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Substitutions on the benzene ring of the phenyl acetic
2020-11-19

Substitutions on the benzene ring of the phenyl acetic beta lactamase moiety were evaluated to study their effect on DP and CRTH2 selectivity (). Compound has strong affinity for CRTH2, but it only has moderate affinity for DP. Small substitutions such as methoxy () and fluorine () next to the ary
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br Results and discussion Compounds were tested for their bi
2020-11-19

Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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Recent data obtained with etifoxine
2020-11-19

Recent data obtained with etifoxine suggest that facilitation of GABAergic inhibition may be also associated with an indirect mechanism implying activation of the peripheral benzodiazepine receptor with a subsequent increase in neurosteroid production (Schlichter et al., 2000, Verleye et al., 2005).
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Introduction The carnitine choline acyltransferase
2020-11-19

Introduction The carnitine/choline acyltransferase family is a family of enzymes that play diverse roles, ranging from (the regulation of) MMP-2 Inhibitor I synthesis and fuel metabolism in mitochondria and peroxisomes to the generation of the neurotransmitter acetylcholine. In mammals, this famil
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In contrast to PEGylated proteins which tend to have reduced
2020-11-19

In contrast to PEGylated proteins which tend to have reduced Spectinomycin hydrochloride hydrate in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applic
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One of the therapeutic proteins used in cancer
2020-11-19

One of the therapeutic proteins used in cancer therapy is glucarpidase, also known as Carboxypeptidase G2, CPG2, which originates from the bacterium Variovorax paradoxus (old name, Pseudomonas sp. strain RS-16). It has no mammalian equivalent (Thompson et al., 1994; Kamlage, 1994) and is a zinc-depe
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In the current study although
2020-11-19

In the current study, although EP4 agonist was the most effective in relaxing corpus cavernosum, it did not affect the neuronally-mediated relaxation. On the other hand, both alprostadil and iloprost, which were less effective as direct relaxants, potentiated EFS-induced relaxation of rat corpus cav
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Previously published data showed an interaction of tubulin a
2020-11-19

Previously published data showed an interaction of α-tubulin and CK1δ [15] that was validated in the present study using SPR (Fig. 1A). The dominant motifs involved in the CK1δ/α-tubulin interface were defined using a peptide library of peptides covering the CK1δ amino SB 525334 sequence (Supplemen
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The N B method has the overall advantage that it
2020-11-19

The N&B method has the overall advantage that it is not restricted to certain dyes specific for energy transfer [55], and is also able to detect higher order receptor LY294002 on the focal point in living cells. Conclusion The N&B method has shown to be a powerful tool to locate and quantify the
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br Conclusion br Declaration of interest br Introduction
2020-11-19

Conclusion Declaration of interest Introduction Glyphosate [N-(phosphonomethyl)glycine] is the main active ingredient in one of the most widely used herbicides in the world. The commercially used concentrations of glyphosate range from 1% for domestic use to 41% for conventional agricultura
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Another important consideration with respect to drug conditi
2020-11-18

Another important consideration with respect to drug conditioning suggested by the present findings is the observation of an attenuated BEC on the second extinction trial. Seemingly, if ERK measurements were made following a partial reduction in the conditioned response the ERK response would prese
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br A major physiological action of ET is to function
2020-11-18

A major physiological action of ET-1 is to function as one of the most powerful vasoconstrictors of human blood vessels. As such, ET-1 plays a major role in regulating vascular function in all organ systems, including the kidney (Fig. 1). As in other vessels, ET-1 is thought to be released from en
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Among the high value compounds derived from agricultural res
2020-11-18

Among the high value compounds derived from agricultural residues there are enzymes with industrial application. The extraction processes have been focused on the development of new strategies that guarantee high recovery rates with maximum activity (Nadar et al., 2017). The residues of these two fr
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Moreover Hypericum perforatum L was also included in the
2020-11-18

Moreover, Hypericum perforatum L. was also included in the initial screening, showing only a weak percentage of inhibition on both enzymes. In fact, it was not selected among the most active plants. The phytochemical profiles of these three Hypericum species were already reported to be significantly
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btk inhibitor hnRNP E functions in a number
2020-11-18

hnRNP E1 functions in a number of mRNA regulatory processes including transcription [74], [75], splicing [7], [74], [76], [77] and translation [6], [8], [69], [78], interacting with RNAs through CU rich regions such as the differentiation control element (DICE) and the TGFβ activated translation (BA
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