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Interestingly we have shown that OA required FFAR
2022-06-10
Interestingly, we have shown that OA required FFAR4 to induce osteoblast gene expression in MC3T3-E1 pre-osteoblasts, but not to inhibit osteoclastogenesis in RAW264.7 murine macrophages. As previously suggested, FFAR1 may mediate the effects of OA in osteoclasts. However, FFAR1 has also been shown
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Recently they reported an enyne chemotype agonist
2022-06-10
Recently, they reported an enyne chemotype agonist (21, Fig. 13) with low lipophilicity, small polar surface area (PSA) and high potency (Clog P=3.8, tPSA=37 A2, EC50=20nM), further derived from TUG-424. The compound endowed fast oral Nicardipine HCl (tmax=15min) and a decent pharmacokinetic profile
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With the nitrogen containing heterocycle components
2022-06-10
With the nitrogen-containing heterocycle components and the acidic components in hand, the final products were synthesized according to the procedure as depicted in . Reaction of – with various β-substituted phenylpropionic such as (, and ), followed by deprotection by TFA, smoothly provided the c
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Interestingly the subcellular localization of FBPase in hepa
2022-06-10
Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Study Design reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the abi
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Although angiogenesis is crucial for cerebral
2022-06-10
Although angiogenesis is crucial for cerebral ischemic rehabilitation, the mechanism underlying NGF promotion of angiogenesis is not clear. Previous studies showed that angiogenesis can be promoted by FAK, in a breast cancer model [19]. Recent studies showed that FAK phosphorylation participated in
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It is well known that TLR induced inflammation is associated
2022-06-10
It is well known that TLR4-induced inflammation is associated with behavioural alterations including fever, hypolocomotion, altered appetite, anxiety and anhedonia (Dantzer, 2006, Dantzer et al., 2008). The current data demonstrate that while PF3845 potently attenuates TLR4-induced cytokines in the
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In human cancers it has been identified that FOXC AS
2022-06-10
In human cancers, it has been identified that FOXC2-AS1 functions as an oncogenic RNA. For instance, in osteosarcoma, FOXC2-AS1 regulates the expression of FOXC2 at the transcription and post-transcription levels to promote doxorubicin resistance by facilitating ABCB1 expression (C.L. Zhang et al.,
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br Experimental br Results and discussion One of the major
2022-06-10
Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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br Materials and methods br Results
2022-06-10
Materials and methods Results Discussion The major findings of the present study are that: 1) the response to inverse agonists may be crossregulated by the activation of either Nemadectin H1 or H2 receptors, 2) histamine H1 and H2 receptor inverse agonists crossdesensitize the receptor´s r
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Histamine modulates an attentional state which might affect
2022-06-10
Histamine modulates an attentional state, which might affect performances in the object recognition test. Indeed, systemic injection of H3 receptor inverse agonists enhances the attentional state (41). However, the memory recovery in our study is unlikely to be due to the enhanced attentional state.
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br Methods br Acknowledgements We are grateful to Eric Olson
2022-06-10
Methods Acknowledgements We are grateful to Eric Olson for providing Yap/Taz floxed mice, and to members of the Epstein lab for helpful comments and advice. This work was supported by NIH R01 HL118768, R35 HL140018, the Cotswold Foundation and the WW Smith Endowed Chair to J.A.E. The Hippo
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br Conflict of interest br Acknowledgments We thank Professo
2022-06-10
Conflict of interest Acknowledgments We thank Professor Chen Rui (Southeast University, China) for providing plasmid P1P2N-HIF1. This study was supported by research grants from National Natural Science Foundation of China (81573189, 81730087). Introduction The consumption of large amounts
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Therefore we believe that HIF mediated effects
2022-06-10
Therefore, we believe that HIF-mediated effects on CSC markers, apoptosis are mediated through HO-1. Our plan is to look for more mechanistic studies to understand the role of HO-1 degradation products (CO, Fe, and bilirubin) in cellular apoptosis, stemness under hypoxia. The model of role of HO-1 i
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br Author contributions br Conflict of interest
2022-06-10
Author contributions Conflict of interest Acknowledgments We appreciate technical support of the Research Support Center at the Graduate School of Medical Sciences of the Kyushu University. This study was supported by the Uehara Memorial Foundation and a KAKENHI grant from the Ministry of E
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Two distinct mechanisms have been
2022-06-10
Two distinct mechanisms have been described for niacin’s macrophage-based actions [21,22]. First, niacin blocks recruitment of macrophages to atherosclerotic lesions. Second, niacin upregulates macrophage ABCA1 and ABCG1, transporters involved in reverse cholesterol transport. Upregulation of choles
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