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The phylogenetic relationship demonstrates that both bovine
2024-12-10
The phylogenetic relationship demonstrates that both bovine and porcine 12/15-LO is more related to the human enzyme than the rabbit enzyme, despite the fact that the rabbit reticulocyte enzyme is a 15-lipoxygenase. The rabbit is one single species that expresses a 12/15 LO with 15-LO activity while
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Aromatization of the pyrrole ring
2024-12-10
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Growth inhibition assays are the
2024-12-10
Growth-inhibition assays are the most commonly used to identify antifungal small molecules. However, they have several facts that limit their use since many pathogenic fungi grow as filaments making difficult a correlation between growth and OD (optical density). They are not useful for identifying
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br Future directions outlook Peptide based macrocycles are a
2024-12-10
Future directions-outlook Peptide-based macrocycles are among the privileged scaffolds in antibiotic drug discovery. Many compounds were discovered by natural product screening and developed unchanged, or as semi-synthetic derivatizations. Since the golden age of antibiotic discovery (1940s-mid 1
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br AR mediated actions in cells of the vascular
2024-12-09
AR-mediated actions in Myriocin of the vascular wall Sex hormones may influence the size and composition of atherosclerotic lesions indirectly by modifying systemic cardiovascular risk factors such as plasma lipids profiles and insulin sensitivity; this aspect of their action is discussed elsewh
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We have recently begun to
2024-12-09
We have recently begun to demonstrate this concept by reporting a novel class of β-hairpin peptidomimetics, built on a piperidine-pyrrolidine semi-rigid β-turn inducer [12] and bearing two recognition pentapeptide sequences, designed on oligomeric and fibril structures of Aβ1-42 (compound 1, Fig. 1)
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Accumulating evidence indicates that experience dependent al
2024-12-09
Accumulating evidence indicates that experience-dependent alterations in glutamate transmission in the NAc, such as those produced by repeated exposure to cocaine, involve alterations in postsynaptic signaling mediated by AMPA-type receptors (Pierce and Wolf, 2013, Wolf and Ferrario, 2010). In the N
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Blockers will reduce perioperative myocardial ischemia and s
2024-12-09
β-Blockers will reduce perioperative myocardial ischemia and studies published in the 1990s suggested that their routine administration before surgery provided protection against perioperative CV complications.31., 32., 33. Based on these early studies, several national organizations endorsed the pe
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Adenosine receptors are proposed to
2024-12-09
Adenosine receptors are proposed to play proangiogenic role in vascular and immune EPZ 005687 receptor within microenvironment of hypoxic tissues to maintain tissue oxygenation in chronic ischemic condition [9]. Adenosine also stimulates the production of angiopoetin-1, VEGF and Interleukin-6 (IL6)
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Diabetes or inflammation is associated with up regulation
2024-12-09
Diabetes or inflammation is associated with up-regulation of A2AAR (Pang et al., 2010). High levels of A2AARs are found in macrophages and microglial cells that are poised, on activation, to abrogate the immune response (Trincavelli et al., 2008). In addition, hyperglycemia is associated with increa
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Recently several groups including ours have started to use t
2024-12-09
Recently, several groups, including ours, have started to use the C. elegans multi-dendritic PVD neurons as a model system to dissect the molecular mechanisms of dendrite development. During larval development, PVD elaborates complex and stereotyped dendritic arbors by sequentially adding primary (1
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A variety of quinazoline or fused pyrimidine
2024-12-09
A variety of quinazoline or fused pyrimidine-substituted diaminotriazoles showed sub-100nM inhibition of Axl (). Diaminotriazoles similarly substituted with quinolines, isoquinolines and benzothiazoles also showed potent Axl activity (data not shown), but generally exhibited potent cytotoxicity and
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Docking studies were performed on the selected
2024-12-09
Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-838
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br Materials and methods br
2024-12-09
Materials and methods Results Discussion We have developed a high-throughput functional genomic screen that allows the identification of genes that confer drug resistance. Several factors have been identified which must be taken into account to develop a reliable screen. In particular, cons
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Autocrine regulations of several adipokines
2024-12-07
Autocrine regulations of several adipokines (e.g., leptin and resistin) on adipocytes have been reported (Karastergiou and Mohamed-Ali, 2010, Ye et al., 2010). Several lines of evidence have shown that apelin influences adipocyte functions, such as, lipolysis and glucose uptake (Dray et al., 2008, Y
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