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Ligand selectivity may directly be related to the conformati
2022-04-12

Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This
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However the clinical development of was terminated in
2022-04-12

However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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Our biological data also showed that in presence of
2022-04-11

Our biological data also showed that, in presence of LEDGF/p75, R or S of glycerol T instead of T4, T8 or T12 loop in the T30695-GQ differently affected the integration activity of the enzyme (Table 2), whereas the position but not the chirality of glycerol T affected the inhibitory efficiency of T3
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Here we examined Meckel s cartilage
2022-04-11

Here, we examined Meckel's cartilage of mice where Setdb1 was knocked out only in neural crest derived SR 95531 hydrobromide with the purpose of investigating the roles of Setdb1 in Meckel's cartilage, a supportive tissue for mandible formation. We observed enlarged Meckel's cartilage that was a res
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In our previous study we
2022-04-11

In our previous study, we designed and synthesized compounds of A series from the starting material 4-hydroxy-3-methoxycinnamic BS-181 (ferulic acid). These compounds with R group being amino acid residues, fatty acyl group and sulfuryl group showed moderate HDAC inhibition and in vitro antitumor p
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PLP has been found to be effective inhibitor
2022-04-11

PLP has been found to be effective inhibitor of many enzymes that have fxr agonist for phosphate-containing substrates or effectors, including RNA polymerase [14], [15], reverse transcriptase [16], and DNA polymerase [17], [18]. Oka et al. [19], [20] reported that vitamin B6 deficiency generally en
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It was revealed that various
2022-04-11

It was revealed that various injured or infected organs of Hippeastrum produce a mixture of an orange-colored chalcone and flavans which can be oxidized to red-colored dimer (Wilmowicz et al., 2014, Wink and Lehmann, 1996), preventing the penetration of injured tissues by Phoma narcissi, Botrytis ci
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Despite the similarities there are some differences
2022-04-11

Despite the similarities, there are some differences between the augmentation by hypoxia and that by thymoquinone. While in porcine coronary arteries they both depend on calcium sensitization mediated by ROCK12, 32, 33, L-type calcium channels are involved only in thymoquinone-induced augmentation.
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The PI K PTEN Akt mTORC GSK pathway
2022-04-11

The PI3K/PTEN/Akt/mTORC1/GSK-3 pathway also plays key roles in metabolism, obesity, diabetes and cardiovascular diseases (, , , , ). Sometimes such clinical problems such as diabetes, obesity and metabolic disorders are interlinked with cancer. Clearly further elucidation of the roles of GSK-3 could
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GPR GPR GPR GPR and
2022-04-11

GPR80, GPR81, GPR82, GPR93 and ψGPR79 all shared identities to P2Y GPCRs or P2Y-like oGPCRs. Previously, at least three different nucleotide receptor phenotypes have been observed in mammalian tissue, including GPCRs activated by ion channel nucleotides (e.g. P2Y1 and P2Y11), uridine nucleotides (e
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hGPR was mapped to human chromosome q and in the
2022-04-11

hGPR55 was mapped to human chromosome 2q37, and in the human CNS it is predominantly localized to the caudate, putamen, and striatum (Sawzdargo et al., 1999). In rats, in situ hybridization indicated expression in hippocampus, thalamus and regions of the midbrain (Sawzdargo et al., 1999). Ryberg et
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For some agonists these stable GPR responses
2022-04-11

For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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For a long time the mechanism
2022-04-11

For a long time, the mechanism for the TG-lowering effect of nicotinic lipoxygenase inhibitor has been thought that the lowered NEFA substrate from adipose tissue limits TG production from the liver (so-called NEFA hypothesis) [[1], [2], [3], [4]]. However, recent emerging evidences have suggested
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The timing and growth of
2022-04-11

The timing and growth of follicles relative to follicle deviation was assessed in 49 cows (Fig. 4) that had NFWE following treatment onset and that had not already established dominance. Because day of deviation did not differ due to treatment, day of estrous cycle, or replicate, data are presented
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Our inhibitor studies revealed the presence of a signaling n
2022-04-11

Our inhibitor studies revealed the presence of a signaling network triggered by dicarbonyl stress. Nevertheless, p38-MAPK activation was clearly necessary for NADPH-oxidase mediated production of ROS. This is consistent with data from other groups using different cell culture systems [37], [38], [39
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