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Contrary to the downregulation of
2020-11-18

Contrary to the downregulation of S1PR family GPCRs, CLL cells have increased mRNA expression of the lysophosphatidic blue (LPA) family receptors LPAR1, LPAR3 and LPAR4 compared to normal B cells [47]. Increased LPAR1 mRNA has been shown to be associated with more aggressive disease [47] and LPA si
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br Significance Our understanding of the
2020-11-18

Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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The members in apple are similar in
2020-11-18

The 8 members in apple are similar in number to the 7 in Arabidopsis and the 8 in rice, but fewer than the 10 found in mammalian species. GenBank numbers have also been reported for DGK homologues from tomato (AW035995), maize (AY106320), wheat (BT009326), a Populus cross (BU828590), grape (CB981130
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br Diacylglycerol kinases and T cell responses
2020-11-18

Diacylglycerol kinases and T cell responses Diacylglycerol kinases and cancer Several studies implicate DGKα in tumor progression, but its function is debated, as it might also have roles as a tumor suppressor. Diminished DGKα expression is linked to malignant transformation in epithelia. High
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Acknowledgments We are grateful to Dr Jean Marie Bernassau f
2020-11-18

Acknowledgments We are grateful to Dr. Jean-Marie Bernassau for his leadership in establishing our virtual screening platform and Dr. Julie Bick for protein purification. X-ray data collection for compound 4 was performed by Shamrock Structures at Southeast Regional Collaborative Access Team (SER-C
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Compound was advanced to a
2020-11-17

Compound 52 was advanced to a chronic efficacy study in db/db mice maintained on a high fat diet. Animals were dosed with 0.5% methylcellulose vehicle, Punicalin 52 (1, 3 or 15mg/kg, po, Q.D.) or 1 (0.3mg/kg) for 14days. Over the course of the study body weight and food intake were measured daily f
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br Results and Discussion br
2020-11-17

Results and Discussion Materials and Methods Acknowledgements Introduction Inorganic pyrophosphate is generated as a by-product in several enzymatic reactions in cells. These reactions include DNA and RNA synthesis, activation of fatty acids and amino acids, as well as synthesis of the c
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Moreover recent structural studies of VEEV
2020-11-17

Moreover, recent structural studies of VEEV nsP2pro in complex with E-64d revealed an important molecular interaction at the interface of two subdomains. In this structure, Asn475 which is in polar contact with carbonyl oxygen of Asp507 of the protease subdomain makes an H-bond with Arg662 of the MT
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hypoxia inducible factor The CysLT receptor antagonist BayCy
2020-11-17

The CysLT2 receptor antagonist BayCysLT2RA significantly suppressed multiple antigen challenge-induced infiltration of eosinophils and mononuclear hypoxia inducible factor into the lung, indicating that CysLT2 receptor activation is involved in leukocyte migration. In contrast to the present finding
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br Material and methods br
2020-11-17

Material and methods Results Discussion Monomeric CDK5 shows no enzymatic activity and requires the association with a regulatory partner for activation (Dhavan and Tsai, 2001). Here, we found that CDK7 might be one of the partners required for activation of CDK5 in the skin tissue, based o
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Alvocidib flavopiridol is a piperidine chromenone http www
2020-11-17

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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br Most reported binding data are
2020-11-17

Most reported binding data are obtained by performing heterologous competition binding experiments and expressing the results as relative binding affinity (RBA). The constructed binding curves should theoretically be sigmoidal in shape with a Hill slope value of one, for a single ligand binding to
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br Discussion Estradiol is known as one of
2020-11-17

Discussion Estradiol is known as one of the stress signaling molecule [3,4,14]. Here, we showed that PH induced estradiol production before hepatocyte proliferation (Fig. 1). Conversely, the ovariectomized and orchitectomized mice produced less estradiol after PH, and had delayed liver regenerati
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Being a rare renal tumor its description as primary renal
2020-11-17

Being a rare renal tumor, its description as primary renal tumor has been confined to the documentation of anecdotal case reports in the past [4], [9], [10], [11]. However, recent years have seen an increased interest in defining ES/PNET of kidney as a distinct entity, with the study undertaken by t
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br Introduction As a serine proteinase
2020-11-17

Introduction As a serine proteinase and a sub-family of the chymotrypsin-like proteinase, Glutamyl endopeptidase (GE), which is mainly found in Bacillus species, specifically cleaves negatively charged amino 7-Ethoxyresorufin residues (Glu/Asp) (Yokoi et al., 2001). Madsen et al. (Madsen & Qvist
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