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The ETA receptor has a higher affinity for endothelin
2022-02-08
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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Ertapenem sodium salt br To explore further the functional i
2022-02-08
To explore further the functional impact of the similarity of the UTY and KDM6A proteins, the FANTOM5 human dataset was analysed to determine whether or not the genes were expressed at the same time in the same tissues (which would suggest that they are controlled by the same regulators) or with o
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To solve the atomic structures
2022-02-08
To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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br GSK Glycogen synthase kinase GSK
2022-02-08
GSK-3 Glycogen synthase kinase-3 (GSK-3) is a ubiquitous serine/threonine kinase that is involved in multiple signaling pathways that are crucial for cellular metabolism and proliferation (Doble and Woodgett, 2003, Frame and Cohen, 2001, Grimes and Jope, 2001, Woodgett, 1990). GSK-3 is known to d
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br Materials and methods br Results
2022-02-08
Materials and methods Results Discussion In this report, we have analyzed the function of an orphan GPCR, and GPR84, using genetically-deficient mice. The expression of GPR84 in the T and BAY 57-9352 synthesis in the spleen prompted us to examine the functional responses of these cells unde
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br Materials and methods br
2022-02-08
Materials and methods Results Discussion Previously, it is well known that methionine and choline deficient (MCDD) or choline-deficient, L-amino acid-defined (CDAA) models are widely accepted in NASH research. MCDD or CDAA dietary model has been mimic human NASH in rodents by sequentially p
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In addition researchers studying GPR agonists favor
2022-02-08
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it MK-8245 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (no
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Trypanosomatid GLO enzymes are monomeric and contain a
2022-02-07
Trypanosomatid GLO2 enzymes are monomeric and contain a zinc–iron binuclear metal center (Irsch and Krauth-Siegel, 2004, Silva et al., 2008), similar to all other glyoxalases II. As mentioned, in T. brucei there are two GLO2 genes but only one encodes an enzyme with glyoxalase II activity (Irsch and
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neurokinin receptor antagonist Histamine functions as a key
2022-02-07
Histamine functions as a key neurotransmitter in multiple circuits to control various behaviors. In Drosophila photoreceptor, neurokinin receptor antagonist is produced de novo by histidine decarboxylase (Burg et al., 1993); meanwhile, maintaining normal histamine content also depends on the histam
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guanylate cyclase We also demonstrated that inhibition of N
2022-02-07
We also demonstrated that inhibition of NAAG hydrolysis to suppress glutamate production through a GCPII inhibitor is a viable target for cancer therapy. GCPII is also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I) or NAAG peptidase (Pinto et al., 1996), and its increased express
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br Biologically active non peptide galanin
2022-02-07
Biologically active non-peptide galanin receptor ligands The first successful attempt in overcoming these weaknesses was undertaken by Saar et al. (2002). Screening of galanin sequence established that Trp-2, Asn-5, Tyr-9 were pharmacophores, responsible for biochemical action of the peptide. Bas
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Considering the conformational preferences of
2022-02-07
Considering the conformational preferences of the SRSRY sequence in the x-ray structures of soluble uPAR (SuPAR) [18], [19], [20], [50], [51], it is included in a quite flexible linker delimited by Cys76 and Cys95 residues. The SRSRY sequence adopts either α-turned or β-extended conformation. In any
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By measuring the accumulation of unprenylated Rap a as
2022-02-05
By measuring the accumulation of unprenylated Rap1a as a surrogate marker for the inhibition of FPPS [8], [9], [10], [11], we found that upregulation of FPPS expression in Hela cells reduced the accumulation of unprenylated Rap1a in response to 24h' treatment with 0–50μM ZOL. As expected, cells cult
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Histamine which was used as the agonist had low
2022-02-05
Histamine, which was used as the agonist, had low potencies in our functional experiments when compared to its affinity from binding studies (e.g. Lim et al., 2005). This phenomenon is related to the fact that the coupling of the presynaptic receptor to the transduction machinery and the final funct
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To prevent toxicity of free hemoglobin as well
2022-02-05
To prevent toxicity of free hemoglobin as well as its degradation metabolites heme and free iron, several scavenger proteins and degradation enzymes protect the body. Haptoglobin (Hp) is the most well described hemoglobin scavenging protein that binds free hemoglobin and transports it to macrophages
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