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br Indirect GLI antagonists br Direct
2022-04-09

Indirect GLI antagonists Direct GLI antagonists Concluding remarks Targeting GLI effectors represents a promising therapeutic strategy for cancer treatment. This is particularly relevant for certain tumors, such as MB, since, although classified into four distinct molecular groups (Hh- or W
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br Introduction G protein coupled receptors GPCRs
2022-04-09

Introduction G-protein coupled receptors (GPCRs) represent one of the largest family of receptors involved in cell membrane signal transduction and have become one of the leading therapeutic targets worldwide (Chakraborty and Chattopadhyay, 2015; Bouvier, 2001; Sriram and Insel, 2018). GPCRs sign
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How changes in APP processing by secretase lead to
2022-04-09

How changes in APP processing by γ-secretase lead to AD is still not well understood. Deposition of amyloid beta (Aβ) peptide fragments of the amyloid precursor protein (APP) in amyloid plaques and hyperphosphorylated tau in neurofibrillary tangles are the cellular hallmarks of AD (O’Brien and Wong,
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Isolation and application of cold adapted galactosidase in t
2022-04-09

Isolation and application of cold-adapted β-galactosidase in the production of low lactose dairy products would play a critical role in improving access to low lactose dairy products for lactose intolerant individuals [9,11]. Milk contains high levels of K+, Ca2+, and Na+, and β-galactosidase used i
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As mentioned earlier two different
2022-04-09

As mentioned earlier two different isoforms of TFE3 [16] have been reported viz. the full length (TFE3L) and smaller (TFE3S) without exon 1&2. TFE3S lacks an N-terminal acidic activation domain which is present in TFE3L hence is a dominant negative form of TFE3L [51]. This dominant negative feature
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The chemical structure of BAs consists of a steroid nucleus
2022-04-09

The chemical structure of BAs consists of a steroid nucleus with an acidic side chain. They are amphipatic molecules characterized by a hydrophilic α-face and a hydrophobic β-face. The hydrophobic pocket of the FXR LBD interacts with BAs largely through the β-face. The α-face contains several hydrox
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Since we were able to
2022-04-09

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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Ligand selectivity may directly be related to
2022-04-09

Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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Corresponding to the different insulinotropic signaling the
2022-04-09

Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Miglitol on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site for full agonists
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Glucose metabolic pathways are well defined but the subcellu
2022-04-09

Glucose metabolic pathways are well defined but the subcellular organization of these pathways is poorly understood in liver and kidney. Several factors affect the net flux of gluconeogenesis and allow the CP-673451 to respond to physiological changes [1]. Ovadi and Srere have suggested that a new
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polycomb repressive complex The other type of cell death tha
2022-04-09

The other type of cell death that occurs in activated T polycomb repressive complex is caused by growth factor withdrawal following TCR-mediated activation, whereby most of the activated T cells die by apoptosis following the eradication of bacteria during an acute infection in order to reduce the
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br Materials and methods br Results br
2022-04-09

Materials and methods Results Discussion Since early times, herbs and their extracted substances have been used as foods and medicinal resources worldwide (Petrovska, 2012). A Ginger is one of the most important and oldest spices, consisting of the prepared and sun-dried rhizomes of Zingibe
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Following the discovery of diketo compounds
2022-04-09

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent MK-4827 Racemate based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase
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The root of Danshen has been
2022-04-09

The root of (Danshen) has been widely used as traditional Chinese medicine for many years and shown to exhibit significant pharmacological activities for a variety of human diseases including cancers. Tanshinones, the major active components, belong to a group of an abietane-type diterpenes containi
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brucine Literature review suggests a strong
2022-04-09

Literature review suggests a strong presence of central histaminergic transmission in the brucine areas targeted by caffeine to induce its behavioral actions. Interestingly, it is reported that caffeine administration increases the histamine neuronal activation and release of histamine in the brain
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