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YO-01027 synthesis Fig illustrates the different signaling p
2022-02-16
Fig. 1 illustrates the different signaling pathways elicited or modulated by H3R activation. Collectively, the modulation of the release of histamine and other neurotransmitters through H3R activation could be linked to several neurological disorders such as sleep disorders like narcolepsy, Alzheime
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Hh signaling pathway plays an essential role in
2022-02-16
Hh signaling pathway plays an essential role in the regulation of invertebrate and vertebrate tissue development and metabolic homeostasis. Components of Hh signaling pathway have been identified in succession, including Hh ligands, membrane protein receptors, cytoplasmic components and transcriptio
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HCV NS A inhibits induction
2022-02-16
HCV NS3/4A inhibits induction of the type I interferon response by cleaving MAVS from the mitochondrial surface (Li et al., 2005b). MAVS is cleaved at cysteine 508, and mln0128 of cysteine 508 to arginine (C508R) abrogates cleavage (Li et al., 2005b). GBV-B and the related canine hepatitis virus al
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br Conclusion The addition of cellulose to natural substrate
2022-02-16
Conclusion The addition of Difopein to natural substrate increases the number of H-bonds which indicates an increase in the stability of the docking systems. The investigated compounds are more stable than natural substrate in docking systems, where the natural substrate has two H-bonds while the
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Etoposide VP a semisynthetic podophyllotoxin derivative agen
2022-02-15
Etoposide (VP-16), a semisynthetic podophyllotoxin derivative agent, is widely used as a chemotherapic treatment for many cancers (Hande, 1998). VP-16 has been known that its activity is mediated by the interaction with topoisomerase II (an ATP-dependent nuclear enzyme) which regulates DNA topology
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Based on the results of compound appeared to have the
2022-02-15
Based on the results of , Clonidine HCl appeared to have the best overall profile, so our efforts were then devoted to using 5-(-propyl)pyrimidine as the right-hand nitrogen attachment to optimize the R group of (). Analog was synthesized using the reaction conditions from , while analogs and
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Molecular dynamics studies have proved an effective means
2022-02-15
Molecular dynamics studies have proved an effective means of characterising transition state pathways between the inward- and outward-facing states, and providing the relative propensity for each state. For example, long-timescale simulations of the membrane-embedded LeuT dimer, totalling ∼21 μs, ha
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GK allosteric activators validate the importance
2022-02-15
GK allosteric activators validate the importance of GK from a therapeutic perspective, but the nature of allosteric activation of GK remains unclear. The GK allosteric activator site, the pocket where GKAs bind, is ~20 Å remote from the active site (Fig. 1A). The allosteric site is the locus of many
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Although GLP has greater insulin releasing
2022-02-15
Although GLP-1 has greater insulin-releasing effects at pharmacological concentrations [10], it is apparent that the higher circulating concentrations of GIP combined with more pronounced increase in secretion following feeding make GIP the major physiological incretin [7], [11]. The peptide exerts
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In the liver ghrelin has
2022-02-15
In the liver, ghrelin has opposite effects to insulin on the expression of the enzyme PEPCK, thereby promoting gluconeogenesis and also causing a decrease in glucose uptake and fatty MCC950 sodium oxidation (Rigault et al., 2007). Ghrelin also stimulates hepatic lipogenesis de novo in a GH-independe
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Similar to C lividipennis RDL
2022-02-15
Similar to C. lividipennis RDL (Jiang et al., 2015), we found that the intracellular loop variants of A. mellifera RDL had no effect on GABA EC50 (Table 1). Also, as with C. lividipennis, there was no significant difference in maximal GABA responses (Table 1). However, whereas the 31 amino acid inse
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dopamine receptor This excellent tolerability is especially
2022-02-15
This excellent tolerability is especially interesting in the light of the fact that intravenous administration of liposomal ponatinib was predicted to yield much higher plasma concentrations as compared to the orally administered free drug. In addition, liposomal drug dose in absolute numbers was te
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The activation of GPR FFA signaling
2022-02-15
The activation of GPR40/FFA1 signaling triggers the PLC/PIP2 signaling pathway and results in Ca2+ release from the endoplasmic reticulum (ER). Increased Ca2+ levels may lead to activation of different protein kinases, such as Ca2+/calmodulin-dependent protein kinase type IV, Akt, extracellular sign
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survivin (baculoviral IAP repeat-containing protein 5) (21-2
2022-02-15
Next, we aimed to investigate if the cardiac apoptosis induced by CO-HFD, LA, T1DM or hyperglycemia involves up-regulation and activation of Fas/FasL-mediated cell death and if such effects are mediated by ROS and/or Ca+2/calcineurin/NFAT signaling axis. Similar to previous reports, [8], [9], [10],
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br Histamine H R The cloning of
2022-02-15
Histamine H4R The cloning of the H3R (Lovenberg et al., 1999) provided a template for the search of other LDN193189 Hydrochloride receptors, and resulted in the most recent discovery of histamine H4R. This concluded with six independent groups that have reported the cloning of the H4R (Leurs et
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