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Alvocidib flavopiridol is a piperidine chromenone
2020-04-16
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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Recently we have created CRISPR Cas
2020-04-16
Recently, we have created CRISPR/Cas9-mediated col14a1a knockout fish to interrogate the function of col14a1a during regeneration using the caudal fin model. Using AFM, we showed that collagen XIV-A transiently acts as a molecular spacer responsible for BM biomechanics possibly by helping laminins i
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Labetalol HCl Recently we have created CRISPR Cas
2020-04-16
Recently, we have created CRISPR/Cas9-mediated col14a1a knockout fish to interrogate the function of col14a1a during regeneration using the caudal fin model. Using AFM, we showed that collagen XIV-A transiently acts as a molecular spacer responsible for BM biomechanics possibly by helping laminins i
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To develop novel EPAC inhibitors Zhou and co
2020-04-15
To develop novel EPAC inhibitors, Zhou and co-workers optimized the HTS hit as the chemical lead. After modifications of the substituents on the phenyl ring or C6-position of compound , compound () was identified to be the more potent compound in this series with an IC value of 4.0µM (EPAC2). Dock
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The Wnt catenin signaling pathway is a downstream target
2020-04-15
The Wnt/β-catenin signaling pathway is a downstream target of SOX9 and is involved in a variety of cellular responses, including cell migration, proliferation, and differentiation [14]. Several studies have identified the Wnt/β-catenin signaling pathway as essential for cartilage function, and it is
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It has been shown that DAPK induces
2020-04-15
It has been shown that DAPK induces cell death through an increase in DAPK catalytic activity and subsequent phosphorylation of target proteins (Shang et al., 2005, Yamamoto et al., 2002), but its multidomain structure enables also a close physical interaction with other proteins (Bialik and Kimchi,
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br Materials and methods br Results br Discussion CDK has
2020-04-15
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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An important role for the precursor molecule of
2020-04-15
An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener
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br Future perspectives Understanding how peptides are degrad
2020-04-15
Future perspectives Understanding how peptides are degraded, particularly those which may be therapeutically useful, such as GLP-1, has proved to be invaluable in providing a rationale for the development of a novel class of therapeutic agents. However, while DPP-4 plays an important role in the
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br Related work Goal of this section is to
2020-04-15
Related work Goal of this section is to show related work focused on methods useful to assess the reliability of clustered COTS-based systems. Connelly et al. [1] propose an approach to delineate safety assurance for the use of COTS OS in safety-related applications, which must fall in SIL2. The
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Cy5 carboxylic acid (non-sulfonated) In principle in vitro t
2020-04-15
In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized Cy5 carboxylic acid (non-sulfonated) lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transf
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Besides being the only enzyme E is
2020-04-14
Besides being the only enzyme, E1 is also the largest and arguably most complex protein encoded by papillomaviruses. As the replicative helicase, E1 plays a central role in the viral life cycle. To do so, E1 engages in multiple protein–protein and protein–nucleic W 54011 synthesis interactions to c
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GLP signaling mediates important renal functions
2020-04-14
GLP-1 signaling mediates important renal functions [101], as suggested by the expression of both DPP-4 and GLP-1R in the kidney of several species, including humans [102]. However, controversial data exists on the specific expression pattern of these proteins, based on the specificity and sensitivit
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Acknowledgments br Introduction Steroidogenesis the process
2020-04-14
Acknowledgments Introduction Steroidogenesis, the process of testosterone synthesis, occurs in the adrenal cortex, testis and ovary, and it is controlled by luteinizing hormone (LH), which is synthesized and secreted from the pituitary (Hanukoglu, 1992, Payne and Youngblood, 1995). In the testis
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The work described by Dong Groves and co workers tested
2020-04-14
The work described by Dong, Groves, and co-workers (11) tested the hypothesis that neural stem cell development is sensitive to the clustering and mechanical state of the EphB4:ephrin-B2 receptor-ligand complex. They show that the quality of ephrin-B2-ligand signaling depends on its biophysical stat
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