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br Acknowledgements This work was supported by the National
2022-07-26

Acknowledgements This work was supported by the National Key Research and Development Program of China [2017YFD0400106]; Innovation of modern Project[F18R02-03]. Introduction The Vesiculovirus genus is one of the six genera of the rhabdovirus family. The prototype vesiculovirus is vesicular s
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In Locusta migratoria a worldwide agricultural pest we previ
2022-07-26

In Locusta migratoria, a worldwide agricultural pest, we previously identified 51 CPRs containing eight endocuticle structural glycoproteins, which are homologs of SgAbd-1, SgAbd-2, SgAbd-3, SgAbd-4, SgAbd-5, SgAbd-6, SgAbd-8, and SgAbd-9 in the adult desert locust, Schistocerca gregaria [17,26]. Al
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The role of the ER EK variant which is
2022-07-25

The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of R406 free base sale levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protec
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5 03 The potential therapeutic actions of GHSR in the centra
2022-07-25

The potential therapeutic actions of GHSR in the central nervous system has been in the limelight lately. Peripheral administration of GHSR agonists have been shown to inhibit oxidative stress, apoptosis, proinflammatory cytokine production, microglia activation, mitochondrial dysfunction, and excit
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Natural product based drug discovery
2022-07-22

Natural-product-based drug discovery can be enhanced with computational methods [205]. Because most of the reported small-molecule natural inhibitors of fMLF-induced functional responses were not evaluated in Nitecapone binding assays, we used molecular modeling to predict how well these compounds
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Acquiring resistance to the FGFR inhibitor
2022-07-22

Acquiring resistance to the FGFR inhibitor may determine treatment outcomes in patients with GC dependent on FGFR2 amplification, and we investigated the mechanism of AZD4547 resistance in FGFR2-amplified GC cells. We established a FGFR2-amplified GC cell line resistant to the selective FGFR inhibi
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In NAFLD models the first
2022-07-22

In NAFLD models, the “first hit” is liver fat accumulation, which causes insulin resistance, whereas the interplay of inflammatory cytokines, which causes inflammation, acts as the representative “second hit” [9]. However, recently, the “multiple hit” hypothesis has taken into consideration that mul
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It is important to mention that the
2022-07-22

It is important to mention that the IC50 of cetirizine needed to achieve histamine H2 receptor desensitization was 0.43 µM or 170 ng/ml (Fig. 1B), becoming clinically relevant since pharmacokinetic studies after oral administration of the clinically used dose (10 mg/day) reported a maximal plasma co
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h89 In an RNAi screen to interrogate
2022-07-22

In an RNAi screen to interrogate the function of transmembrane proteins in ISCs/EBs, we identified the SJ protein tetraspanin 2A (Tsp2A) as a tumor suppressor. Further characterization reveals that Tsp2A expression initiates in ISCs and Tsp2A protein assembles at the SJs in the progenitor h89 that
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HER genotype was determined in breast cancer
2022-07-22

HER2 genotype was determined in breast cancer tissue of 73 breast cancer patients. As previously reported, Ile655Val and Ala1170Pro genotypes measured in breast cancer tissues were available for 71 and 69 breast cancer patients, respectively. Briefly, 77.5% (55/71) of patients were homozygous for th
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Finally worth of mention are few papers that report
2022-07-22

Finally, worth of mention are few papers that report on the discovery of HO-2 selective inhibitors. In 2013, starting from the screening of a (±)-Bay K 8644 library, the above-mentioned Canadian research group identified Clemizole (Table 6) as a new hit compound for the development of the first ser
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Epigenetic drugs such as HDAC inhibitors regulate gene expre
2022-07-22

Epigenetic drugs, such as HDAC inhibitors, regulate gene expression by affecting the activity of histone or DNA modifying enzymes and their associated transcriptional response [141]. BET bromodomain protein inhibition is another epigenetic approach for blocking the Hedgehog pathway at the downstream
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These inhibitors possess a cap group
2022-07-22

These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a
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BG45 Historically pharmacological investigations have been c
2022-07-22

Historically, pharmacological investigations have been carried out by first identifying a biological response to a ligand, and then subsequently using that ligand to identify the receptor(s) responsible for the response (Wilson et al., 1998). However, this approach needed revision with the discovery
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br Materials and methods br Results br
2022-07-21

Materials and methods Results Discussion Main results obtained in this work are presented in Table 1 and can be summarized as follows: 1) AEA inhibits FcεRI receptor-induced degranulation with the participation of CB2 and GPR55 receptors by a PTX-insensitive mechanism; 2) AEA does not block
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