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Despite their undisputed importance however FPR receptors ar
2021-12-20
Despite their undisputed importance, however, FPR receptors are not in the limelight of GPCR-related research (for review [12] and references therein). We, therefore, draw attention to this GPCR receptor family, in order to re-initiate FPR-related research, particularly in the light of biased agonis
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The co crystal structure of GPR complexed with TAK provided
2021-12-20
The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly
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Apoptosis is one of critical toxic mechanisms of benzene met
2021-12-20
Apoptosis is one of critical toxic mechanisms of benzene metabolites. In this work, overexpression of HIF-1a could significantly reduce the increase in cell apoptosis caused by 40 μM BQ. At the meanwhile, anti-apoptotic protein Bcl-2 level was significantly elevated in HIF-1a overexpression cells th
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The central region of Azalanstat can be substituted
2021-12-20
The central region of Azalanstat can be substituted with connecting alkyl chains of different nature and length. Interesting results were given by compounds with a four or five AICAR phosphate receptor chain, incorporating heteroatoms, such as oxygen (Fig. 2, compound 4) or sulfur, and different fun
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To identify structurally novel autophagy inhibitors a
2021-12-18
To identify structurally novel autophagy inhibitors, a medium throughput screen of our in-house library of approximately 160,000 compounds was performed. In the screening assay, MCF7 Nitidine chloride stably transfected with eGFP-tagged light chain 3 (LC3), were employed, which can be detected by a
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The PAS and CC domains of sGC have been studied
2021-12-18
The PAS and CC domains of sGC have been studied less by comparison, though their function in sGC signal transduction is likely important. PAS domains are versatile as they can play varied roles in different proteins, such as quaternary structure organization, cofactor binding, and signal transductio
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gaba receptor agonist br Concluding remarks br Conflict of i
2021-12-18
Concluding remarks Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We thank all the present and former members in our laboratory for their contributions to
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We previously evaluated the immuno modulatory efficacy
2021-12-18
We previously evaluated the immuno-modulatory efficacy of GSNO in different EAE models and reported prophylactic and therapeutic efficacy of GSNO against the clinical disease of EAE [22], [36]. GSNO inhibited the IL-6-induced STAT3 activation (Tyr705 phosphorylation) by S-nitrosylation of the STAT3
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br Materials and methods br Results
2021-12-18
Materials and methods Results Discussion The compound P7C3 has been reported to activate NAMPT (Wang et al., 2014) and augment NAD+ levels, thereby promoting the survival of mature neurons and postnatal neurogenesis throughout the post-ischemic Macitentan australia (Loris et al., 2017). Ho
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As well as the above studies Meier and
2021-12-18
As well as the above studies, Meier and coworkers used TUG-891, alongside omega-3 fatty acids, to show a potential role for FFA4 in inhibiting proliferation of DU145 prostate cancer cells [68]. Given that these cells express both FFA4 and FFA1 and the current view that TUG-891 may not be sufficientl
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The amyloid precursor protein APP is a membrane
2021-12-18
The amyloid precursor protein (APP) is a membrane protein thought to be involved in plasticity, synapse formation and repair, and export of metal ions [68]. The APP present in the brain can be cleaved by three different secretases [73], [74]. Cleavage of APP first by alpha secretase and then gamma-s
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br All platelet agonists acting through specific receptors a
2021-12-17
All platelet agonists, acting through specific receptors and triggering different signaling pathways, activate phospholipases (PLCß or PLCγ) and the subsequent messengers inositol 1,4,5-trisphosphate (IP3) and 1,2 diacylglycerol which activate inositol 1,4,5-trisphosphate (IP3) receptors (IP3R) or
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br Acknowledgements br Introduction The study methods consis
2021-12-17
Acknowledgements Introduction The study methods consisted of the review of articles included in the Pubmed and Medline databases and in the clinicaltrials.gov clinical trials register between 2013 and 2016, and of the preliminary results of therapies presented at international trichology confe
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In addition to their functional
2021-12-17
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic AMI-1 to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unlabele
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hepititis b br Materials and methods br Results
2021-12-17
Materials and methods Results Discussion To fulfill its role in tissue homeostasis, repair and immunoregulation, MSCs must be able to (i) renew themselves by cell division and proliferation, (ii) migrate to its target end-site in response to chemotaxis signals and (iii) undergo appropriate
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