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Our own search towards aryl imidazole
2021-12-20
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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Liver is the house for a variety of xenobiotic
2021-12-20
Liver is the house for a variety of xenobiotic-metabolizing pmsf that produce reactive oxygen species as well as reactive metabolites (Johansson et al., 2009; Noh et al., 2017; Puntarulo and Cederbaum, 1998). When the enzymes act upon pre- or pro-haptens, the chemicals would be activated to reactive
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According to its major function as master regulator
2021-12-20
According to its major function as master regulator of BA homeostasis, FXR has been shown to have a specific tissue distribution; it is expressed along the entire gastrointestinal tract with a peak in the liver and ileum, as well as in the kidney, and adrenal glands [30], [66], [135]. Low FXR expres
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We have isolated various bioactive
2021-12-20
We have isolated various bioactive ack1 inhibitors acting by binding to the receptors of endogenous bioactive peptides such as opioid, bradykinin, neurotensin, and complements C3a and C5a etc. [24]. Rubimetide is the first example of an agonist peptide of the FPR2 of exogenous origin. Anxiolytic-li
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Because FPR is expressed in VSMCs and its role
2021-12-20
Because FPR-1 is expressed in VSMCs and its role in non-hematopoietic cells is still unclear, we questioned whether FPR-1 would have physiological relevance for vascular behavior, in the same way as it does in neutrophils (Ca2+ homeostasis and smad inhibitor polymerization). First, we tested if FPR
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Evidence suggests that phosphorylation increases synaptotagm
2021-12-20
Evidence suggests that phosphorylation increases synaptotagmin affinity for the SNARE complex [15], [128]. It is, however, unclear how this might affect release. Synaptotagmin has been identified as part of the minimal vesicle docking machinery in chromaffin Meropenem [129]. Thus, phosphorylation o
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Histamine H and H receptor
2021-12-20
Histamine H2 and H3 receptor expression is altered in the bafilomycin a1 of Hdc mice (Chepkova et al, 2012, Fitzsimons and et al, 2001). Because these mice lack HA, expression of HA receptors might be thought to be irrelevant. This is not the case in Hdc heterozygotes, however, or in patients with
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Maillard reaction also known as non enzymatic browning
2021-12-20
Maillard reaction, also known as non-enzymatic browning reaction, is a complex chemical reaction between carbonyl groups of reducing sugars and free amino groups of amino acids, peptides, proteins or some other nitrogen containing compounds. Maillard reaction plays an important role in food industry
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Hippo signaling is unique in that it does
2021-12-20
Hippo signaling is unique in that it does not possess a cognate ligand and receptor system. Instead, numerous upstream sensors that monitor cell morphology, cell polarity, cell-cell contact, and mechanical stress impinge onto the Hippo pathway core kinases, MST, and LATS. This in turn indicates the
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br Hh Proteins at a Glance
2021-12-18
Hh Proteins at a Glance Hh family proteins are evolutionarily conserved morphogens that provide cells with positional information and fate instruction during early embryonic development. After development, Hh ligands contribute to tissue homeostasis and wound healing 1., 2.. Consistent with these
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Chronic exposure of cells to cytotoxic drugs can
2021-12-18
Chronic exposure of cells to cytotoxic drugs can result in the selection of multiple phenotypic and genetic changes. Thus, the use of MCF7/VP cells, which were selected for resistance to VP-16, was potentially problematic. However, a thorough characterization of MCF7/VP cells demonstrated that they
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Pharmacologic approaches of inhibiting GSNOR
2021-12-18
Pharmacologic approaches of inhibiting GSNOR activity have reached the point of clinical development with the recent announcement of the first cystic fibrosis patients treated with the first-in-class GSNOR inhibitor, N6022 (N30 Pharmaceuticals). Clinical development is ongoing for other indications
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dna-pkcs br Experimental br Results and discussion br Conclu
2021-12-18
Experimental Results and discussion Conclusion In the current work, a novel method for separation and preparation of flavonoid glycosides from L. chinensis was successfully developed using a 2 D-HILIC × RPLC system based on a zwitterionic Click XIon column and a polar-modified Atlantis T3 c
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fluvastatin In order to elucidate the mechanisms
2021-12-18
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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Disrupting the dialog between microbiota and the
2021-12-18
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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