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As described above we designed and synthesized a new di
2019-12-30
As described above, we designed and synthesized a new 1,4-di-substituted isoquinoline lead compound, and was identified as a ligand with moderate potency for the CRTH2 receptor. We initially we examined the effects of the steric factor of R group on the CRTH2 binding potency (). When the methyl gro
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thyrotropin releasing hormone Common to all models for nucle
2019-12-30
Common to all models for nuclear transport is the binding of importins/exportins to FG repeats found in about a third of the ∼30 nucleoporins, the so-called FG-Nups (Iovine et al., 1995, Rexach and Blobel, 1995); for review, see Grossman et al. (2012), Stewart (2007), and Terry and Wente (2009). FG-
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The following is the supplementary
2019-12-30
The following is the supplementary data related to this article. Funding This work was supported by departmental funding to Prof. Mühl. Funding derived from the State of Hessia to the Institute of General Pharmacology and Toxicology at the pharmazentrum frankfurt (Head: Prof. Josef Pfeilschifter
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Does hydroxylation of proline have a specific role in the
2019-12-30
Does hydroxylation of proline have a specific role in the structure and function of the conotoxins? Several studies in the literature provide insights into the role of proline hydroxylation in the Conus peptides. The consequences of proline hydroxylation on oxidative folding and biological activity
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This structure guided the variation of the
2019-12-30
This structure guided the variation of the compounds aiming either at enhanced interaction with CK1 or to exclude interaction with CK1 (R=Me, 15). We chose the 5-cloro substituted oxoindole as backbone as it is supposed to show enhanced metabolic stability, which is commonly used in medicinal chemis
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CK enzymes belong to a conserved family
2019-12-30
CK1 enzymes belong to a conserved family of serine/threonine protein kinases that plays an important and diverse role in vesicular trafficking, DNA repair, Piericidin A progression and cytokinesis in organisms from yeast to humans [15]. In multicellular organisms CK1 enzymes also regulate developmen
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br PFL AE as a model for the
2019-12-30
PFL-AE as a model for the GRE–AEs Most of the GRE–AEs have proven difficult to study due to instability, difficulty in overexpression, lability of the iron-sulfur cluster, or other reasons. PFL-AE is the exception, and after the initial discovery of the iron–sulfur cluster in this enzyme [60], co
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Aliskiren Hemifumarate synthesis OxLDL down regulates eNOS a
2019-12-30
OxLDL down-regulates eNOS and up-regulates iNOS, thereby augmenting the formation of NO and protein S-nitrosylation in human endothelial Aliskiren Hemifumarate synthesis [26]. Importantly, iNOS-mediated S-nitrosylation plays an increasingly significant role in cardiovascular diseases [34]. For exam
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Nrf and HO are key factors
2019-12-30
Nrf2 and HO-1 are key factors in the regulation of oxidative stress in the body. Research has shown that KLF2 can activate Nrf2 and HO-1 [14]. To investigate the mechanisms by which KLF2 regulates eNOS uncoupling and oxidative stress, Nrf2 was inhibited or HO-1 was knocked down in KLF2 overexpressin
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Agarose GPG/ME sale br Transparency document br Introduction
2019-12-30
Transparency document Introduction Cigarette smoke is modifiable factors to alter the neurovascular functions. Now a day, cigarette smoking in public place is offense due to toxic exposure cause the neurological and respiratory system damage to non-smoker population [1]. A literature survey ex
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Our knowledge of DDR induced
2019-12-30
Our knowledge of DDR-induced signaling pathways is still fragmentary. In particular, we do not know which signaling effectors interact with the phosphorylated receptors and how different effectors are linked to the control of specific cellular functions. The DDRs are at the interface between RTKs an
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br Results br Discussion Taking advantage of the highly
2019-12-30
Results Discussion Taking advantage of the highly specific protein–protein interactions among cognate CCT007093 mg that mediate SUMO conjugation to substrates, we have developed a novel strategy for achieving inhibition of SUMO conjugation in vivo based on disruption of SUMO E1–E2 interactions
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br Chemistry A total of
2019-12-30
Chemistry A total of 35 new ThDP analogs in the series of 7, 12, 15, and 19 were designed and synthesized (Scheme 1). The synthetic route is simple and convenient. In this synthetic route, 4-amino-2-methylpyrimidine-5-carbaldehyde 3 is a key intermediate for the synthesis of title compounds 7, 1
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br Materials and methods br
2019-12-30
Materials and methods Results Discussion Plg plays important roles in various physiological processes, such as fibrinolysis, proteolysis, cell migration, differentiation, tissue remodeling, and inflammation [6], [7], [8]. We herein found that Plg deficiency enhanced insulin secretion, and w
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AMPHs facilitate dopamine release which further triggers dop
2019-12-30
AMPHs facilitate dopamine release, which further triggers dopamine depletion [72]. Indeed, we observed that repeated treatment of MPA significantly inhibited TH-, DAT-, and VMAT-2 levels. Since DAT and VMAT-2 are important for dopaminergic terminal markers [10], their decreases suggest that MPA-indu
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