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br Conclusions br Conflict of interest statement br Acknowle
2021-07-20

Conclusions Conflict of interest statement Acknowledgments This research was funded by São Paulo Research Foundation (FAPESP) (ProcessN. 2012/08621-1). Thanks to F.J.H. Blázquez and the staff of the Laboratório de Anatomia Microscópica e Imuno Histoquímica (LAMIH − FMVZ − USP) for the permi
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The in vivo IC M in
2021-07-20

The in vivo IC (0.0003μM) in the adipose tissue assay is in very good agreement with the in vitro IC (0.0005μM), and it is larger than the one measured in the OLTT assay (0.00005μM) for this compound. These differences in in vivo IC between OLTT and TAG synthesis are expected as we used free ST 2825
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Our study demonstrated that the sequential events of PKA and
2021-07-20

Our study demonstrated that the sequential events of PKA and AMPK activation were involved in kinsenoside-mediated lipolysis. Within 1 h, PKA transiently inhibited AMPK activation by mitigating LKB1-mediated AMPK phosphorylation at Thr172, and PKA reduced AMPK-mediated phosphorylation at HSL-Ser565
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br Advantages of modified proteins
2021-07-20

Advantages of modified proteins over unmodified ones In contrast to small-molecule drugs, proteins are readily amenable to site-specific alterations through genetic engineering. In principle, therefore, it is possible to build in features that allow them to remain active for longer in the body an
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The following is the supplementary data related to this
2021-07-20

The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter
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On the other hand the properties
2021-07-20

On the other hand, the properties of collagen materials could be efficiently improved by proper chemical modification. The crosslinking agents for collagen generally involve aldehydes (e.g., glutaraldehyde (GA), isocyanates (e.g., hexamethylene diisocyanate (HMDI), photoreactive agents, polyepoxy co
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Rapalink-1 The present study sought to determine if chlorodi
2021-07-20

The present study sought to determine if chlorodifluoroacetophenones, such as 3 and 4, were amenable to a radiolabelling methodology to generate potential 18F imaging agents with high cholinesterase affinity. A number of procedures have been reported for the synthesis of trifluoromethyl ketones, inc
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ERR and ERR share high sequence homology at their DNA
2021-07-19

ERRα and ERRγ share high sequence homology at their DNA binding domain (98% identity) and bind response elements in a similar fashion (Fig. 3 and Liu et al., 2005), yet ERRγ shows high variability in its capacity to stimulate the different response elements, whereas ERRα does not (Fig. 6A). For exam
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An important focus of the present study has been the
2021-07-19

An important focus of the present study has been the interaction of HUVECs with extracellular matrix in the regulation of angiogenesis. Matrigel is a gelatinous protein extract secreted by Engelbreth–Holm–Swarm mouse sarcoma cells, and is considered to be a good model of the extracellular matrix (Kl
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The effects of the endocrine active agents on hepatic
2021-07-19

The effects of the endocrine active agents on hepatic ERα were varied. Both nonylphenol and genistein caused an increase in hepatic ERα in female rats, whereas EE2 did not. It is doubtful that the small changes in hepatic ERα induced by genistein and nonylphenol in female rats are sufficient to alte
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The differences between ground and transition state properti
2021-07-19

The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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br In half a century after
2021-07-19

In 2015–2016, half a century after its first biochemical characterization as a template-independent polymerase, it was shown that TdT can, firstly, assemble a DNA synapsis by itself, optimally with one micro-homology base-pair between strands [] and secondly, perform a template-dependent nucleotid
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We recently reported that the information about the
2021-07-19

We recently reported that the information about the electronic density obtained from a QTAIM analysis is useful to describe the molecular interactions that stabilize and destabilize the different complexes L-R [13], [14], [15]. Specifically in our previous work reported for DHFR inhibitors, the QTAI
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Contrary to genetic aberrations epigenetic
2021-07-19

Contrary to genetic aberrations epigenetic methylation markers with broad coverage of OvCa subtypes were detected in primary tumors [21]. Ibanez de Caceres et al. [22] identified hypermethylation of BRCA1, APC, p16, p14, DAPK or RASSF1A in 50 of 50 primary tumors. Moreover the methylation pattern wa
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In conclusion our work provides the preclinical evidence
2021-07-19

In conclusion, our work provides the preclinical evidence showing the potent in vivo efficacy of AT7519 on chemoresistant cancer e-mail and its underlying mechanisms of action. Our work supports the biological rationale behind the clinical trials initiated with AT7519, particularly for the treatmen
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