 1988, Calmettes et al., 2016, Kodde et al., 2007, Pedersen et al., 2002, Rosano, 2011, Schindler and Foley,
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