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We first set out to
2021-12-15

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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Previous studies showed that pregnancy rate
2021-12-15

Previous studies showed that pregnancy rate improves when ewes have a BCS that exceeds a minimum threshold [43]. The pregnancy rate is increased in sheep with BCS ≥2.5 [44] and >2 [45]. In this work, pregnancy rate was higher in the GnRH group with low BCS compared to the hCG and Control groups. Des
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br Introduction Edible bird s nest EBN known as the
2021-12-15

Introduction Edible bird's nest (EBN), known as the health and precious food, is produced from the saliva secretion of several different swiftlet species. Researches have shown the nutritional value of the EBN with the containing of glycoproteins, carbohydrates, essential amino acids, minerals an
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Latrunculin B To date glycine receptors have been found in f
2021-12-15

To date, glycine receptors have been found in five distinct transmembrane protein subunits (one β subunit and four α subunit (α1–α4)), combining to form two different types of functional receptors [4], [14], either α homomeric, the immature extrasynaptic glycine receptor subtype, or αβ heteromeric,
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In the present study co administration of TM AT receptor
2021-12-15

In the present study, co-administration of TM (AT1 receptor blocker) and PD (AT2 receptor blocker) were made in ischemic mice to explore the significance of AT2 receptors in cerebral ischemia while blocking central AT1 receptors. Also to prove that AT2 receptors should be free after ischemic injury
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The highest metabolic stability observed for compound k
2021-12-15

The highest metabolic stability observed for compound 4k (EC50=0.41μM corresponding to 218ng/mL) among the four selected frontrunner candidates was the principal decisive point in nominating this compounds for pharmacokinetic characterization in mice at the dosage of 10mg/kg (administered intravenou
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br Introduction Isoprenoid structures play an essential role
2021-12-14

Introduction Isoprenoid structures play an essential role in biology and over 30,000 natural products of this class are known (Greenhagen et al., 2003). Like other animals, insects require these compounds for many disparate processes, including electron transport (e.g., ubiquinones), protein glyc
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More direct evidence of a role for Hat
2021-12-14

More direct evidence of a role for Hat1 in the acetylation of newly synthesized histone H4 has come from a number of recent studies that have shown that Hat1 is responsible for at least a portion of the acetylation that occurs on histone H4 lysines 5 and 12 in the pool of cytosolic histones. In chic
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Although no data exist on Ptc gene
2021-12-14

Although no data exist on Ptc52 gene Cyclosporine in other plant species, the expression pattern presented in this study shows perceptibly low levels of transcript accumulation in tomato seeds and roots, low levels in the stem, flower and green fruit, and high levels in the leaves. This coincides w
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Gp induces cell death by apoptotic mechanisms and increases
2021-12-14

Gp120 induces cell death by apoptotic mechanisms and increases intracellular Ca, and activates messengers related to cell death. Intracellular mechanisms of neuronal damage are mainly a consequence of the activation of the N-methyl-d-aspartate receptor (NMDAR) [2], [5], which induces excitotoxicity
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At the second step blind docking simulation of
2021-12-14

At the second step, blind docking simulation of 150 independent runs was performed with smaller grid box. Structures of open (1v4t.pdb), semi-closed (4dch.pdb) and two structures of closed configuration of GK (pdb codes are 1v4s and 3vev) were used for simulation (for detailed explanations on can se
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Cys loop GABA receptors are well studied targets for insecti
2021-12-14

Cys-loop GABA receptors are well-studied targets for insecticides and also play an important role in nematode biology. These receptors are also targets for the anthelmintic piperizine (Accardi et al., 2012). The nematode GABA receptor most studied is the UNC-49 receptor which plays a role in muscle
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In summary P P macrocyclization
2021-12-13

In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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To identify structurally novel autophagy inhibitors a medium
2021-12-13

To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 sanguinarine stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automa
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Bupivacaine is one of the local anesthetics commonly used in
2021-12-13

Bupivacaine is one of the local anesthetics commonly used in spinal anesthesia. Previous studies had shown that bupivacaine induced neuronal apoptosis and axon degeneration among various neuronal populations in spinal cord, such as sciatic nerves and dorsal root 11-dUTP (DRG) neurons [5], [6], [7],
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