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Pyrimidine is the important pharmacology core in
2023-05-25
Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Alogliptin core as well
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Phagosomes acquire some hydrolases early during their
2023-05-25
Phagosomes acquire some hydrolases early during their journey from the cell surface to lysosomes. An example for such hydrolase is cathepsin H which is most concentrated in the early phagosome at a pH of approximately 6.3 (Claus et al., 1998), the pH optimum of enzyme activity (Schwartz and Barrett,
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In liver the essential organ of lipoprotein
2023-05-25
In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic CRA-024781 mg to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge bet
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The known crystal structures of class C GPCR VFTs
2023-05-25
The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S
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br Interaction between ASK and TRX Thioredoxins
2023-05-25
Interaction between ASK1 and TRX Thioredoxins are small (∼12kDa) dithiol oxidoreductases ubiquitously expressed in species ranging from plants to archaea and mammals. They perform various biological functions, such as reducing protein disulfide bonds, supplying reducing equivalents to redox GW966
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Human hepatocyte transplantation resulted in some animals
2023-05-25
Human hepatocyte transplantation resulted in some animals with relatively sparse repopulation while others had >90% of their liver containing human hepatocytes. The presence of circulating human albumin varied based on the amount of repopulation as the degree of humanization is reported to correlate
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br Acknowledgment This study was
2023-05-25
Acknowledgment This study was supported by Japan Society for the Promotion of Science Grants-in-Aid for Scientific Research (KAKENHI) [grant number 15K15031]. Introduction Glioma is the leading malignancy of astrocyte origin in the brain. The most aggressive, invasive, and destructive glioma
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The reduction of heterodimerization of KOR and
2023-05-25
The reduction of heterodimerization of KOR and APJ by both doses of apelin found in the present study may result in inducing protective effects of apelin on the myocardium imposed to high pressure in renovascular hypertension conditions. The finding that apelin in both doses reduced heterodimerizati
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br Mechanism of action In general the main
2023-05-24
Mechanism of action In general, the main targets for antifungal drug development are cell wall polymer (glucans, chitin, mannoproteins), cell membrane (especially ergosterol) biosynthesis, DNA and protein synthesis (topoisomerases, nucleases, elongation factors and myristoylation), and signal tra
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α-mangostin australia br Concluding Remarks and Future
2023-05-24
Concluding Remarks and Future Perspectives Fluorescent α-mangostin australia have helped researchers to elucidate antibiotic MOA and off-target interactions, to screen for new antibiotics, to detect antibiotics in the environment, to track antibiotic uptake throughout cells and organisms, and to
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IL-2, human recombinant Complementing the effects of ARB and
2023-05-24
Complementing the effects of ARB and ACEI on HDL capacity to elicit cholesterol efflux, HDL of ARB- and ACEI-treated groups significantly lessened macrophage production of superoxide (Fig 2). As with efflux, there was no difference in this effect between the ARB and ACEI groups. These data are inter
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Several ceritinib resistant mutations following the second l
2023-05-24
Several ceritinib-resistant mutations following the second-line treatment of ALK+-NSCLC have been discovered [64]. These mutations include C1156Y, F1174L, and L1152R, which were first observed in crizotinib-resistant tumor samples. The G1202R ceritinib-resistant mutation occurs within the hinge and
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Compounds and with potent ALR inhibitory activity were also
2023-05-24
Compounds , and with potent ALR2 inhibitory activity were also tested for their inhibition ability against ALR1, as shown in . They all showed low activity with inhibition percentages no more than 45% at the concentration of 10μM, demonstrating good selectivity for ALR2. To evaluate the antioxida
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Compounds and with potent ALR inhibitory activity were also
2023-05-24
Compounds , and with potent ALR2 inhibitory activity were also tested for their inhibition ability against ALR1, as shown in . They all showed low activity with inhibition percentages no more than 45% at the concentration of 10μM, demonstrating good selectivity for ALR2. To evaluate the antioxida
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mu receptor antagonist br Adenosine and tumor microenvironme
2023-05-24
Adenosine and tumor microenvironment In the majority of carcinogenic processes a proinflammatory state is generated [36], [37]. In addition, a tumor hypoxic environment is generally due to inadequate perfusion of oxygen to the tumor [38]. Immunomodulators are molecules that regulate the immune r
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