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The phenolic hydroxyl group of ezetimibe tolerated various s
2021-04-29

The phenolic hydroxyl group of ezetimibe tolerated various structural modifications (disaccharide, carboxyalkyl and glucuronide) that retained inhibitory activity.13, 14, 15 We conjugated glycylglycine to phenolic hydroxyl group and synthesized ten 1H-pyrrole-2,5-dione derivatives 14a-j successfully
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br Target enzyme attributes and substrate peptide
2021-04-29

Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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It is currently believed that acute morphine administration
2021-04-29

It is currently believed that acute morphine administration can impair learning and memory (Friswell et al., 2008). Chronic morphine treatment can also impair access to and retention of spatial memory (Spain and Newsom, 1991, Zheng et al., 2002). Using the Morris water maze experiment, we have previ
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br Introduction As a strong analgesic morphine is
2021-04-29

Introduction As a strong analgesic, morphine is often used to treat acute and chronic pain. However, morphine is a substance with low lipid solubility that slowly enters the nerve tissue through the blood–brain barrier and produces neurotoxicity. Morphine-induced neurotoxicity can be produced aft
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br Discussion The biochemical separation of
2021-04-29

Discussion The biochemical separation of exonuclease activity from DNA-PK dependent endonuclease activity reported in this manuscript is consistent with genetic separation of Artemis enzymatic activity. Mutations in the protein which result in disruption of endonuclease activity have no effect on
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DHODH activity has been traditionally measured
2021-04-29

DHODH activity has been traditionally measured with the standard colorimetric assay that monitors 2,6-dichloroindophenol (DCIP) reduction as absorbance decrease at 600 nm . This assay has permitted the identification of several families of DHODH inhibitors in a successful high-throughput screening (
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Here we were able to show for the first time
2021-04-29

Here, we were able to show for the first time that stimulation of VSMCs with two different growth factors resulted in a dramatic decrease in gp130mRNA expression occurring four to six hours after stimulation with Ang II and PDGF-BB. The mRNA level remained extremely low within 12 hours after stimula
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CYP A is involved in the metabolism of approximately of
2021-04-29

CYP3A is involved in the metabolism of approximately 50% of all drugs that are currently prescribed to patients [1], [15], [16]. Marked interindividual variabilitity of the catalytic function for metabolizing CYP3A substrates has been demonstrated with variability exceeding 20-fold [1]. Levonorgestr
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2021-04-29

Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase Diperodon HCl receptor [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tum
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It has been reported that NMDA receptor hypofunction upregul
2021-04-29

It has been reported that NMDA receptor hypofunction upregulates the expression of immediate early genes in several boc boc regions [39], [40]. Consistent with this finding, we demonstrated that MK-801 increased the number of c-Fos-positive cells in the PVN and PC/RS (Fig. 5). Importantly, the MK-80
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Other mutations in the SYNE region exons
2021-04-29

Other mutations in the SYNE1 3′ region (exons 81–85) have been implicated in an upper motor neuron disease, ARCA1 (Gros-Louis et al., 2007). The disease is characterized by progressive movement, coordination, and balance problems caused by disrupted Purkinje cell function and their impaired signalin
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br Conclusion This patient was hypercoaguable as evidenced b
2021-04-28

Conclusion This patient was hypercoaguable as evidenced by a lower extremity DVT, pulmonary emboli, and a splenic infarct. Excluding acute CMV infectious mononucleosis, she had no disorders predisposing to splenic infarcts.4, 5 In this case, CMV infectious mononucleosis was accompanied by CMV lun
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The mechanism by which OC
2021-04-28

The mechanism by which OC use leads to impaired glucose tolerance is yet to be fully clarified. Decreased insulin sensitivity appears to be mainly accounted for by estrogenic component and this effect may be modified by progestogenic component [14], [15]. Estrogenic effect on glucose tolerance has b
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Damage of PE HD due to both
2021-04-28

Damage of PE-HD due to both mechanisms is usually considered to emerge from a local stress concentration in the material, leading to the initiation of a crack, which subsequently propagates further through the material, and finally leads to macroscopic failure. In this process, crack growth occurs o
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Within the X CX PX RX motif of several
2021-04-28

Within the X1CX3PX5RX7 motif of several prokaryotic FGE substrates, the residues of X3, X5, and X7 are variably found as mixtures of alanine, glycine, threonine, or serine residues [26], [27]. The docked model of our identified HCTPRRP motif revealed that position X1 (H1) and position X7 (P7) were n
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