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Recently several Pt IV complexes as
2020-07-24
Recently, several Pt(IV) complexes as prodrugs have been designed and studied to enhance anti-tumor efficacy of traditional Pt(II) drugs, improving their cellular uptake and blood-circulation time [26], [27], [28], [29]. Compared with their Pt(II) counterparts, six-coordinated Pt(IV) complexes with
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br Nuclear estrogen receptors Indirect genomic signaling
2020-07-24
Nuclear estrogen receptors: Indirect genomic signaling As mentioned earlier, the transcription of several genes that do not contain EREs in their promoter regions can also be regulated by estradiol, without direct binding of the estrogen receptors to the DNA. According to the most recent reports,
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br Discussion We are reporting
2020-07-24
Discussion We are reporting a cryptic insertion of chromosome 22 material (EWS) to the long arm of chromosome 11 (11q24, FLI-1) recognizable by FISH in nor-NOHA acetate synthesis exhibiting trisomy 8 as the sole cytogenetic anomaly. In ES and PNET tumors, trisomy 8 is the most common secondary a
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br Experimental procedures br Acknowledgments br Introductio
2020-07-24
Experimental procedures Acknowledgments Introduction Receptor tyrosine kinases (RTKs) control many fundamental cellular processes, such as cell proliferation, differentiation, migration, and metabolism (Lemmon and Schlessinger, 2010). RTK activity is normally tightly controlled, and dysregu
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The development of novel approaches to study GPCR mediated
2020-07-24
The development of novel approaches to study GPCR-mediated transactivation in live Rifabutin is important, and this study describes a unique BRET-based quantification of Grb2 recruitment to the EGFR as a direct readout of GPCR-mediated transactivation. We have previously used the recruitment of Grb
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br Results and discussion br
2020-07-24
Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz
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NPC L NPC Niemann Pick C like like intracellular
2020-07-24
NPC1L1 (NPC1 [Niemann-Pick C-like-1]-like intracellular cholesterol transporter) is the rate-limiting transmembrane transporter for cholesterol MS436 sale from the intestinal lumen, and it mediates the absorption of both dietary and biliary cholesterol., , NPC1L1 is the target of the cholesterol-low
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br Author contribution br Acknowledgements We want to thank
2020-07-24
Author contribution Acknowledgements We want to thank Dr. Manuel Rodriguez, Dr. Ch. Blattner, Dr. Jorge Moscat, Dr. Erwin Knecht and Dr. Peter Tontonoz for materials. This work has been supported by grants from the Spanish Ministry of Education and ScienceSAF2011-27442 and a grant from General
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Although we observed increases in AR mediated cAMP productio
2020-07-23
Although we observed increases in α1-AR mediated cAMP production separately in the nucleus and cytoplasm, compartment specificity was observed for PKA activation. GPCRs and their effector proteins are commonly found in multiprotein signalosomes with A-kinase anchoring proteins (AKAPs) serving as sca
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br Materials and methods br Results Overexpression of KLF in
2020-07-23
Materials and methods Results Overexpression of KLF2 increased the cell viability and reduced the LDH leakage rate and O2•− and ONOO− generation in H/R HUVEC model. To evaluate the effect of KLF2 on H/R HUVEC injury, KLF2 was overexpressed in HUVECs. Cell viability and extracellular LDH level
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br Conclusion Conventional surgical excision of
2020-07-23
Conclusion Conventional surgical excision of the tumoral lesions is the primer therapy for the BCC. Recurrence rates are significantly higher for surgical margin positive lesions that also creates challenges for the surgeons on obtaining best cosmetic and oncologic results. In our study, EGFR her
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In general graphene nanoplatelets have many useful
2020-07-23
In general, graphene nanoplatelets have many useful features for the design of multifunctional composite materials, including excellent electrical and thermal conductivities, considerable weight-saving lightness, and high mechanical strength [26]. Moreover, they are characterized by a high specific
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Altogether these data suggested that GlmU might be involved
2020-07-23
Altogether these data suggested that GlmU might be involved in the M. smegmatis biofilm mediated defence mechanisms. GlmU belongs to a metabolic pathway leading to UDP-GlcNAc from fructose-1-phosphate involved in the biosynthesis of peptidoglycan and lipopolysaccharide (Fig. 8). Recently, we demonst
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Cyclin D inhibits the transcriptional activity of the
2020-07-23
Cyclin D1 inhibits the transcriptional activity of the transcription factors myogenin and MEF2 [39,40]. In addition, myogenin activates MEF2 expression, which feeds back to amplify the myogenin promoter [38]. In this study, DGKδ suppression, in addition to the increase of cyclin D1, inhibited myogen
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Alvocidib flavopiridol is a piperidine chromenone http www a
2020-07-23
Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK
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