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Grapiprant is a selective antagonist for prostaglandin E
2019-08-14

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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Potential break through technology poised to
2019-08-14

Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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Importantly we observed significantly the reduced myocardial
2019-08-14

Importantly, we observed significantly the reduced myocardial infarct size, the improved left ventricular function and the inhibited fibrosis after I/R with oral GA-BH4 supplementation before ischemia (Fig. 1, Fig. 2, Fig. 3). Usually, there is a view that the antioxidation induced by reducing agent
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For any vector let and For let The information matrix
2019-08-14

For any vector , let , and . For , let The information matrix for the partial likelihood at Eq. (2.2) can be expressed as It is well known that GGsTop msds under certain regularity conditions such as (A)–(D) in Andersen and Gill (1982), where and denote the maximum likelihood estimator from E
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Another layer of CK regulation in
2019-08-14

Another layer of CK1 regulation in the Hh and Wnt pathways is to employ different CK1 isoforms to phosphorylate distinct pathway components or even distinct sites on the same substrates. In this regard, it has been shown recently that the membrane-associated CK1 isoform CK1γ, but not the cytosolic i
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In the present study we investigated the role played
2019-08-13

In the present study, we investigated the role played by CRF1 and CRF2 receptors located within the mouse PAG on the anxiogenic and antinociceptive effects produced by local infusion of CRF. To block CRF receptors, we used the selective CRF1 and CRF2 ampicillin sodium antagonists, respectively, NBI
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AZD 3965 Various domains of the HSA molecule have also
2019-08-13

Various domains of the HSA molecule have also been used to make bioconjugates with increased stability, better targeting properties, and/or extended half-lives in blood. For example, domain I of HSA has been used in the preparation of antibody conjugates. This was achieved through the use of a cyclo
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In the original ELF study patients
2019-08-13

In the original ELF study [7], patients were considered eligible if they were due to undergo liver biopsy for the investigation of chronic liver disease, defined as abnormal biochemical liver function tests persisting for more than 6 months, ability to provide informed consent and age between 18 and
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faah inhibitor Diclofenac ibuprofen and meloxicam are consid
2019-08-13

Diclofenac, ibuprofen, and meloxicam are considered among the most commonly used NSAIDs in many countries [4]. Cardiovascular events were reported with these NSAIDs in several clinical studies. In this study, we provide novel information that diclofenac and ibuprofen altered gene expression and may
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br Experimental Procedure br Acknowledgment This work
2019-08-13

Experimental Procedure Acknowledgment This work was supported by Ministry of Education, Singapore (MoE Tier-2) grant (R-154-000-625-112) and R154-000-A72-114 (AcRF Tier 1 grant) respectively. We acknowledge the Advanced Photon Source Beamline 24-ID-C, Argonne National Laboratory, USA. D.N. is
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In this work we fabricated a kind of
2019-08-13

In this work, we fabricated a kind of multifunctional nanoparticles, based on HAuNS coated by chitosan-stearic AICAR copolymer (CSO-SA), which was employed frequently to form micelles for hydrophobic drug delivery in our previous work [21], [22]. The nanoparticles can encapsulate DiR efficiently, a
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br Material and methods br Results and discussion
2019-08-13

Material and methods Results and discussion Conclusions Prostanoid-E receptor selective antagonists that inhibit EP2 or EP4 receptor activities may be used as a pharmacological strategy to limit cyst formation and ADPKD progression. Our study follows on from our previous observations of the
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The repair pathway of DNA DSBs through
2019-08-13

The repair pathway of DNA-DSBs through HR and the role of BRCA1 in repair kinetics by HR is also an important factor to unravel the radiation sensitization of novel small molecule inhibitors. The involvement of the breast cancer susceptibility gene 1 (BRCA1) in tumorigenesis and its role in facilita
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A An optimized BEI SEIscore based on the
2019-08-13

(A) An “optimized BEI-SEIscore” based on the trends, emerged from the statistical analysis of several optimization studies in pharmaceutical industry (Abad-Zapatero, 2007, Abad-Zapatero and Blasi, 2011). This type of optimized scores has been used in many previous studies. Ki=1nM at 300° K, compare
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Social interaction is known to be the main source of
2019-08-13

Social interaction is known to be the main source of stress in human beings (Dickerson and Kemeny, 2004, Tamashiro et al., 2005). An animal model of social stress should closely mimic real-life situations in human life (Neisewander et al., 2012); in this context, social defeat in an agonistic encoun
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