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To date the underlying mechanism of ropivacaine in inducing
2022-02-10
To date, the underlying mechanism of ropivacaine in inducing neurotoxicity remains unclear. Cell death was intimately involved in local-anesthetic neurotoxicity [6,18]. Two classic signaling pathways triggered cell death: the extrinsic pathway and the intrinsic pathway [12]. Our study demonstrated t
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Previous evidence suggests that PRC
2022-02-10
Previous evidence suggests that PRC2 is an important regulator of chromatin looping interactions in embryonic stem topoisomerase inhibitors . The new study by Donaldson-Collier and colleagues provides the first evidence that similar processes may be at play in lymphoma. It is still largely unclear,
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A second H R antagonist with
2022-02-10
A second H3R antagonist with benzamide-based structure from Johnson & Johnson is JNJ-31001074, known as Bavisant and under chemical IUPAC name of (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone. It is a compound with molecular weight 329.44, HBA four, and MLogP 1.52 encompas
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Heparin The more important effect of pitolisant is related t
2022-02-10
The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced Heparin release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers ref
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It is an open question
2022-02-10
It is an open question if these in vitro findings have implications for the use of sGC activators in the in vivo situation and in patients. Assuming that incorporation in de novo synthesised enzyme occurs during therapy, one might speculate that the duration of drug administration has an influence o
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Both plant hormones and some second messengers are involved
2022-02-10
Both plant hormones and some second messengers are involved in Fe-deficiency-related responses in plants (Kobayashi and Nishizawa, 2012). Among these second messengers, nitric oxide (NO) accumulation was induced by Fe deficiencies in tomato and Arabidopsis roots, and it acts as the downstream signal
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A number of in vivo
2022-02-10
A number of in vivo studies have investigated the antitumor activity of distinct GSK-3 inhibitors in a variety of cancer cell line-derived tumor xenograft models [14], [21], [22], [24], [33], [39], [40]. These studies utilized toolkit GSK-3 inhibitors as monotherapies. Although inhibition of tumor g
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As part of their ongoing effort in the
2022-02-10
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile (3S,5S)-Atorvastatin sodium s
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Flaviviruses consist of a nucleocapsid composed
2022-02-10
Flaviviruses consist of a nucleocapsid, composed of multiple copies of the capsid protein (C) and the single-stranded, positive-sense RNA genome. The nucleocapsid is surrounded by a lipid bilayer in which two transmembrane proteins are inserted, the envelope glycoprotein E and the membrane protein M
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br Short Communication Free fatty acid receptors FFAR
2022-02-09
Short Communication Free fatty Pirfenidone australia receptors (FFAR) play significant roles in energy metabolism (Brown et al., 2005; Ichimura et al., 2009). The receptor FFAR1 is involved in insulin secretion in humans (Meidute Abaraviciene et al., 2013). Activation of the receptor FFAR2 increa
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br Materials and methods br
2022-02-09
Materials and methods Acknowledgments We are grateful for financial support from the National Natural Science Foundation of China (Grants No. 81661148046 and 81773762, China) and the “Personalized Medicines—Molecular Signature-based Drug Discovery and Development”, Strategic Priority Research
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The objective of this study is to design and
2022-02-09
The objective of this study is to design and synthesize drug-like molecules with agonistic activity on both receptors; PPARγ and FFAR1. These agents would act as insulin sensitizers and insulin secretagogues through their action on PPARγ and FFAR1, respectively. The design of drugs with dual mode of
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Our results are consistent with the
2022-02-09
Our results are consistent with the hypothesis that reduced Fas-mediated apoptosis in maternally activated T-lymphocytes could result in insufficient trophoblast invasion of the spiral Moxidectin as the activated T-lymphocytes become able to enhance the destruction of the cytotrophoblasts. A reduced
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CTGF is an established YAP TAZ target
2022-02-09
CTGF is an established YAP/TAZ target gene which plays a central role in tissue remodeling. Downregulation of CTGF mediates collagen loss in chronologically-aged human skin whereas persistent activation of CTGF can result in excessive deposition of collagen and fibrotic disorders [63]. The authors f
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br Materials and methods br
2022-02-09
Materials and methods Results Estimations of OMP generated by the proposed mechanism (Fig. 1) were first performed for the range of 0.001–2 mM of rac1 inhibitor concentration in the cytosol. It was assumed that only 5% of all VDACs in MOM form the ANT-VDAC1-HKI contact sites, and that the fra
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