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To study systemic potential of the selected
2020-12-18
To study systemic potential of the selected compounds as EP1 receptor antagonist, they were evaluated with regard to the sulprostane-induced increase of intravesical bladder pressure in rats. Some of the analogs, 13 and 15–17, which were selected on the basis of their in vitro EP1 receptor affinity,
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CRT0044876 br Materials and methods br Results
2020-12-18
Materials and methods Results Discussion and conclusion The cardiac hypertrophy model can be established by two methods: drug induction and operation. The drug induction method is simple, while the operation method is closer to the real development of the disease. In this experiment, accord
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br Funding This work was supported by the
2020-12-18
Funding This work was supported by the PACA Region and Avignon Université. Acknowledgements Introduction Cancer is a pivotal health problem all over the world [1]. In spite of enormous advances achieved in diagnosis and treatment over the past decades, it still accounts for over 22000 deat
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Enolases are among the most abundantly expressed cytosolic p
2020-12-18
Enolases are among the most abundantly expressed cytosolic proteins. They are metalloenzymes that catalyze the conversion of 2-phosphoglycerate to phosphoenolpyruvate [18]. Eubacteria and archaebacteria have a single enolase gene (reviewed in [19]). Despite the lack of signal peptides or cognate pro
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adenosine antagonist Expression of both CH H and CYP
2020-12-18
Expression of both CH25H and CYP7B1 by lymphoid stromal adenosine antagonist is required for the synthesis of 7α,25-OHC in lymphoid tissues and the correct positioning of B cells. Production of EBI2 ligand by hematopoietically derived cells appears limited [24] but may occur under some circumstance
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To function as Ub ligases E proteins must interact
2020-12-18
To function as Ub-ligases, E3 proteins must interact with E2s. As compared to the extensive studies on E3s, functional studies on E2s are relatively rudimentary in higher plants. We previously reported that there are 48 genes encoding Ub-conjugating (UBC) fold-containing putative E2 proteins in the
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Compounds were synthesized using a facile step convergent
2020-12-18
Compounds were synthesized using a facile 8-step convergent synthesis ( and ). Briefly, (Boc)cyclen (compound ) was coupled using TBTU to Fmoc- or Cbz-protected amino alkyl acids (–), followed by deprotection using 20% piperidine in DMF, or H on Pd/C, respectively (–) (). Deprotected linkers were co
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br Methods br Results br Discussion
2020-12-18
Methods Results Discussion Preclinical data indicate that nepicastat modulates sympathetic drive to the myd88 inhibitor with a mild pressor effect in various animal models of hypertension (Stanney et al., 1998). However in this clinical study, the doses of nepicastat employed did not signif
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Next we evaluated whether DPP
2020-12-18
Next, we evaluated whether DPP-4 inhibitor suppressed osteoclast formation by downregulating LPS-induced RANKL expression in stromal cells; DPP-4 inhibitor did not inhibit LPS-induced RANKL expression. Furthermore, we evaluated the effect of DPP-4 on LPS-induced RANKL expression in stromal cells, bu
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For LAU extracted ion chromatograms of the blank t and
2020-12-17
For LAU 399, extracted Vinorelbine chromatograms of the blank, t0, and t120 samples for the diagnostic product ion m/z 163.0216 are provided in Fig. S11, and extracted ion chromatograms of the t120 sample for m/z 163.0216 (diagnostic product ion), and m/z 308.1677 and 306.1522 (metabolites) are sho
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br Discussion Our data demonstrate that
2020-12-17
Discussion Our data demonstrate that the bicyclam AMD3100 strongly interacts with CXCR-4, whereas DS and AR177, two other compounds that also interfere with virus entry into the pkm2 (and interfere with virus binding), do not. AMD3100 is a unique compound in that it interferes with the chemokine
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A number of immune relevant
2020-12-17
A number of immune-relevant genes have been studied to explore the immunologic mechanisms in large yellow croakers; however, the chemokine receptor CXCR family has never been studied in this organism. Chemokines are a large superfamily of chemotactic cytokines that are utilized to direct the traffic
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The notion that a small subset of inducible
2020-12-17
The notion that a small subset of inducible cellular transcripts, encoding immunological important factors, is translocated across the nuclear envelope by the karyopherin CRM1 is gaining support from various recent studies. For example, experimental evidence has been provided demonstrating that the
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The aim of the present study
2020-12-17
The aim of the present study was to investigate the participation of CRF1 and CRF2 in the alterations of the dorsal and ventral striatal dopamine release and the vertical and horizontal locomotor activity observed in rats following chronic nicotine treatment and consequent acute withdrawal. In this
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The pyrrolo benzodiazepines PBDs are a
2020-12-17
The pyrrolo[2,1-][1,4]benzodiazepines (PBDs) are a family of antitumour antibiotics that includes the natural products anthramycin and DC-81. They exert their cytotoxicity by covalently bonding to the exocyclic C2–NH group of guanine residues in the minor groove of DNA through their N10–C11 imine fu
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