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Routine administration of exogenous GC is pertinent
2022-01-25
Routine administration of exogenous GC is pertinent during late gestation, particularly in women who are at risk of delivering a preterm infant, aiming at ensuring proper neonatal outcome and survival (Kamath-Rayne et al., 2012). Unfortunately, despite its beneficial roles in foetal survival, variou
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Also the decrease in adipocyte
2022-01-25
Also, the decrease in adipocyte cAMP levels seen after an acute glucose challenge in wild-type mice was strongly reduced in mice lacking GPR81, indicating that the activation of PDE3B alone was not sufficient to mediate the effect of insulin on cAMP levels and lipolytic activity. The fact that insul
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Terfenadine To combat the detrimental effects of neuropathol
2022-01-25
To combat the detrimental effects of neuropathological conditions, additional therapeutic interventions that either dampen chronic neuroinflammation or attenuate reductions in hippocampal neurogenesis are critically needed. The cannabinoid system has already been shown to rescue impaired neurogenesi
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Glucagon was described as an insulin secretagogue as early a
2022-01-24
Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β lamotrigine clearly show that glucagon is
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br Other strategies for ferroptosis
2022-01-24
Other strategies for ferroptosis In addition to ROS-generating and GPX4 inactivating nanomaterials, small molecules and genetic manipulation targeting key factors in the ferroptosis pathway have also been tested for their anticancer effects [39,47,48]. Among a myriad of proteins involved in ferro
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PD PD L signaling is critical for the induction of
2022-01-24
PD-1/PD-L1 signaling is critical for the induction of exhausted CD8+ T Letrozole during the tumor immune response (Barber et al., 2006; Wherry et al., 2007; Wherry and Kurachi,2015; Pauken and Wherry, 2015), but the relationship between PD-1/PD-L1 signaling and Fas/FasL signaling in exhausted CD8+
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Paroxysmal or sustained atrial fibrillations profoundly acti
2022-01-24
Paroxysmal or sustained atrial fibrillations profoundly activate platelets and induce coagulation factors in the heart (Choudhury and Lip, 2003). Accumulating factor Xa and downstream thrombin in the fibrillating left atrium activate PAR1 and/or PAR2 signaling to modulate electrical characteristics
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Fenofibric acid receptor Here we report a new human genetic
2022-01-24
Here, we report a new human genetic disorder in a patient with hypoalgesia, altered fear and memory symptoms, and a non-anxious disposition. This disorder is attributable to co-inheritance of a microdeletion in a novel pseudogene and a known FAAH hypomorphic SNP. The microdeletion is flanked by repe
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Electrochemical techniques have attracted broad attention fo
2022-01-24
Electrochemical techniques have attracted broad attention for their outstanding advantages, such as satisfactory sensitivity and convenient operation. Nowadays, nucleic fak inhibitor nanostructures such as DNA tetrahedron structure, nucleic acid-mimicking structure, exhibit noticeable application i
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br STAR Methods br Acknowledgments We thank
2022-01-24
STAR★Methods Acknowledgments We thank P. Adler, V. Riechmann, N. Tapon, E. Knust, the Vienna Drosophila RNAi Center, the Australian Drosophila Research Support Facility (www.ozdros.com), the Bloomington Drosophila Stock Center, and the Developmental Studies Hybridoma Bank for D. melanogaster s
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br Structural studies of GCAP Recoverin was the
2022-01-24
Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding caspase pathway to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. The
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The finding that GPR acts as a receptor for acyl
2022-01-24
The finding that GPR35 acts as a receptor for 2-acyl LPA is noteworthy, because P2Y5, which has homology with GPR35 (29%), has recently been shown to act as a receptor for 2-acyl LPA [14]. LPA3 is also a specific receptor for 2-acyl LPA [15]. It is also worth noting that GPR55, which has homology wi
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Because of its excellent GPR potency good hERG selectivity
2022-01-24
Because of its excellent GPR119 potency, good hERG selectivity and favorable rat t, Isorhamnetin synthesis was scaled-up and further profiled. The synthetic protocols described in , were both suitable for a multi-gram scale synthesis of compound . An off-target screen was performed against an extens
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br FXR Agonists Azepinol b indole
2022-01-24
FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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No compounds in this series showed any
2022-01-24
No compounds in this series showed any appreciable activity at GlyT2 and can thus be considered GlyT1-selective. For the GlyT2 IC was >20μM. To determine CNS penetration of -(2-(azepan-1-yl)-2-phenylethyl)-benzenesulfonamides, select compounds were evaluated in a cassette CNS exposure screen in ma
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