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Therefore the rational design of target
2023-08-29

Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site
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EPSP analogs were retrieved from PubChem database and
2023-08-29

EPSP analogs were retrieved from PubChem database and docking procedure yielded about eight best binding analogs (Fig. 10). The selected molecules were further assessed for their theoretical Ki values using AUTODOCK software version 4. The predicted binding efficiency of retrieved analogs was estima
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br Future directions outlook Peptide based
2023-08-29

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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The advantage of active immunotherapy is long term
2023-08-29

The advantage of active immunotherapy is long-term antibody production from short-term drug administration at limited cost. Conversely, immune response may be inconsistent or lacking, especially in older individuals, and adverse reactions—if immunologically based—may also be long-lasting. Initial ex
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Evidence shows that glial activation increases
2023-08-29

Evidence shows that glial activation increases the expression of cytokines and chemokines in Parkinson's disease, which precede the degeneration of the substance nigra (Halliday and Stevens, 2011, Tansey and Goldberg, 2010). The use of non-steroidal anti-inflammatory drugs (except aspirin) can preve
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AMP activated protein kinase AMPK is a key
2023-08-29

AMP-activated protein kinase (AMPK) is a key cellular energy sensor that maintains energy homeostasis at the cellular and whole-organism level (Hardie et al., 2012). Functionally, the AMPK pathway sustains adenosine triphosphate (ATP) production through activation of fatty FTI 277 HCl oxidation and
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A previous study showed that miR c is involved in
2023-08-29

A previous study showed that miR-200c is involved in glucose-mediated pathological processes (Zhang, Guan, & Jin, 2017). Glucose metabolism is critical for the growth and proliferation of both normal GSK621 and cancer cells, and reprogramming glucose metabolism now has been considered as a target o
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According to their structures and substrate
2023-08-29

According to their structures and substrate specificity, MMPs are divided into five major groups: collagenases (e.g., MMP1), gelatinases (e.g., MMP2, MMP9), stromelysins (e.g., MMP3, MMP10), matrilysins (e.g., MMP7), and membrane-type MMPs [7]. Among them, MMP1 is a major collagenase that degrades t
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To validate the identified phosphorylation sites
2023-08-29

To validate the identified phosphorylation sites in the mouse heart, we analyzed HEK 293T glycyrrhizic acid transfected with Adrb1 based on the hypothesis that protein residues phosphorylated both in vivo and in vitro are more likely to be physiologically relevant. All of the phosphorylation sites
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Although the role of mossy
2023-08-28

Although the role of mossy fiber sprouting in epileptogenesis has been challenged (Elmer et al., 1997, Nissinen et al., 2001), in addition to astrogliosis, mossy fiber sprouting is one of the characteristic histopathological findings in TLE (Kharatishvili et al., 2006, Pitkanen et al., 2007, Represa
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Toxicity is the main reason
2023-08-28

Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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Regarding androgens it is known that they are also
2023-08-28

Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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br Regulation and pharmacology of mPGES mPGES kDa
2023-08-28

Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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Hypotaurine receptor We have previously shown that
2023-08-28

We have previously shown that the antinociceptive effect of tramadol, an analgesic that, like paracetamol is able to increase serotonin levels within CNS, is potentiated or antagonized respectively by a 5-HT1A/B nonspecific Hypotaurine receptor blockade or activation (Rojas-Corrales et al., 2000).
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br Disclosure statement br Acknowledgements The work was sup
2023-08-28

Disclosure statement Acknowledgements The work was supported by the National Science Foundation of China (Nos. 81273526, 81473268) and Natural Science Foundation of Colleges and Universities (Nos. KJ2017A197). What is already known What this article adds Introduction Sevoflurane is o
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