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According to the aforementioned preclinical and clinical dat
2022-07-16
According to the aforementioned preclinical and clinical data, GHS-R1a blockade appears to be a potential pharmacological approach to treat AUD. Given that GHS-R1a has high constitutive (ligand-independent) activity, inverse agonism of the receptor may exert more potent and desirable effects than pu
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br Conflict of interest statement br Acknowledgements br Int
2022-07-16
Conflict of interest statement Acknowledgements Introduction Galanin is a multi-functional neuropeptide that is widely distributed in the neuroendocrine system and peripheral tissues of various species. This 29-amino-acid peptide (30 in humans) is proteolytically processed from its precurso
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BMS 753 Somatostatin analogues are among the first peptide
2022-07-16
Somatostatin analogues are among the first peptide-based drugs used in cancer imaging and therapy (for review see Reubi, 2003). Treatment of tumors by the use of peptide analogues labeled with cytotoxic agents acting via specific receptors is also under investigation for neuropeptide Y (Koglin and B
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Enasidenib Introduction Since the development of the
2022-07-16
Introduction Since the development of the first radioimmunoassay (RIA) to measure hormone levels in the late 1950s, for which Rosalyn Sussman Yalow was awarded the Nobel Prize for Medicine in 1977 (the second woman ever receiving it), the use of Enasidenib in molecular research has increased treme
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Thus this work aims to evaluate
2022-07-16
Thus, this work aims to evaluate the effect of tannic NT157 synthesis on β-galactosidase activity, by observing the variations in the molecular interaction kinetic parameters ( and ). Besides, these data were correlated with the modifications that the tannin caused to the enzyme’s secondary structu
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Since our new compound Fex could be a
2022-07-16
Since our new compound Fex-3 could be a new FXR ligand, we try to demonstrate that Fex-3 was an intestinal-restricted FXR agonist which only activated FXR in the intestine not in the liver or other organs. Initially, we investigated this in Caco-2 Iniparib with transwell experiments. From and , we
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Recently Bristol Myers Squibb and Merck reported their GPR
2022-07-16
Recently, Bristol-Myers Squibb and Merck reported their GPR40 agonist research focused on the modification of α,β-position of phenylpropionic SAR 405 derivatives. For example, in recent published patent applications, Bristol-Myers Squibb claimed the pyrrolidine and dihydropyrazole GPR40 agonists wit
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br Conclusion In this research we have successfully formulat
2022-07-15
Conclusion In this research we have successfully formulated a PEGylated liposomal formulation encapsulating IRL-1620. The liposomal nanocarriers loaded with IRL-1620 were characterized for their particle size, PDI, zeta potential, and loading efficiency. We established that the treatment with IRL
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Materials and methods br Results and discussions br
2022-07-15
Materials and methods Results and discussions Conclusions In this study, we identified 7 histone acetyltransferases and 12 histone deacetylases in Marchantia polymorpha. The present phylogenetic analysis of MpHATs and MpHDACs provide the insight into the evolutionary relationships of these tw
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Efficiency of methylated process was assessed by calculating
2022-07-15
Efficiency of methylated process was assessed by calculating PMI and SMI. On average, PMI was 0.9 and ranged from 0.1 to 3.8 while SMI was 4.9 and ranged from 0.3 to 21.3. The observed differences in the arsenic methylation can be associated with the inter-individual variations caused by a genetic p
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The absence of direct oxidation of Fe by L in
2022-07-15
The absence of direct oxidation of Fe2+ by L1 in experiments in solution would be consistent with the recognized low O2 affinity of sGC. It is known that, in NPS-2143 hydrochloride with other hemoproteins, such as globins and heme-containing oxygenases with a Fe2+-proximal histidine linkage, sGC pre
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We have previously established the
2022-07-15
We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in Picrotoxin sale and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]. The co
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The HIV genome encodes for a variety of viral
2022-07-15
The HIV-1 genome encodes for a variety of viral proteins necessary for target cell entry and viral replication. gp120 is an HIV-1 envelope glycoprotein that mediates viral particle entry by binding to cell surface receptor CD4 and co-receptors CXCR4 and/or CCR5 depending on viral tropism. While CXCR
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Adenosine triphosphatase ATP is a signaling molecule
2022-07-15
Adenosine triphosphatase (ATP) is a signaling molecule in acute pain and chronic pain(Burnstock, 2009, Burnstock, 2013, Burnstock, 2014, Chizh and Illes, 2001). It is also known that presynaptic A1 receptors are involved in the inhibition of transmitter release (Vizi and Knoll, 1976). Extracellular
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br Significant efforts are currently focused
2022-07-15
Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) Adenosine 5-monophosphate hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-con
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