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thiotepa High throughput screening HTS of the AstraZeneca
2020-05-16
High throughput screening (HTS) of the AstraZeneca thiotepa collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and was
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CDK S phosphorylation status influences the differential cel
2020-05-15
CDK5-S47 phosphorylation status influences the differential cellular proliferation versus migration response: Previous work from our laboratory has shown CDK5 to be a critical determinant of the cellular proliferation-migration dichotomy whereby CDK5 activation downstream of stimulated epidermal gro
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Unlike the CRF receptor the CRF a
2020-05-15
Unlike the CRF1 receptor, the CRF2(a) receptor binds and is activated by agonists with a broad range of potencies. Therefore, we assessed the ability of strong and weak ligands to desensitize retinoblastoma CRF2(a) receptors. Although stresscopin\'s N-terminus is two Minocycline HCl longer than the
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br Conflict of interest statement br Introduction Endothelin
2020-05-15
Conflict of interest statement Introduction Endothelins (ETs) are a family of multifunctional, naturally occurring peptides with long-lasting vasoconstrictor and pressor effects (Zhou et al., 2004). They are synthesized as a large protein, the pre-proET-1 or Big ET-1, which is subsequently cle
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br Guidance of B cell localization
2020-05-15
Guidance of B cell localization by EBI2 EBI2 expression and B cell disease Although chemoattractant receptors of the GPR family play essential roles in coordinating the migration of lymphocytes for efficient responses against pathogens, their dysregulation can result in the initiation or progr
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The larger eukaryotic ligases such
2020-05-15
The larger eukaryotic ligases, such as LigI and LigIV, also possess an additional N-terminal DNA-binding domain (DBD) that is required for efficient ligation (Fig. 1c) and enables these ligases to encircle DNA [17]. An equivalent helix–hairpin–helix domain is also present in the bacterial NAD-depend
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br Conclusion br Competing interests br Authors
2020-05-15
Conclusion Competing interests Authors\' contributions Acknowledgements The work was supported by Aurigene Discovery Technologies (M) Sdn. Bhd., Industrial Doctoral Program sponsorship by Ministry of Higher Education, Malaysia and research grants by the University of Malaya, grant number
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Nepafenac Classical DHFR inhibitors such as methotrexate MTX
2020-05-15
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Nepafenac residues as well as hydrophobic
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In contrast to PEGylated proteins which tend to have reduced
2020-05-15
In contrast to PEGylated proteins which tend to have reduced Curcumin synthesis in the body relative to their native counterparts, proteins conjugated to albumin tend to accumulate in certain locales in vivo. This means that albumin-based drug carrier systems have particular applications in the fiel
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Iris domestica L Goldblatt Mabb syn Belamcanda
2020-05-15
Iris domestica (L.) Goldblatt & Mabb. (syn. Belamcanda chinensis L.) DC. (Iridaceae) occurs naturally in South and East Asia. Despite the fact that former monotypic genus Belamcanda has been included in the extended genus Iris, this classification has been questioned (Wilson, 2011; Mavrodiev et al.,
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Tacrine amino tetrahydroacridine I Fig was the first AChEI t
2020-05-15
Tacrine (9-amino-1,2,3,4-tetrahydroacridine) (I, Fig. 1) was the first AChEI to be approved by the Food and Drug Administration (FDA) for the treatment of AD [25], [26], [27], [28]. However, despite its good AChE inhibitory activity, tacrine was far from ideal due to its low bioavailability and shor
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br Discussion Of the age related differences in serum
2020-05-15
Discussion Of the age-related differences in serum non-cholesterol sterols, we first deal with the cholesterol precursors. After birth, the markedly elevated serum desmosterol values decreased during the first year of life, and after 1 year of age they were similar between the other age groups. S
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To our knowledge immunohistochemical analysis for proGRP was
2020-05-15
To our knowledge, immunohistochemical analysis for proGRP was done in 5 cases [9], [10], [17], [18]. Takagi-Takahashi et al. reported that the tumor WZ3146 were positive for proGRP in one case [9]. Yamaguchi et al. also showed that tumor cells in two patients of ES/PNET with elevated serum proGRP w
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Another important issue in biosensors is to design
2020-05-14
Another important issue in biosensors is to design a simple and potable detection strategy to meet the requirement of the point-of-care (POC) test applications. According to the recent research, by using invertase determining molarity for hydrolyzing sucrose into glucose, the range of personal gluc
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The sixth affected individual individual is a year old
2020-05-14
The sixth affected individual (individual 6) is a 35-year-old female who presented with a complex combination of congenital and acquired symptoms. She was born to healthy, unrelated parents with an unremarkable family history, apart from the presence of polycystic kidney disease in her father and pa
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