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It has long been known that native BChE
2020-08-08
It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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Udenafil also has shown the ability to
2020-08-08
Udenafil also has shown the ability to significantly inhibit the decrease of vascular endothelial cell function and inhibit the decrease in endothelial cell and smooth muscle contents, thus preventing their fibrosis within the penile corpus cavernosum in diabetic or hyperlipidemic animal models when
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The intimate interactions between flavonoids and ER have bee
2020-08-08
The intimate interactions between flavonoids and ERα have been more extensively studied than their ERβ interactions because of the dominant role of ERα in some important diseases (Ye et al., 2018) including breast cancer (more than 80% of human breast cancers are ERα positive) (Turner et al., 2015),
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Our previous high throughput screening
2020-08-08
Our previous high-throughput screening (HTS) campaign using automated, robust, and sensitive fluorescence based TOK-001 assay [10], [11] led to the identification of several EPAC specific inhibitors (ESIs), and was subsequently followed by extensive hit-to-lead optimizations [20], [21], [22], [23],
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The selectivity of a ligand for two receptors usually is
2020-08-08
The selectivity of a ligand for two receptors usually is calculated by measuring the equilibrium dissociation constant (KD) for the two subtypes, in this case ETA and ETB, to provide a ratio of selectivity65, 66 in ligand-binding assays. There is no standardized method or general agreement among pha
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Thirty eight papers are reported in
2020-08-06
Thirty-eight papers are reported in PubMed upon the keyword search “DDR1 AND kidney”. Careful examination of those papers shows that only 31 are related to DDR1\'s role in glomerulosclerosis and renal fibrosis, 24 of those being research and the rest review articles. Since the original paper describ
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AT13148 sale This manuscript illustrates the preclinical pha
2020-08-06
This manuscript illustrates the preclinical pharmacological profile of CR3465 (l-Tyrosine, N-[(2-quinolinyl)carbonyl]-O-(7-fluoro-2-quinolinylmethyl) sodium salt), a new potent and selective leukotriene Cys-LT1 receptor antagonist synthesized by Makovec et al. (2001). CR3465 also has additional anti
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Immunology Compound Library Experiments on the rat model of
2020-08-06
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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It has been emphasized that CRF can
2020-08-06
It has been emphasized that CRF can activate Gs-protein-coupled CRF1 or CRF2 receptors triggering the cAMP-PKA cascade pathway (Chang et al., 1993, Chen et al., 1993, Lovenberg et al., 1995, Perrin et al., 1995, Vita et al., 1993). Moreover, both receptor subtypes have been found strongly expressed
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br Conclusions br Funding br Introduction
2020-08-06
Conclusions Funding Introduction One major challenge in the chemistry and physics of actinide and lanthanide (f-ion) complexes is the understanding of the role that f-electrons play in the magnetism in general and in the exchange coupling in particular. This is in marked A-1155463 to transi
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Although the authors findings increase our mechanistic under
2020-08-06
Although the authors’ findings increase our mechanistic understanding of how WT and mutant RAS isoforms interact to promote tumor progression and modulate responses to DNA-damaging chemotherapies, interesting questions remain. For example, the effect of the WT KRAS allele on mutant KRAS-driven tumor
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There are two types of DDRs DDR
2020-08-05
There are two types of DDRs, DDR1 and DDR2, which are type I transmembrane RTKs characterized by an N-terminal extracellular discoidin domain containing a collagen binding site [8]. DDR1 expression is somewhat restricted to epithelial cells, while DDR2 is often expressed in cells of mesenchymal orig
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In conclusion the major new
2020-08-05
In conclusion, the major new findings of the study were the observation that PTPN2 gene polymorphism affected the progression rate of already-established beta-cell autoimmunity among children with HLA class II conferred risk for T1D as well as the finding that IKZF4-ERBB3 SNPs locus altered the prog
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br Acknowledgments The authors acknowledge funding
2020-08-05
Acknowledgments The authors acknowledge funding from the National Key Research and Development Program of China (2016YFA0502900) and the National Science Foundation of China (31570188). Compartment Size Regulation Regulation of compartment size is one of the most fundamental issues in biology
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bioactive Here we report the development of a
2020-08-05
Here we report the development of a new fluorescence intensity (FLINT), signal increase, high-throughput assay that measures the oxidation of L-DHO to -orotate by DHODH. In this reaction, the reducing equivalents from the oxidation of the L-DHO are transferred to the FMN, yielding the reduced enzyme
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