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Although we observed increases in AR mediated cAMP
2020-12-14

Although we observed increases in α1-AR mediated cAMP production separately in the nucleus and cytoplasm, compartment specificity was observed for PKA activation. GPCRs and their effector proteins are commonly found in multiprotein signalosomes with A-kinase anchoring proteins (AKAPs) serving as sca
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The question arises as to how the massive conformational cha
2020-12-12

The question arises as to how the massive conformational changes determining whether APC/CCDC20–MCC is inhibited or able to catalyze MCC ubiquitylation are naturally controlled? This transition likely involves APC/C regions near the subunit APC15, because reducing cellular APC15 levels stabilizes MC
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SEW 2871 br Results br Discussion The ubiquitin system
2020-12-12

Results Discussion The ubiquitin system has in recent years become an exciting area for drug discovery (Cohen and Tcherpakov, 2010), as multiple enzymatic steps within the ubiquitylation process are druggable. The potential of targeting the ubiquitin-proteasome pathway was first demonstrated i
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DNA methylation is associated with transcriptional silencing
2020-12-12

DNA methylation is associated with transcriptional silencing of tumor suppressors or other genes important for normal cellular function and plays an important role in the development of cancer and other diseases (such as breast and colorectal cancers) [19]. DNA methyltransferases (MTases) are a fami
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Because conventional KO mice die within h of birth
2020-12-12

Because conventional KO mice die within 24h of birth, it is difficult to analyze higher npy receptor functions using them. Therefore, in this study, we generated brain-specific conditional DGKδ-KO mice and used these mice to perform behavioral and pharmacological tests. Results Discussion OC
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Group B phytocystatins are also expressed in caryopses Altho
2020-12-12

Group B phytocystatins are also expressed in caryopses. Although their expression patterns during germination are similar to those of the group A inhibitors, their expression patterns during seed development vary, indicating that they play different roles in the latter process. The highest levels of
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Quercetin competitively inhibited BFC activity in
2020-12-11

Quercetin competitively inhibited BFC activity in human recombinant cDNA-expressed CYP3A4 with Ki=15.4±1.52μM, and myricetin noncompetitively with Ki=74.6±7.99μM (Fig. 4). The degree of inhibition by quercetin was not affected by a pre-incubation step and was similar in the microsomes from both gend
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angiotensin ii causes Alvocidib flavopiridol is a piperidine
2020-12-11

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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These evidence prompted us to investigate the effectiveness
2020-12-11

These evidence prompted us to investigate the effectiveness of CT-133, a newly discovered, well-tolerated, selective and potent CRTH2 antagonist, as a treatment of ALI. CT-133 has shown a potential response in treating chronic obstructive pulmonary disease (COPD), allergic rhinitis and formula for d
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Immunofluorescence Cells were fixed with
2020-12-11

Immunofluorescence. Cells were fixed with 4% paraformaldehyde (PFA) in PBS and extracted by 0.5% Triton X-100-PBS, or fixed in cold methanol. The cells were immunostained with mouse monoclonal calculating dilution against α-tubulin (Sigma), γ-tubulin (Sigma), Ran (Upstate), rabbit polyclonal antibo
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br Proposed methodology At the outset the
2020-12-11

Proposed methodology At the outset, the wind power outputs must be obtained which are to be included in the OPF model. This work utilizes a modified version of the simulation method. Rather than using the simulated wind power values for each hour of the year, the probability of each wind power in
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6XHis br Study br Study meta
2020-12-11

Study 1 Study 2: meta-analyses Discussion Ten studies have examined the associations of 5-HTTLPR and COMT Val158Met with alexithymia. However, the findings were mixed. In this study, we found that neither the 5-HTTLPR nor COMT Val158Met is associated with alexithymia. The previous findings
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Low estrogen levels in young
2020-12-11

Low BHQ levels in young women, irrespective of etiology, might have harmful effects on cardiovascular physiology. Indeed, a study in premenopausal women with low estrogen levels owing to hypothalamic hypogonadism showed an increased incidence of angiographic CAD in these women compared with premeno
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ABT br Advent of SMEPT br SMEPT
2020-12-11

Advent of SMEPT SMEPT for localized synthesis of nitric oxide Critical evaluation and outlook Examples discussed in this review present SMEPT as a methodology for localized drug synthesis – a unique opportunity for site specific therapeutic interventions using implantable biomaterials. This
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Difopein The role of ETB clearing
2020-12-11

The role of ETB clearing receptors has been studied in detail in endothelial cell–specific ETB knock-out mice. In these animals, clearance of an intravenous Difopein of labeled ET-1 was reduced significantly compared with wild-type controls. Importantly, functioning ETB were retained on all other c
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