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Nowadays more than kinases have been identified of
2024-08-17
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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To identify the kinase s
2024-08-17
To identify the kinase(s) mediating H3.3S31 phosphorylation, we devised a 96-well-plate-compatible immunostaining assay, with PX-478 2HCl specific for H3.3S31ph, and utilized it to screen both a Qiagen siRNA library covering 720 human kinases and a kinase inhibitor library (Selleck) containing 194
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Introduction Mitotic kinases play an essential role in mitos
2024-08-17
Introduction Mitotic kinases play an essential role in mitosis, Aurora and other mitotic kinases are often observed over-expression in human solid and many hematologic cancers. As one of serine/threonine kinases, Aurora kinase family is involved in centrosome maturation, mitotic spindle formation,
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br ACL Inhibition Lowering Blood LDL C to Reduce ASCVD
2024-08-17
ACL Inhibition: Lowering Blood LDL-C to Reduce ASCVD Risk Given its strategic position in the lipid biosynthesis pathway, ACL has been considered an attractive target for lipid-lowering even before statins and their effects on cholesterol homeostasis were elucidated (Box 2). Cells carefully maint
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N6-Methyl-ATP The use of FTAI can overcome the
2024-08-17
The use of FTAI can overcome the negative impact of low estrus detection efficiency, but implies effective synchrony of luteal function as well as synchronous growth and ovulation of a viable N6-Methyl-ATP follicle. Pregnancy rates obtained with FTAI may be comparable or better than those obtained
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Plasma apelin levels predict the major cardiovascular event
2024-08-17
Plasma apelin levels predict the major cardiovascular event after percutaneous coronary intervention in patients with ST elevation myocardial infarction (STEMI), and adverse events are higher in patients with lower plasma apelin levels [75]. Apelin and its receptor are markedly upregulated in the he
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br The role of apelin
2024-08-17
The role of apelin in respiratory diseases At present, several scientific studies have suggested that the apelin/APJ system may play an important role in the development of pulmonary diseases (Table 4). For example, in an experiment on rats suffering from acute lung injury, apelin-13 decreases th
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br Telmisartan Telmisartan is one of the widely used antihyp
2024-08-16
Telmisartan Telmisartan is one of the widely used antihypertensive agents, which has demonstrated favorable safety and tolerability profiles, both alone and in combination therapies. It has a number of pharmacological properties that distinguish it from other ARBs—the longest plasma half-life, hi
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br Introduction Metabolic cues are crucial inputs in dictati
2024-08-16
Introduction Metabolic cues are crucial inputs in dictating acute responses through governing cellular signaling pathways as well as in shaping up long-term transcriptional and epigenetic profiles to control chronic cellular responses (Lu and Thompson, 2012). It has been well documented that meta
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The G R mutation is
2024-08-16
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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label rna br Materials and Methods br Results In
2024-08-16
Materials and Methods Results In the Base Analysis (53% of patients having access to the ALK test in both Current and Alternative Scenarios), a total of 16,583 patients were tested of whom 1,252 were assumed to be ALK-positive. A more extensive use of Ventana in the Alternative Scenario determ
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Flavonoids protein interactions studies play a substantial p
2024-08-16
Flavonoids-protein interactions studies play a substantial part in the hunt for novel molecules which are to interact with a selected disease-relevant target [35]. The mode of potential interaction gives information about the flavonoid effectiveness and selectivity. Lately, possible target molecules
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The cavity volume of the binding pocket
2024-08-16
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino colorimetric assay synthesis substitution within a binding pocket may result in a change in the cavity volume. This
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The putative physiological meaning of epinephrine
2024-08-16
The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of
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APPL was the first adaptor protein identified that interacts
2024-08-16
APPL1 was the first adaptor protein identified that interacts directly with adiponectin receptors [18]. A two-hybrid study by Dong and colleagues revealed that the C-terminal extracellular domain of AdipoR1 interacts with adiponectin, whereas the N-terminal cytoplasmic domain of AdipoR1 interacts wi
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