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Importantly both genetic deletion and pharmacological inhibi
2022-08-24

Importantly, both genetic deletion and pharmacological inhibition of FAAH also reduced NTG-induced neuronal hyperactivity in the trigeminal nucleus, which receives sensory input from craniofacial deep tissues. NTG is known to evoke the robust neuronal activation, as evidenced by the induction of the
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In addition the interplay of membrane curvature induced tens
2022-08-24

In addition the interplay of membrane curvature induced tension at the fusion pore and Methyllycaconitine citrate induced tension across the PM seems to be a worthwhile target for investigation. The roles of dynamin and myosin II and especially their spatial and temporal dynamics during activity wa
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An azabicyclic compound named S a a hexahydro
2022-08-24

An azabicyclic SKF 81297 hydrobromide named S 38093, (4-[3-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)propoxy]benzamide), was introduced by Servier with H3R antagonist and inverse agonist activity (Sors et al., 2017). The compound contains all the drug-likeness criteria owing to its physi
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The dramatically reduced expression of CFTR in human colorec
2022-08-24

The dramatically reduced expression of CFTR in human colorectal cancer tissues identified herein is consistent with our previous findings using human breast cancer tissues, prostate cancer tissues, and colon cancer tissues, and suggests that the loss of CFTR is likely a general phenomenon in epithel
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The following are the supplementary data related
2022-08-24

The following are the supplementary data related to this article. Introduction Target therapies have achieved significant gains in the fight against cancer, however, they are still a long way from providing generally curative treatments for the majority of cancers. Targeted agents can be used wi
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br Material and methods br Results br Discussion HBV develop
2022-08-24

Material and methods Results Discussion HBV develops several strategies to suppress antiviral immune responses. Here, we used a bifunctional siRNA molecule to silence HBx and activate RIG-I, which induced HBV inhibition partly mediated by RIG-I in HBV-carrier mice. Furthermore, this 3p-siHB
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Transcriptional elongation is a checkpoint for productive
2022-08-24

Transcriptional elongation is a checkpoint for productive transcription. In ESCs, ∼50% of the genes enriched for H3K4me3 are initially transcribed but do not enter productive elongation (Guenther et al., 2007, Rahl et al., 2010). Following promoter escape, the transcriptional elongating protein comp
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To identify structurally novel autophagy
2022-08-24

To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 ASC-J9 stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by automated fl
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Interestingly in vivo infusion and uptake of Ang II
2022-08-24

Interestingly, in vivo infusion and uptake of Ang II in intact mice indicated that multiligand endocytic receptor megalin has at least some role in the uptake of Ang II and the downstream signaling process in proximal tubule GSK 0660 synthesis (PTCs) in vivo [173]. Earlier in vivo studies showed th
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br Results and discussion br Conclusion In
2022-08-24

Results and discussion Conclusion In summary, starting from our previous lead Difopein 1, we replaced the 5-nitropyrimidine core with pyrimidopyrimidine to obtain a series of novel compounds as drug candidates of GPR119 agonist for treatment of type 2 diabetes. Some derivatives showed good ag
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It is possible that maternal separation
2022-08-24

It is possible that maternal separation-induced USV in neonatal rodents is not a good model of adult anxiety for examining GlyT1 inhibitors, if the expression levels of GlyT1, GlyA, and GlyB markedly differ between pups and adults. However, several reports provide evidence that this is not the case.
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The dramatic increase in the development of EAAT
2022-08-24

The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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br Acknowledgements This research was funded by Ministry of
2022-08-24

Acknowledgements This research was funded by Ministry of Education Malaysia (MOE), and supported by the Department of Nutrition, Exercise & Sports, Department of Drug Design, University of Copenhagen, Denmark and Universiti Malaysia Pahang (UMP), Malaysia. HPLC equipment used for high-resolution
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One may carefully evaluate the concept
2022-08-23

One may carefully evaluate the concept ‘pancreas derived GLP-1′ as this may dependent on the specificity of the ret proto oncogene used in immunohistochemistry or radiommunoassays. If either a side-viewing antibody or a C-terminal wrapping antibody raised against GLP-1 is applied one may also ident
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The first FPR ligand described is the
2022-08-23

The first FPR1 ligand described is the fMLF peptide, which binds with high affinity (in the nM range) to and activates FPR1. Formylated peptides derived from Listeria monocytogenes also selectively activate FPR1 [10] (Table 1). Formylation of peptides also occurs in mitochondria. Thus, the release o
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