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her2 inhibitor br No Evidence for Further ET Receptor
2020-11-12
No Evidence for Further ET-Receptor Subtypes Further receptor subclassifications have been proposed including suggestions that ETB could be subdivided into ETB1, present on endothelial cells, and ETB2 on smooth muscle cells, but there currently is no evidence that the receptors expressed by these
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PHA-665752 The different serotypes A G have
2020-11-12
The different serotypes (A-G) have unique receptors to which they bind to produce the toxic effect on the nerve cells. (Lance, 2004, Rosetto et al., 2014). Intracellularly, the endopeptidase activity of different serotypes of BoNT target selectively a unique group of proteins, the SNARE PHA-665752
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During the past few years several studies have addressed
2020-11-12
During the past few years, several studies have addressed macrophage phenotype in experimental models, such as angiotensin II-induced AAA. A first study investigated macrophage phenotype using flow cytometry to identify M1 and M2 macrophages and qPCR analysis for expression of NOS2 and Ym1/2. The au
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The discovery of proteases that are active in
2020-11-12
The discovery of proteases that are active in organic solvent media has greatly extended their ability in the synthesis of useful products. Microbial proteases which are able be catalyse in non-aqueous solvents present new expectation in enzyme applications. This kind of enzymes gives a major contri
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A role for the E E interface in governing
2020-11-12
A role for the E2–E3 interface in governing mono- versus polyubiquitination is not mutually exclusive with that of the E2 backside, which has previously been shown to mediate polyubiquitination through its ability to bind to Ub [21], [25], [33]. Brzovic and colleagues first demonstrated the importan
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Protein degradation via UPP involves two steps
2020-11-12
Protein degradation via UPP involves two steps. One step is the conjugation of multiple ubiquitin to a substrate. The other step is the degradation of tagged protein by the downstream 26S proteasome complex. Protein ubiquitination is the E1–E2–E3 enzymatic cascade (Hershko & Ciechanover, 1998). E1-a
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naphthalimide a well known DNA intercalator
2020-11-11
1,8-naphthalimide, a well-known DNA intercalator, has been extensively investigated in the development of antitumor agents [10]. Some of the naphthalimide derivatives, such as amonafide, elinafide and bisnafide (Fig. 1), have entered into phase II clinical trials stage [10]b), [11]. Among them, elin
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Otilonium Bromide A novel series of DHODH inhibitors was dev
2020-11-11
A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h
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zd 14 The positive correlation between ATG and DCTPP
2020-11-11
The positive correlation between ATG7 and DCTPP1 (TCGA data) suggested our hypothesis that DCTPP1 may affect the phenotype of prostate tumor, or maybe other types of tumors as well, through its role in autophagy. To test this hypothesis, we carried out western-blot experiments in which the ratios of
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During the course of our research on mGlu PAMs
2020-11-11
During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology,
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Similar to Bdnf acute administration of RG did not
2020-11-11
Similar to Bdnf4, acute administration of RG108 did not alter gene expression of Gria1 and Hdac2, despite their relevance for the task. Gria1 belongs to the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic thymidine phosphorylase inhibitor receptor (AMPAR) family that is known to be crucial for LTP
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Goel et al reported study of diacetoxy methylcoumarin DAMC a
2020-11-11
Goel et al. reported study of 7,8-diacetoxy-4-methylcoumarin (DAMC) 63 and its thiocoumarin derivative 7,8-diacetoxy-4-methylthiocoumarin (DAMTC) for their effect on human non-small cell lung cancer A549 cells. The study suggested that the 7,8-diacetoxy-4-methylcoumarin (DAMC) 63 downregulates Bcl-x
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br Cholesterol handling in the arterial wall
2020-11-11
Cholesterol handling in the arterial wall cells Foam cell formation in the arterial intima is a major hallmark of early-stage atherosclerotic lesions, which is attributed to uncontrolled uptake of modified lipoproteins, excess cholesterol esterification and impaired cholesterol release [44]. As a
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Increased leukocyte trafficking and infiltration of
2020-11-10
Increased leukocyte trafficking and infiltration of the vascular wall are thought to provide a key stimulus for SMC activation and subsequent neointima formation in response to vascular injury [19], [20]. The essential trigger regulating the accumulation of leukocytes in the vessel wall is the upre
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Circulating NK subsets also show
2020-11-10
Circulating NK subsets also show considerable differences in homing molecules. CD56bright amiodarone hcl express the chemokine receptor CCR7 and L-selectin, which drive their migration to secondary lymphoid organs (Fehniger et al., 2003). In contrast, CD56dim display a high density of CX3CR1 and CXC
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