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According to their structures and substrate specificity MMPs
2024-05-08
According to their structures and substrate specificity, MMPs are divided into five major groups: collagenases (e.g., MMP1), gelatinases (e.g., MMP2, MMP9), stromelysins (e.g., MMP3, MMP10), matrilysins (e.g., MMP7), and membrane-type MMPs [7]. Among them, MMP1 is a major collagenase that degrades t
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raas inhibitors The decreased AR mediated response has been
2024-05-08
The decreased βAR-mediated response has been attributed to different mechanisms, including an attenuation of PKA activation, an impaired generation of cyclic AMP, a reduced receptor density, and a less efficient coupling to adenylyl-cyclase [10]. However, currently there is no single molecular or ce
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br Transparency document br Introduction G
2024-05-08
Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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Acitretin The synthetic adipoR agonists AdipoRon and
2024-05-08
The synthetic adipoR agonists, AdipoRon (1) and 112254 (2), are both detectable in human plasma [18]. However, with increasing knowledge about their metabolism [19], a method for detection from human urine is conceivable and would be preferred given the easier accessibility and greater frequency of
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The anorexic effect observed when AR is
2024-05-08
The anorexic effect observed when AR231630 is infused into the VTA could be the result of the DA release inhibition, as previously described [11]. However, there is also a hedonic aspect in feeding that possibly involves dopaminergic mechanisms of reward. Helm et al. showed a functional link between
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In fact serotonin is a major modulator of
2024-05-08
In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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Adenosine is an endogenous nucleoside that plays pivotal rol
2024-05-08
Adenosine is an endogenous nucleoside that plays pivotal roles in different physiological and pathophysiological processes by triggering specific cell-surface receptors both in the Rimonabant sale and in the periphery. The adenosine receptors (ARs) are four different subtypes of G protein-coupled r
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Among the enzymes involved in adenosine metabolism adenosine
2024-05-08
Among the enzymes involved in adenosine metabolism, adenosine kinase plays an important role in regulating formation and release of endogenous adenosine in cardiomyocytes as well as vascular endothelial cells Decking et al., 1997, Kowaluk et al., 1998, Smolenski et al., 1994. Inhibition of adenosine
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Actin is capable of polymerizing spontaneously However this
2024-05-08
Actin is capable of polymerizing spontaneously. However, this process is relatively slow and kinetically unfavorable in cells. Formation of butein dimers and trimers, which can easily disassemble due to their instability, is a rate-determining step in actin polymerization [5], [6]. The shape and th
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The syntheses of a and
2024-05-08
The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each Azaperone austra
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Despite the growing knowledge surrounding the link between A
2024-05-08
Despite the growing knowledge surrounding the link between ATX and cholestatic pruritus in PBC, it remains unclear if the role of the ATX-LPA signaling axis includes lymphocytes homing in the liver of PBC, and if the resulting inflammation is associated with PBC pruritus (Fig. 3). PBC is characteriz
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Another topic for research will be the combination of
2024-05-08
Another topic for research will be the combination of other cytotoxic agents with Aurora kinase inhibitors. Particularly interesting might be the combination of Aurora kinase inhibitors and agents that depend on the spindle checkpoint for their activity, such as the taxanes, given the importance of
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Matthew et al synthesized and carried out SAR studies
2024-05-08
Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that sr9011 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC50
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Why do glutamate and glycine bind to the receptor
2024-05-07
Why do glutamate and glycine bind to the purchase in such different ways? Given the overall structural similarity between the GluN2A and GluN1 LBDs, one might conclude that the LBDs also bind ligands via similar processes. NMDA receptors with engineered disulfide linkages that lock the GluN1 lobes
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br Conclusions In summary the present results showed that
2024-05-07
Conclusions In summary, the present results showed that ageing diminished arginase activity only in clearance tissues and that l-arginine supplementation did not induce major changes in arginase activity thus refuting a role of arginase in the potential deleterious effects of l-arginine supplemen
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