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AMPK is a serine threonine
2024-05-11
AMPK is a serine/threonine protein kinase composed of a catalytic α subunit with the activating phosphorylation site (Thr172) and two regulatory subunits, β and γ. The two AMPK variants, α1 and α2, show different cellular localization in mammalian cells. AMPKα2 is detected in nuclear and non-nuclear
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Caffeic acid dihydroxycinnamic acid is a natural compound th
2024-05-10
Caffeic voltage gated potassium channel (3,4-dihydroxycinnamic acid) is a natural compound that inhibits 5-LO and exerts potent anti-inflammatory and antioxidant properties. Recently, Takeda et al. reported that caffeic acid provided neuroprotective and anti-depressive activities [23]. Sertraline,
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The uterine muscle also changes to meet the
2024-05-10
The uterine muscle also changes to meet the demands of pregnancy. Over the course of pregnancy, the myometrium undergoes structural remodeling to accommodate a growing fetus, followed by a functional switch from quiescent to contractile characteristics for parturition. Studies on the mouse model ind
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Afuresertib australia Assessment of antibiotic appropriatene
2024-05-10
Assessment of antibiotic appropriateness is receiving increased attention in the face of growing concerns about the emergence of MDROs, as well as the rise in adverse outcomes associated with antibiotic use such as C. difficile infection. In this study, 15% of cultured Gram-negative organisms met th
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br HIF Blockade in AA Therapy In
2024-05-10
HIF-α Blockade in AA Therapy In lieu of the evidence supporting a central role for HIF-α signaling in tumor angiogenesis and CC pathobiology, significant efforts have focused on the discovery of small-molecule HIF-α inhibitors (for exhaustive compendia, see [28,44,45]). In brief, inhibitors vary
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AMPK is a cellular energy sensor that
2024-05-10
AMPK is a cellular energy sensor that is phosphorylated in response to high intracellular ADP levels to increase GLUT4 translocation into the cell, and subsequently, increase intracellular glucose levels to provide substrate to replenish ATP levels [25]. In metabolic syndrome, sequestration of plasm
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Several ceritinib resistant mutations following the second
2024-05-10
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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Last decade has provided a number of studies indicating
2024-05-09
Last decade has provided a number of studies indicating that AhR signaling could play a role both in the development and in progression of multiple cancer types, with potential implications for cancer therapy (for review see (Kolluri et al., 2017; Murray et al., 2014)). Activation of AhR is consider
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br Functional consequences of ADK regulation on astrocyte fu
2024-05-09
Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in nadph oxidase (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of ADK exp
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CDK4 inhibitor The zebrafish Danio rerio is a popular model
2024-05-09
The zebrafish (Danio rerio) is a popular model organism for virtually any biological function of vertebrates, and has, therefore, received a wide distribution in particular in developmental biology and toxicology (Strähle et al., 2012). With respect to AChE, the zebrafish has, e.g., been identified
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br ARIs in the prevention of
2024-05-09
5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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br Funding br Introduction l Dihydroxyphenylalanine l DOPA
2024-05-09
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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Having established the structural requirements for potency i
2024-05-09
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 vit
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The synthesis of compounds in
2024-05-09
The synthesis of compounds in which the ethyl linker has been modified to the carbamate and urea derivatives , and is shown in . Thus the diamine was reacted with glycolic Dabrafenib to give the alcohol followed by Mitsunobu reaction with phthalimide to give . Deprotection with hydrazine gave the a
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br Materials and methods br
2024-05-09
Materials and methods Results Discussion Recent studies have highlighted AM251 and autophagy as novel targets for the treatment of liver fibrosis [7,14]. In this study, we demonstrated that catalpol protected the rat liver from CCl4-caused injury and fibrogenesis in vivo and in vitro for t
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