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A high throughput small molecule ACK biochemical inhibition
2024-12-10

A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found ISRIB to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perfor
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br Perspectives Given the complexity of the
2024-12-10

Perspectives Given the complexity of the cellular interactome and of protein scaffolding, further progress in revealing how individual membrane proteins, including APP and AChE, interact with each other at various levels, from cell-surface shedding to gene regulation, will clarify some intrinsic
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The following are the supplementary data related to
2024-12-10

The following are the supplementary data related to this article. Conflict of interest Acknowledgements Disclosure of interest Introduction Since the introduction of platinum-based chemotherapy, metastatic testicular cancer has become a curable disease and most testicular cancer patient
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br Cytochrome b br Cytochrome P hydroxylase lyase P
2024-12-10

Cytochrome b5 Cytochrome P450 17α-hydroxylase/17,20-lyase (P450 17A1) A number of P450s involved in steroid biosynthesis are multifunctional as they carry out two or more sequential hydroxylation reactions on the same substrate(s). P450 17A1 is a dual function endoplasmic reticulum enzyme enco
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NOXA a BH only protein is best
2024-12-10

NOXA, a BH3-only protein, is best known as a selective inhibitor of MCL-1, which is a highly expressed pro-survival protein in many human malignancies [30]. In addition, NOXA was recently proven to act as a direct activator via directly binding to BAX to induce apoptosis [31]. Given that its levels
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Song et al reported series
2024-12-10

Song et al. reported series of 1,2,3-triazolylsalicylamide derivatives and screened over kinase panel and found compound 31 as most potent which inhibited Aurora-A, specifically with IC50 of 0.37 μM. Compound 31 was about 10-fold more active for Aurora-A than for Aurora-B (IC50 = 3.58 μM reported se
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When skeletal muscle ages there is an increase in
2024-12-10

When skeletal muscle ages, there is an increase in frailty, which is coincident with a decrease in muscle mass and function—this condition is called sarcopenia (Cruz-Jentoft et al., 2010). It has been shown that one of the major pathways downregulated at the onset of sarcopenia is the mitochondrial
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br Leptin Adiponectin a permissive imbalance Leptin
2024-12-10

Leptin/Adiponectin: a permissive imbalance Leptin, a satiety hormone, is encoded by the obesity (ob) gene. It essentially functions as an energy sensor which is involved in the regulation of body weight by sending signals to the Sildenafil Citrate receptor to reduce appetite (Woods and D'Alessio,
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Ibandronate sodium ARG I is one of
2024-12-10

ARG I is one of the most important mammalian enzymes responsible for nitrogen metabolism since it comprises the main route for the elimination of excess nitrogen resulting from amino Ibandronate sodium and nucleotide metabolism [18]. ARG I deficiency leads to hyperargininemia, characterized by prog
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glycoprotein iib iiia inhibitors Furthermore to address the
2024-12-09

Furthermore, to address the concern that the observed positive in vitro activity results might be stymied by the propensity of such assays to display false positives due to the inherent noxiousness of the tested compounds, all analogs were evaluated against Vero cells in an MTT assay. Some of the mo
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Mechanistically NAergic signaling in the VTA modulates neuro
2024-12-09

Mechanistically, NAergic signaling in the VTA modulates neuronal activity presumably via α1-AR. The majority of α1-ARs are found in the VTA are located presynaptically on unmyelinated BD 1047 dihydrobromide synthesis and axon terminals of glutamatergic and GABAergic neurons. However, α1-ARs are als
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Our studies suggest that AdipoR
2024-12-09

Our studies suggest that AdipoR1 and AdipoR2 genes are expressed in multiple tissues in the chicken wherein both receptors are likely to mediate the physiological effects of adiponectin. We determined the relative expression of AdipoR1 and AdipoR2 mRNA in various tissues and found that skeletal musc
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AdipoRon acts on the anti
2024-12-09

AdipoRon acts on the anti-diabetic effects of adiponectin, exhibiting its effect through the activation of AMPK and PPARα pathways via AdipoR1 and AdipoR2, respectively [23]. AdipoR activation is a promising treatment for diabetes, nonalcoholic fatty liver disease, and cardiovascular disease, demons
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Lipotoxicity is the accumulation of excess
2024-12-09

Lipotoxicity is the accumulation of excess lipids in non-adipose tissues that leads to cell dysfunction or cell death. It may play an important role in the pathogenesis of diabetes, and contributes to the rate of progression of CKD [7,8]. Emerging evidence indicates that renal lipid dysregulation is
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hydroxydopamine OHDA is a selective catecholaminergic neurot
2024-12-09

6-hydroxydopamine (6-OHDA) is a selective catecholaminergic neurotoxin mainly used to generate lesions in the nigrostriatal pathway in rats (Ungerstedt, 1968). The most common use of 6-OHDA is via unilateral injection into the rat medial forebrain bundle (MFB). DA depletion, nigral DA cell loss, and
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