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Alogliptin As a part of our continuing efforts towards disco
2022-03-04

As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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A great number of proteins entering
2022-03-04

A great number of proteins entering the nucleus possess a characteristic nuclear localization sequence (NLS) in their primary structure. One of such sequences is the KKKGK motif [30]. It is present in all known muscle (but not liver – except human liver) FBPase sequences (human, rabbit, rat and mous
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To identify genes with significant expression differences we
2022-03-03

To identify genes with significant 5-Carboxymethylester-UTP differences, we performed differential gene expression analysis between the two individuals with TRRAP variants (combined as biological replicates) and two unaffected controls. Gene ontology (GO) enrichment analysis of these genes with the
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YAP TAZ nuclear function is also influenced by
2022-03-03

YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 xanthine oxidase inhibitor exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits
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Propranolol HCl Similarly towards the acylsulfamoyl benzoxab
2022-03-03

Similarly, towards the 5-acylsulfamoyl benzoxaboroles, the boronate intermediate was prepared according to , while the boronate , an intermediate towards 4-acylsulfamoyl benzoxaboroles, was prepared according to . The sulfonamides and used in the synthesis were made from the starting sulfonyl chlori
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The isoenzyme hGSTP is an attractive
2022-03-03

The isoenzyme hGSTP1-1 is an attractive drug target due to its high levels of disease association (target validation) and druggability (target tractability) properties [5,6,[17], [18], [19], [20], [21]]. hGSTP1-1 functions as a homodimer protein [18]. Each monomer has two domains, an α/β domain (N-t
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The GPR receptor is also emerging as an important therapeuti
2022-03-03

The GPR55 receptor is also emerging as an important therapeutic target. GPR55−/− mice possess no overt phenotype, but were protected in models of inflammatory and neuropathic pain (Staton et al., 2008). Staton et al. (2008) reported that no GPR55 mRNA could be detected by RT-PCR in the animals. Also
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In the present study we found that the expression of
2022-03-03

In the present study, we found that the expression of GPR120 in decidua from women of spontaneous abortion was significantly downregulated compared to the decidua from that of normal pregnancy. Moreover, GPR120 deletion (GPR120−/−) or inhibition predisposed mice to LPS or RU486 induced abortion, ind
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More recently several groups have characterized a role for G
2022-03-03

More recently, several groups have characterized a role for GPR120 signaling via omega-3 fatty acids in amelioration of alcoholic hepatic injury and non-alcoholic fatty liver disease (NAFLD) [18], [19]. Nakamoto et al. demonstrated protective effects of the omega-3 fatty limonin mg docosahexaenoic
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GW was also the starting point for a
2022-03-03

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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br Introduction Verticillium dahliae Kleb is
2022-03-03

Introduction Verticillium dahliae (Kleb.) is a soil-borne fungal pathogen that is able to infect hundreds of plant species, and causes vascular wilt disease [1], [2]. In nature, the infection of V. dahliae initiates from the germination of resting structures called microsclerotia [3]. The germina
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This resembles a vicious cycle since BBB
2022-03-03

This resembles a vicious cycle since BBB disruption and inflammation are thought to be caused by epilepsy, but other contributing factors are also known to be their cause, such as peripheral infection, autoimmunity, rotenone trauma and stroke that also underlie epilepsy [18]. Additional triggers th
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Long non coding RNAs lncRNAs are mRNA
2022-03-03

Long non-coding RNAs (lncRNAs) are mRNA-like transcripts of greater than 200 nucleotides (nt), with little or no protein-coding potential [13,14]. LncRNAs have been suggested to participate in transcription and post-transcription regulation as scaffolds, guides, decoys or repressors, activators, and
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br GLP R expression in the vascular endothelium Immunohistoc
2022-03-02

GLP-1R expression in the vascular endothelium Immunohistochemistry studies utilizing GLP-1R antibodies that have now been demonstrated to be non-specific [46], initially identified GLP-1R protein expression in both mouse mesenteric artery SMCs and heart coronary SMCs [7]. However, evidence for VS
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Although GLP has greater insulin releasing effects at pharma
2022-03-02

Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts
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