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The physiological and pharmacological roles of GPR remain la
2022-02-01

The physiological and pharmacological roles of GPR81 remain largely unclear because of several reasons. The low potency of lactate agonizing GPR81 in the millimolar range, together with its fast metabolic turnover, renders as a challenge in in vivo studies using lactate. Furthermore, there are no po
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ack1 inhibitors In summary our findings support the hypothes
2022-02-01

In summary, our findings support the hypothesis that activation of GPR55 protects against deficits in neurogenesis induced by inflammatory insult both in vitro and in vivo through direct targeting of NSCs. Better understanding of the mechanisms by which GPR55 provides neuroprotection is critically n
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br Materials and methods br Acknowledgements
2022-02-01

Materials and methods Acknowledgements The following reagents were obtained through the NIH AIDS Reagent Program, Division of AIDS, NIAID, NIH: SIVagm155-4 from Dr. Vanessa Hirsch and Dr. Philip Johnson; Anti-SIVmac251 Polyclonal; SIVagm tan-1 infectious molecular bcl-2 inhibitor from Drs. Ma
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Through the analysis of various synthetic GPR agonists
2022-02-01

Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic p-Cresyl sulfate motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discove
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ceritinib The primary requirements of an ideal bioprobe for
2022-02-01

The primary requirements of an ideal bioprobe for glucose transporter-mediated bioimaging include high specificity, sensitivity as well as low cytotoxicity [18]. According to these concepts, we recently reported the simple amide linked glycoconjugates which containing cyanine fluorophores (Cy3 and C
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br Materials and methods br Results br Discussion G
2022-01-31

Materials and methods Results Discussion G-quadruplex structures are extensively studied for its role in central dogma of molecular biology viz. replication problems leading to chromosomal translocations [20], [21], transcriptional inhibition [32] and alternative splicing and translational
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br Conflicts of interest br Acknowledgment br Introduction T
2022-01-31

Conflicts of interest Acknowledgment Introduction The anti fungal growth factor receptors (FGFRs) are a family members of receptor tyrosine kinase (RTK) that represent attractive therapeutic targets for anti-cancer therapy gaining more and more attention in recent years [1], [2]. This famil
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Endothelial cells receive a variety of information from the
2022-01-31

Endothelial cells receive a variety of information from the environment which finally guides them through all phases of neovascularization. Angiogenic signals enhance the proliferation of endothelial cells, upregulated resistance to apoptosis, alterations within proteolytic balance, reorganization
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br Results and discussion Computer modelling
2022-01-31

Results and discussion Computer modelling studies suggested that the endocyclic oxygens in furocoumarin derivatives, such as LY-2228820 synthesis 3a (Fig. 1), could also coordinate metal ions in the HIV-1 IN enzyme active site and inhibit the integration of viral DNA. The coumarin moiety is foun
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The more important effect of pitolisant
2022-01-31

The more important effect of pitolisant is related to its wake-promoting and arousal activities as a result of enhanced TASIN-1 release in animal models (Ligneau, Perrin, et al., 2007). Moreover, its potential in the treatment of severe excessive daytime sleepiness (EDS) in narcoleptic teenagers re
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We have confirmed that HO
2022-01-31

We have confirmed that HO-2 suppressed TLR4/MyD88-dependent signaling by down-regulating the downstream factors (TNF-α and IL-6) in mouse cerebral vascular endothelial cells [13]. In this study, HO-2 overexpression mouse model was generated and to investigated the role of HO-2 in macrophage inflamma
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GPR shares a amino acid sequence identity in humans to
2022-01-30

GPR81 shares a 52% amino capreomycin mg sequence identity in humans to GPR109A [1], [2], [3]. In addition, GPR81 is localized more specifically to the adipose tissue [3]. In 2008, lactate was discovered to be the endogenous ligand for GPR81 [9], [10]. Plasma lactate levels reach concentrations capa
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For another the N terminal sequence of native
2022-01-30

For another, the N-terminal sequence of native glucagon is highly conserved, and positions 8, 9, 16 and 18 are noteworthy in maintaining glucagon activity [18], [20], [21]. It also achieves a degree of selectivity from its C-terminal residues, and a significant contribution is made by the C-terminal
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While ghrelin s role in
2022-01-30

While ghrelin's role in addictive behaviors has been most extensively explored with alcohol, ghrelin has also been implicated in biobehavioral substrates of other drugs of abuse. For example, preclinical experiments suggest that GHS-R1a blockade may improve nicotine [155,156], opioids [[157], [158],
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The mechanism by which Piezo acts
2022-01-30

The mechanism by which Piezo1 acts in the regulation of RBC volume is not firmly established. Its curved structure implies that it is activated by an increase in membrane tension (11), a mechanism indicated by electrophysiological measurements (16). However, the RBC membrane mechanics at its physiol
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