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The enzyme mediated ATP sensing mechanism in zebrafish can b
2025-03-01

The enzyme-mediated ATP-sensing mechanism in zebrafish can be compared with previous studies in other animal species reporting that enzymatic conversion of chemicals in the peripheral olfactory organ results in either “activation” or “inactivation” of odorants and pheromones. In male silkmoth, the a
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Tacrine an aminoacridine derivative Fig
2025-03-01

Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t
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Having established the structural requirements for potency i
2025-02-28

Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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br Methods br Results br
2025-02-28

Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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br Autophagy in cancer br Phytochemicals as a valuable
2025-02-28

Autophagy in cancer Phytochemicals as a valuable source of autophagy modulation agents Epidemiological studies demonstrated that there is a strong association between diet and human cancer mortality so that daily consumption of phytochemicals declines the incidence of different types of cancer
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The identification of novel kinase inhibitor scaffolds is hi
2025-02-28

The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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An alternative more rarely used
2025-02-28

An alternative, more rarely used, electron microscopy-based approach exploits labeling of phagosomes with DAMP (3-(2,4-dinitroanilino)-30-amino-N-methyldipropylamine). DAMP is a weakly basic compound which is membrane-impermeable once it has been protonated. This way, DAMPH+ accumulates in acidic in
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It has been shown that ACLY
2025-02-28

It has been shown that ACLY is localized to not only the cytoplasm but also the nucleus. Nuclear ACLY may supply acetyl-CoA for histone acetylation, leading to global regulation of the gene expression [16], [18]. We previously reported that AZ2 is also localized to both the cytoplasm and nucleus whe
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br Regulatory mechanisms of ASK activity
2025-02-28

Regulatory mechanisms of ASK1 activity The functions of ASK1 in disease ASK1 inhibitor As mentioned above, ASK1 plays a pivotal role in the pathogenesis of various diseases; hence, an ASK1 inhibitor has therapeutic potential. Although inhibitors of the ASK1 downstream kinases p38 and JNK ar
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Experimentally the ECD spectrum of showed three ECD
2025-02-28

Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because
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The habit of prescribing antibiotics just
2025-02-28

The habit of prescribing GDC-0068 “just-in-case” there is an infection is based on the misguided perception that antibiotics are “safe” drugs and therefore pose little risk to patients. Surgeons need to dispel this myth. In the outpatient setting, antibiotic-associated ADEs account for 19% of all e
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Sustained release property is also associated with side effe
2025-02-28

Sustained release property is also associated with side effects reduction [16] that could be confirmed by histopathological analyzes. Massive infiltrating inflammatory cells, hyperproliferation of skin layers and keratin pearls, caused by DMBA and croton oil application [32] are attenuated in Imq-lo
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Consistent with the in vitro results memantine ameliorated A
2025-02-28

Consistent with the in vitro results, memantine ameliorated Aβ-induced cytotoxicity in rat primary cortical cultures. Studies reported that memantine protected neurons against the damage caused by aggregated Aβ40 or Aβ42 oligomers in vivo[26], [27]. These results suggest that, in addition to its neu
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br The lipoxygenase pathway and microvascular complications
2025-02-28

The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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br Regulation of AHR Activity
2025-02-28

Regulation of AHR Activity AHR activity is regulated in various ways. First, AHR protein levels are controlled via ubiquitin-mediated proteosomal degradation: Ligand binding induces AHR ubiquitination and subsequent degradation by the proteasome [5]. AIP, a component of the AHR chaperone complex,
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