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Collectively the results presented here provide new
2021-03-03

Collectively, the results presented here provide new insights into ligand binding, clustering, spatial distribution, and phosphorylation of DDR1b and DDR2 in response to soluble collagen I. As depicted in the cartoon of Scheme 1, we postulate a model in which the spatial distribution and assembly of
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Our recent discovery M P H R
2021-03-03

Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w
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To elucidate the potential mechanism underlying osteosarcoma
2021-03-03

To elucidate the potential mechanism underlying osteosarcoma cell growth decrease by CDK4 inhibition, flow cytometry analysis was used to determine NPE-caged-proton and apoptosis in human osteosarcoma cells after palbociclib treatment. The results showed that osteosarcoma cells were arrested in G1 p
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In recent years there has been
2021-03-03

In recent years there has been a dramatic increase in identification and optimization of potent CRTh2 antagonists which may not only inhibit the recruitment and activation of Th2 cells but also accelerate apoptosis and clearance of these cells from inflamed tissue, thereby promoting the resolution o
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The question remained as to why hCrm was functional
2021-03-03

The question remained as to why hCrm1 was functional and mCrm1 was not in terms of Rev and HIV mRNA nuclear export, and previously we proposed three possibilities (Elinav et al., 2012). One was that human Paprotrain had a positively acting factor that somehow stabilized the hCrm1 and Rev-RRE comple
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br Conflict of interest statement br References and
2021-03-02

Conflict of interest statement References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Acknowledgements We acknowledge financial support by the Swiss State Secretariat for Education, Research and Innovation (Federal
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In conclusion we for the first time
2021-03-02

In conclusion, we for the first time demonstrated the enzyme activity and immunoprotective traits of bioactive recombinant SjCE-2b, which was successfully recovered by protein refolding from inclusion bodies. The results address two essential questions that were undocumented in previous investigatio
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br Signaling of DDR receptor and its regulation
2021-03-02

Signaling of DDR2 receptor and its regulation Being the tyrosine kinase receptor, downstream signaling of DDR2 receptor is initiated by phosphorylation of cytoplasmic tyrosine residue upon ligand binding (Type II collagen) but the authentic facts or detail information of tyrosine phosphorylation
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ion channel br Acknowledgements br Introduction Three struct
2021-03-02

Acknowledgements Introduction Three structurally related fungal metabolites have been isolated from chloroform extracts of submerged rice cultures of Aspergillus terreus 23-1 from stored unhulled rice in Taiwan; these were named territrems A–C to indicate their biological origin (A. terreus) a
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br Conclusion br Conflict of interest br Acknowledgment
2021-03-02

Conclusion Conflict of interest Acknowledgment The authors acknowledge the grant support of the Tehran University of Medical Sciences (94-02-49-29647). Introduction Earlier in vitro observations have also established that the human 5-HT2A, while very similar to the rat isoform, exhibits
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GF 109203X receptor The folate pathway plays an essential
2021-03-02

The folate pathway plays an essential role in cell survival by generating 5, 10-methylene tetrahydrofolate as a one-carbon donor for the synthesis of deoxythymidine monophosphate (dTMP), purines, methionine and histidine. Disruption of this pathway leads to the critical deficiency of these key molec
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The aniline R group was extensively explored and a large
2021-03-02

The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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The use of inhibitors clearly
2021-03-02

The use of inhibitors clearly has its caveats and the field should come to a consensus on etomoxir concentration to maximally block LC-FAO while minimalizing off-target effects. The current papers convincingly show that 200 μM is too high, but it should be noted that 3 μM does not fully suppress LC-
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rotenone synthesis The MOF system described by Farha
2021-03-02

The MOF system described by Farha and coworkers combines rational design of the support and good experimental results regarding activity and stability. However, a further increase in the speed of enzyme loading into the MOF and a decrease in leaching are still required. How can the design rules prop
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Modulating protein stability specifically inhibiting ubiquit
2021-03-01

Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here
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