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Kim et al reported for bioactive compounds originating from
2019-07-30
Kim et al. reported for bioactive compounds originating from the endemic species in Korea, the hexane and EtOAc fractions of the MeOH extracts from the roots of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity b
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P H is a nonheme iron II dioxygenase
2019-07-30
P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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A widely accepted mechanism to differentiate
2019-07-30
A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the metabotropic receptors [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is pivo
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Here we report for the first time
2019-07-30
Here, we report for the first time that EphB4 contains two NLS sequences and localises to the nucleus. This is mediated via an importin-α pathway and we show that EphB4 could potentially have a direct role in gene regulation. These data provide new insight into Eph receptor localisation and action a
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Grapiprant is a selective antagonist for prostaglandin E PGE
2019-07-30
Grapiprant () is a selective antagonist for prostaglandin E (PGE) receptor subtype 4 (EP4) identified as a clinical candidate for the treatment of inflammatory pain associated with osteoarthritis (OA). It is currently under development for use in humans and dogs. The projected dosing regimen of grap
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Introduction PGE is a major mediator
2019-07-30
Introduction PGE2 is a major mediator present at sites of inflammation [1]. It is well established that PGE2 contributes to the localized and systemic symptoms of inflammation. A key study by Portanova et al. [2] demonstrated that anti-PGE2 Liquidambaric acid for were able to reverse the swelling
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br Effects of culture conditions on
2019-07-30
Effects of culture conditions on drug-induced gene death associated protein kinase in primary human hepatocytes Past progress in elucidating the optimal conditions for the long-term cultivation of rodent hepatocytes has helped define some of the key components in the matrix and medium environment
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NAD+ The small intestine in addition to its
2019-07-30
The small intestine, in addition to its primary role of absorption, has the ability to metabolize drugs and other xenobiotics through phase 1 and phase 11 metabolisms [25] since almost all the cytochrome P450 NAD+ present in the liver are also present in the small intestine although, in lower conce
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Regardless of its effect on
2019-07-30
Regardless of its effect on EBV infection, the chemokine system has been found to be regulated in both nasopharyngeal cancer and Hodgkin lymphoma. As such, Hodgkin and Reed–Sternberg (HRS) cells from Hodgkin lymphoma and nasopharyngeal carcinoma cells have been shown to express CXCL8 and CCL17. Furt
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Subgroup analysis showed that patients with
2019-07-30
Subgroup analysis showed that patients with relatively lower CrCl levels (>50–80 mL/min) were more likely to initiate treatment on a lower dose (17% for all DPP-4 inhibitors; 22% excluding linagliptin). Nevertheless, even in patients with higher CrCl value (>80–120 mL/min and >120 mL/min), at least
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Against this backdrop we set
2019-07-30
Against this backdrop, we set out to identify synthetic and endogenous ligands that bind directly to and regulate the activity of Nurr1. Owing to the pivotal role Nurr1 plays in producing and processing dopamine, and the need for neurons to tightly regulate dopamine levels, we postulated that the re
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In this contribution herein we report our newly devised
2019-07-30
In this contribution, herein we report our newly devised molecular probes with a triazole linked benzimidazole-indole-thiazolium mixed heterocyclic framework as depicted in Scheme 1. Their architecture was designed to achieve the advancement in selectivity and specificity toward DNA matrix over RNA
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Introduction Cyclin dependent kinases CDKs
2019-07-30
Introduction Cyclin dependent kinases (CDKs) are a family of proline-directed serine/threonine kinases with roles in regulation of crucial cellular processes such as Tideglusib and transcription [1]. One of the unifying features of this family is its dependence on association with cyclins/cyclin-li
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AMD is equally active against
2019-07-30
AMD3100 is equally active against a broad range of HIV-1 and HIV-2 strains, but not against simian immunodeficiency virus (SIV) strains in human PBMC (De Clercq et al., 1994). At this moment it is not clear what coreceptor SIV is using in human PBMC, but it does not seem to be CXCR-4 (Feng et al., 1
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MTT results show that both pancreatic cell
2019-07-30
MTT results show that, both pancreatic cell lines were quite sensitive to camptothecin (CPT), a well known topoisomerase I poison. Interestingly, CPT does not show any selectivity over cancer cell lines probably due to the duplication times for cancerous (MIA PaCa-2) and immortalized healthy (HPDEC)
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