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Covalent inhibitors are well suited for targeting the E
2019-09-10
Covalent inhibitors are well suited for targeting the E1 BRD-K4477 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circu
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br Transparency document br Introduction The cyclic
2019-09-09
Transparency document Introduction The cyclic nucleotide adenosine 3′,5′-cyclic monophosphate (cAMP) exerts both an endothelium-dependent and an endothelium independent vasorelaxant action in rat gssg pathway [1]. cAMP direct, endothelium-independent vasorelaxant effects have been attributed
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There was a measurable worsening but not a statistically
2019-09-09
There was a measurable worsening, but not a statistically significant change in the baseline and follow-up best ear hearing scores, where the mean worsening change was 11.9 dB (95% CI: −1.11–24.86, p-value = 0.070). However, of the 16 patients, 14 (87.5%) were found to have clinically significant wo
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Progesterone s metabolite THP may also be mediating
2019-09-09
Progesterone\'s metabolite, 3α,5α-THP, may also be mediating burying and freezing responses. Results show female Long–Evans rats in behavioral estrous have higher P4 levels in serum, Benidipine HCl and hippocampus compared to diestrous female Long–Evans rats. Additionally, ovx female Long–Evans rat
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Endothelial dysfunction has been associated with most of
2019-09-09
Endothelial dysfunction has been associated with most of the established cardiovascular risk factors, such as hypercholesterolemia, hypertension, smoking, diabetes mellitus, a positive history of premature CAD and elevated ligand gated ion channels homocysteine 4, 26, 27. Endothelial dysfunction is
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br Introduction Epidermal growth factor
2019-09-09
Introduction Epidermal growth factor receptor (EGFR)-activating-mutant non-small cell lung cancer (NSCLC) often initially responds well to EGFR tyrosine kinase inhibitors (TKIs) (Haber et al., 2011); however, the disease almost always recurs about 10–13 months of therapy. Analysis of clinical spe
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Structure similarity searches were conducted
2019-09-09
Structure similarity searches were conducted using the standalone version of the DALI program with the query structures scanned against a local current version of the PDB that has all chains as separate entries (Holm and Sander, 1995). The structural hits for each query were collected, even if the D
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In the past few years neuroprotection via GLP R activation
2019-09-09
In the past few years, neuroprotection via GLP-1R activation has been shown in several animal models of stroke, Alzheimer\'s, Parkinson\'s, Huntington\'s, ALS and traumatic XAP044 and injury. This research field is rapidly growing and several reviews have been recently published (Darsalia et al., 20
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One of the hallmarks of the terminal stages
2019-09-09
One of the hallmarks of the terminal stages of apoptosis is the fragmentation of chromosomal DNA that proceeds in a two-step manner: the DNA is initially cleaved into 50–300kb fragments and eventually into oligonucleosomal pieces [12], [13]. The two major apoptotic nucleases are DNA fragmentation fa
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br Materials and methods br Statistical
2019-09-09
Materials and methods Statistical analysis All statistical analyses were performed using SPSS software version 20. Protein Metronidazole data of DNMTs and clinicopathological parameters were collected. Mann-Whitney U Test was used to assess the differential expression of nonparametric data of
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br Introduction In mammals there are ten
2019-09-09
Introduction In mammals there are ten known isoforms of the enzyme diacylglycerol kinase (DGK), as well as gene splice variants. Enzymes of this family all have a homologous active site but differ widely in their molecular mass, mechanisms of activation and biological function (Shulga et al., 201
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A range of inhibitors were therefore
2019-09-09
A range of inhibitors were therefore synthesized containing either carboxylic Sodium Picosulfate or ester functionality at the ‘tail’ group as well as variations in the ‘head.’ These were assayed in vitro using the DCIP assay for binding affinity against and human DHODH at 50μM, respectively (). An
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ulixertinib br Pre clinical combination studies using CSF CS
2019-09-09
Pre-clinical combination studies using CSF-1/CSF-1R inhibitors In preclinical models, the CSF-1R pathway can be blocked by using either small molecule kinase inhibitors (GW2580 [30], PLX3397 [31], Ki20227 [32], BLZ945 [33] and CYC11645 [34]), antibody-mediated inhibition of CSF-1 using 5A1 [35] o
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This work aimed to investigate whether the
2019-09-09
This work aimed to investigate whether the increase in liver lipid depots, observed in the fetuses from rats fed a saturated-fat-rich diet, persists later in life in the offspring (a) at 21days of age immediately after weaning and (b) at 140days of age, after healthy nourishing. Furthermore, we want
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Heparin LP a levels are lowered by combined oral hormone
2019-09-09
LP(a) levels are lowered by combined oral hormone therapy [80], [81], [82], [83], [84], whereas for most studies using transdermal HRT little or no changes have been observed [85], [86], [87]. Oral versus transdermal administration In general most markers are influenced in a similar way by oral
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