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br Regulation and pharmacology of mPGES
2023-07-20

Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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The introduction of a pyrazole moiety into any position of
2023-07-20

The introduction of a pyrazole moiety into any position of the sterane core by cross-coupling reactions [13] or by Knorr construction from a CCC bis-electrophilic sterane precursor and an N,N binucleophile building block [17], [19] may serve as an example. Very few reports are to be found, however,
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Many metalloenzyme inhibitors consist of two chemical compon
2023-07-20

Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino Retapamulin residues that form the substrate-binding site of the metalloenzyme. The MGB is of
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An AXL decoy receptor with enhanced
2023-07-20

An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer casein kinase 2 inhibitor and a murine breast cancer cell line in graftin
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terbinafine hydrochloride The ATX LPA signaling axis has bee
2023-07-20

The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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Defining the multiple roles of
2023-07-20

Defining the multiple roles of autophagy in stroke has been a rapidly evolving and exciting venue for translational research, with innovative products being applied from bench to bedside. Spanning pharmacological pathway manipulation and functional experimental validation, altered autophagy activati
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For these reasons the role played by
2023-07-20

For these reasons, the role played by autophagy in environmental neurotoxicity is not always easily determinable. Indeed, although the neuroprotective role of autophagy has been shown by several studies, sometimes induction of autophagy was associate with deleterious effects (Glick et al., 2010, Sri
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AP activation is known to upregulate downstream
2023-07-20

AP-1 activation is known to upregulate downstream target genes including Alfacalcidol D1, c-myc, Bcl-xl, MMP-9, EGFR, and specific miRNAs that are involved in progression and metastasis of tumors. Moreover, matrix metalloproteinase-2 has been shown as a downstream gene of AP-1, triggered by 15-HETE
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A high throughput screening campaign led to
2023-07-20

A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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Estrogen exerts its genomic action via estrogen nuclear
2023-07-20

Estrogen exerts its genomic action via Chaetocin nuclear receptor: ERα and ERβ. The distribution of ERα and/or ERβ positive neurons in CNS of different species has been mapped extensively by various methods [41], [42], [43], [44], [45], [46], [47], [48], [49], [50], although there are some differen
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br Conclusion br Acknowledgments The authors extend
2023-07-20

Conclusion Acknowledgments The authors extend their appreciation to Kayyali Chair for Pharmaceutical Industry, Department of Pharmaceutics, College of Pharmacy, King Saud University for funding this work through the research project Number (G-2016-2). Introduction L-ornithine is a natural
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Varenicline Tartrate Mass spectrometry Matrix assisted laser
2023-07-20

Mass spectrometry. Matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) MS experiment was performed in linear and positive-ion mode on a DE-STR instrument equipped with a nitrogen laser (PE Biosystems, Foster City, CA). Each spectrum was calibrated in the default mode in which 0.1%
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We have shown that an extensive region in
2023-07-20

We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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Although the interactions of PhLP with G and its other
2023-07-20

Although the interactions of PhLP with Gβγ and its other partners have been convincingly documented through in vitro studies, it is not clear how PhLP controls chk1 signaling in vivo. C. elegans provides a powerful genetic model to analyze Phosducin function and study its interacting partners in si
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Animal fat appears to increase C perfringens counts compared
2023-07-20

Animal fat appears to increase C. perfringens counts compared with vegetable oil, so there may indeed be some advantage to vegetable diets at least in terms of fat sources (Knarreborg et al., 2002). Small grains such as wheat, rye, oats, and barley, with high levels of non-starch polysaccharides are
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