• br Materials and methods br

  2021-11-03

  

  Materials and methods Conflicts of interest Some of the peptidomimetic compounds in this work are the subject of the patent application “Peptidomimetics for Imaging the Ghrelin Receptor”, WO/2016/191865 A1, December 8th, 2016. Acknowledgements Special thanks go to Rebecca McGirr (Lawson He

• Gap junctions mediate electrical coupling between cells by

  2021-11-03

  

  Gap junctions mediate electrical coupling between cells by conducting direct ionic currents and thereby modulate their electrical activity (Hormuzdi et al., 2004). In the nervous system, electrical coupling organizes network activity by amplifying and synchronizing neuronal firing (Galarreta and Hes

• br Results and discussion br Conclusions As described above

  2021-11-03

  

  Results and discussion Conclusions As described above, the SAR study based on compound 1 led to the identification of compound 4 as an ideal inhibitor. An enzyme level investigation showed that 4 is a more potent and selective FGFRs tyrosine kinase inhibitor than is Ponatinib. In addition, the

• In a recent study Neelaveni

  2021-11-03

  

  In a recent study, Neelaveni et al. [47] revealed that new thiazolidinedione derivatives (Fig. 6 a and 6 b) produced dual PPARγ and FFAR1 agonistic activity at micromolar concentrations with insulin sensitizing effects and enhanced insulin secretion from the pancreas. These derivatives were reported

• Our previous study had shown that silencing FFAR expression

  2021-11-03

  

  Our previous study had shown that silencing FFAR1 expression weakened the action of PIO in increasing insulin secretion in lipotoxic β Nitazoxanide synthesis [6]. Resent research found that PIO promoted insulin secretion by upregulating FFAR1 [17]. Therefore, we presumed that FFAR1 may be involved

• br Materials and methods br Results

  2021-11-03

  

  Materials and methods Results Discussion Protein degradation plays a vital role in nearly all cellular processes, nearly 5% of genes are dedicated to the control of protein stability [31], [32]. The ubiquitin-proteasome system (UPS) represents the major way for degradation of proteins, wher

• Importantly both genetic deletion and pharmacological inhibi

  2021-11-03

  

  Importantly, both genetic deletion and pharmacological inhibition of FAAH also reduced NTG-induced neuronal hyperactivity in the trigeminal nucleus, which receives sensory input from craniofacial deep tissues. NTG is known to evoke the robust neuronal activation, as evidenced by the induction of the

• Neuropathic pain NP is a chronic pain

  2021-11-03

  

  Neuropathic pain (NP) is a chronic pain caused by lesion or disease affecting any part of the nervous system leading to clinical conditions ranging from painful neuropathy to poststroke central pain. Anticonvulsant drugs, Gabapentin and Pregabalin, acting on αδ subunit-containing voltage-dependent c

• A biochemical characterisation of this functionally crucial

  2021-11-02

  

  A biochemical characterisation of this functionally crucial LSD1-p53 interaction is the focus of this study. Using several complementary assays [29], [30], [31], [32], we find that a well-defined segment of p53-CTD is capable of binding to LSD1 active site, thereby inhibiting the enzymatic activity

• br Conflict of interest br Acknowledgements

  2021-11-02

  

  Conflict of interest Acknowledgements This work was funded by the University of Turin (ex60% 2014), World Wide Style Project (WWS; University of Turin/Fondazione CRT) and University of Florence (ex60% 2014). ACR and AP designed the study; AP, EB and IO conducted the literature search and analy

• Thus synthesized thienopyrimidine derivatives were evaluated

  2021-11-02

  

  Thus synthesized thienopyrimidine derivatives were evaluated in vitro for GPR119 agonistic activity, and the results are summarized in , , . First, we fixed the 4-methylsulfonylphenyl substituent at the R position on the thienopyrimidine ring, and derivatized at the R position. As shown in , and s

• The mechanisms of action of

  2021-11-02

  

  The mechanisms of action of MMF and DMF are not well understood, but a growing body of evidence has demonstrated that DMF may act on both the neurodegenerative and inflammatory response of MS patients. The majority of the data related to the mechanism of action of DMF/MMF demonstrates the associatio

• br Methods br Results br Discussion The measurement

  2021-11-02

  

  Methods Results Discussion The measurement of intraocular pressure was made with a commercially available rebound tonometer, the Tonovet®. In our studies, Tonovet® underestimated the intraocular pressure in both animal models, being this effect more pronounced in the rat. To study the effe

• An advantage of photolabeling with tritiated photoprobes

  2021-11-02

  

  An advantage of photolabeling with tritiated photoprobes followed by microsequencing with Edman degradation is the ability to both identify the photolabeled Caspase-8, human recombinant protein receptor and to quantify photoincorporation which enables assessment of pharmacological specificity and al

• Because FPR is expressed in VSMCs and its

  2021-11-02

  

  Because FPR-1 is expressed in VSMCs and its role in non-hematopoietic cells is still unclear, we questioned whether FPR-1 would have physiological relevance for vascular behavior, in the same way as it does in neutrophils (Ca2+ homeostasis and CX-5461 polymerization). First, we tested if FPR-1 is i

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