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The main function of ATR
2024-05-30

The main function of ATR/CHK1 signaling is activating GSK2656157 checkpoint arrest for S and G2 phases in mammalian cells. There are three checkpoints in response to DNA damage: G1/S, G2/M, and S-phase. The G2/M checkpoint can prevent cells that incur DNA damage in G2 phase or progress into G2 phas
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br Duality of interest br Contribution statement
2024-05-30

Duality of interest Contribution statement Acknowledgments Introduction Rapid, cell surface-initiated steroid actions have been reported for all major groups of steroid hormones and our understanding of membrane-mediated steroid actions has progressed rapidly over the last two decades. M
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Estradiol br Materials and methods br Results br Discussion
2024-05-30

Materials and methods Results Discussion The novel and central finding of the current study is that endothelial 12/15-LO rather than the monocytic/macrophagic 12/15-LO has a critical role in hyperglycemia-induced leukocyte adhesion and retinal endothelial barrier dysfunction. The following
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The binding of TQ to
2024-05-30

The binding of TQ to hsALDH changes the characteristic GW0742 spectrum of the enzyme. Therefore, TQ forms a complex with hsALDH and changes its absorption properties [39]. Ksv and Kb values indicate that the binding of TQ to hsALDH is very strong and of the order of static binding (complex formatio
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Derivatives of M that possess either
2024-05-29

Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these reboxetine mg to maintain 5-HTR antagonist properties as (+)-M100907 was demons
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Some alterations in the integrity
2024-05-29

Some alterations in the integrity of cell membranes caused by toxic agents can be determined by measuring certain enzymes released by damaged cells [8]. The cholinesterases, for example, catalyze the hydrolysis of Z-YVAD-FMK (ACh) in choline and acetic acid. Theses enzymes are divided into two type
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br Introduction Adenosine deaminase ADA also known
2024-05-29

Introduction Adenosine deaminase (ADA), also known as adenosine aminohydrolase, is a key enzyme involved in the purine metabolism that converts adenosine to inosine irreversibly (Lupidi et al., 1997). It is a zinc containing metalloenzyme present in both prokaryotes and eukaryotes. In humans ADA
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On the basis of the
2024-05-29

On the basis of the above information, we designed a new series of benzothiazole–piperazine derivatives (–) that have the aforementioned structural requirements (). Benzothiazole is an important ring system in the drug discovery studies of AD. There are several benzothiazole compounds that show pote
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In summary we could identify and experimentally
2024-05-29

In summary, we could identify and experimentally confirm two novel SBEs within the 5-LO promoter and we were able to demonstrate that TGFβ and SMADs stimulate 5-LO promoter activity. Moreover, an elevated 5-LO expression has been linked to different forms of leukaemia. Therefore, the influence of ML
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The combination of Aurora kinase
2024-05-29

The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the
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Receptor Subtypes and Their Function Critical Appraisal Larg
2024-05-29

Receptor Subtypes and Their Function – Critical Appraisal Largely unselective ligands of the benzodiazepine binding site, such as diazepam, are known to elicit a wide range of in vivo effects including hypnosis, sedation, anxiolysis, and muscle relaxation. Genetically modified mice were introduced
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Since obesity appears to impact leptin
2024-05-29

Since obesity appears to impact leptin and adiponectin levels in opposite manners, several studies have suggested that the serum adiponectin/leptin ratio may be a key parameter in indicating the relative risk of postmenopausal breast cancer (Ollberding et al, 2013, Cleary et al, 2009). Therapeutic s
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PF is orally bioavailable and has appropriate
2024-05-28

PF-06409577 is orally bioavailable and has appropriate pharmacokinetic properties for use in rodents, allowing us to evaluate its impact on lipid and cholesterol biosynthesis in vivo (Cameron et al., 2016). PF-06409577 lowered the incorporation of 14C-acetate into hepatic lipids in vivo in a dose de
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Besides its multiple peripheral effects adiponectin may amel
2024-05-28

Besides its multiple peripheral effects adiponectin may ameliorate insulin resistance by acting in the brain, and intracerebroventricular administration of adiponectin in rodents decreases body weight by stimulating energy expenditure [13]. Adiponectin most likely crosses the blood-CSF-barrier (BCB)
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We have previously shown that the human gonadotropins
2024-05-28

We have previously shown that the human gonadotropins hLH and hCG trigger a partly irreversible stimulation of intracellular cyclic AMP accumulation in mouse Leydig Tumor Toremifene synthesis (MLTC) in contrast to all other tested mammalian LHs and CG (Klett et al., 2016). In order to get a better i
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