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Despite hydrolysis with commercial enzymes like trypsin peps
2024-12-05
Despite hydrolysis with commercial enzymes like trypsin, pepsin, Alcalase, Flavourzyme and Thermolysin have been used to digest parent proteins and generate peptides, microbial fermentation by proteolytic species has also proved to be a successful strategy (Fakhfakh et al., 2013, Jemil et al., 2016,
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br Conclusion There have been multiple
2024-12-05
Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi
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In conclusion we have designed and synthesized a series of
2024-12-05
In conclusion, we have designed and synthesized a series of 4-phenyl-thiazole analogues as potent ATX inhibitors. Total twenty-five compounds were synthesized and evaluated for their inhibitory activity on ATX using FS-3 and human plasma assays. Compound was found to be the most potent derivative pr
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br Conflicts of interest br Financial support This
2024-12-04
Conflicts of interest Financial support This work was supported by grants from the Fondazione Cariplo [Grant number 2011-0463] (Carini); and by Funds for Original Research of the Università del Piemonte Orientale (2016, Project: Carini-Boldorini). The sponsors had no involvement in study desig
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NLX a k a F or befiradol exhibits
2024-12-02
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in JQ1 to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017). Additionally, it has shown
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We aim to evaluate the AK in regulating
2024-12-02
We aim to evaluate the AK in regulating adenosine signaling in the retina. It was reported that the degree of bethanechol chloride injury directly depends on expression levels of AK and the resulting extracellular levels of adenosine (Boison, 2006). Indeed, transgenic mice overexpressing AK are hig
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The purpose of the present
2024-12-02
The purpose of the present study is (1) to characterize AChE from the monogonont B. koreanus and to analyze the modulation of the AChE activity and its transcription level after exposure to six pharmaceuticals, (2) to evaluate the usefulness of AChE as a molecular biomarker upon pharmaceutical expos
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NSAIDs induce gastrointestinal toxicity and evoke asthma by
2024-12-02
NSAIDs induce gastrointestinal toxicity and evoke Protease Inhibitor Cocktail (100X in DMSO, EDTA plus) by decreasing the production of gastroprotective prostanoids and by redirecting the COX substrate AA into LT biosynthesis, thereby causing vasoconstriction in gastric mucosa and airways (Celotti
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Based on the observation that antipsychotic drugs increase H
2024-12-02
Based on the observation that antipsychotic drugs increase 5-HT1A–D2 heteromerization level (Łukasiewicz et al., 2016), we set out to compare the effect of paroxetine to that of risperidone. Paroxetine, a potent SSRI, is very effective in the treatment of depression and anxiety disorders, e.g., gene
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Subsequently Palvimaki et al corroborated Ni and Miledi s st
2024-12-02
Subsequently, Palvimaki et al. (1999) corroborated Ni and Miledi's study by demonstrating that treatment with fluoxetine leads to 43% occupancy of the 5-HT2C receptors. Moreover, the affinity of fluoxetine for 5HT2C receptors (Ki 65 nM) is close to its affinity for 5-HT transporters (Ki 33 nM) (Ni a
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br Funding br Ethics br Conflict of interest br
2024-12-02
Funding Ethics Conflict of interest Acknowledgements Introduction Hepatic fibrosis occurs in response to different etiologies of chronic liver injury, which is mainly accompanied by pathological ic omeprazole of excessive extracellular matrix (ECM) of the liver, as the common reactio
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Ryoichi et al modified potent clinical candidate VX with
2024-12-02
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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In bacteria H gler et al Kanao
2024-12-02
In bacteria (Hügler et al., 2007, Kanao et al., 2001), a glaucophyte alga (Ma et al., 2001), green algae/land plants (Fatland et al., 2002), and filamentous fungi (Nowrousian et al., 2000), ACL enzyme activity requires ACLA, and ACLB (referred to here as dual-subunit ACL, or dsACL) (Kanao et al., 20
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br Introduction Lipoxygenases LOXs are
2024-12-02
Introduction Lipoxygenases (LOXs) are a heterogeneous family of enzymes that catalyze the peroxidation of polyunsaturated fatty acids (PUFAs). By oxidizing free PUFAs, they were shown to contribute to the generation of various bioactive lipid mediators. However, LOX-mediated oxidation of PUFAs es
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On the other hand there were only a
2024-12-02
On the other hand, there were only a few cases that expressed DA2R in our study. Additionally, in the cases whose ACTH-secreting pituitary adenomas expressed DA2R, the ratio of positive staining bicuculline was very low. This suggests that dopamine agonists may be less effective in canine Cushing's
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