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Several of the keloid like
2021-07-28

Several of the keloid-like lesions seen in these individuals were pigmented. It is of potential relevance that genetic variants in DDR1 [MIM: 600408] have been associated with vitiligo, and DDR1 activation is involved when formula for dilution are attached to collagen-IV fibers. Because DDR1 and DD
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In the phase I AURA trial patients with
2021-07-28

In the phase I AURA trial, patients with EGFR activating mutations and centrally confirmed tumor and/or plasma genotyping (BEAMing) T790M result were enrolled. Among 216 patients with both plasma and tissue genotyping results, the concordance rate was 82% for Protein A/G 19 deletions, 86% for L858R
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trk CCR is another chemokine receptor that is
2021-07-28

CCR7 is another chemokine receptor that is upregulated in CLL [3], [61], [71], [96] and is believed to play a role in enabling cell entry into lymph nodes [97]. Higher mRNA and protein expression of CCR7 has been observed in unmutated compared to mutated IGHV CLL [46] and increased expression has be
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The synthesis of compounds a and
2021-07-28

The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of mps1 kinase 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were
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br Introduction Biocatalysis can be used
2021-07-28

Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc
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Cysteinyl leukotrienes CysLTs are potent inflammatory
2021-07-28

Cysteinyl leukotrienes (CysLTs) are potent inflammatory mediators closely associated with cerebral ischemic injury. CysLTs induce inflammatory responses mediated by at least two different CysLT receptors (CysLT1R and CysLT2R) (Bäck et al., 2011, Singh et al., 2010). It has been reported that the Cys
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Introduction Quassinoids are natural products formed through
2021-07-28

Introduction Quassinoids are natural products formed through the oxidative degradation of triterpene derivatives with anti-inflammatory, antimicrobial, antineoplastic, and antiplasmodial effects (Chakraborty and Pal, 2013; Houël et al., 2013). They are characteristic ingredients of the family Simar
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Previously to detect CDKL activity we used a radioactive pho
2021-07-28

Previously, to detect CDKL5 activity, we used a radioactive phosphorylation assay with amphiphysin 1 protein as a substrate [,,]. However, it is necessary to establish a safe and rapid method for analyzing CDKL5 mutant activity. Here, we report a new method for investigating autophosphorylation acti
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Nuclear export mediated by CRM is initiated by
2021-07-28

Nuclear export mediated by CRM1 is initiated by an interaction between RanGTP and the HEAT9 loop of CRM1, triggering a conformational change in the NES binding site that permits NES–cargo protein binding (Dong et al., 2009, Fung and Chook, 2014). Our docking simulation results predicted that DP2392-
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Acknowledgments The authors thank Dr
2021-07-27

Acknowledgments The authors thank Dr. Vladimir Poltoratsky and Zhihui Xiao for their help with the in vitro FRET assay. Support for this research was provided by Saint John’s University. Introduction We predicted the existence of endothelium-derived contractile factors (EDCFs) in 1982 [1]. In 1
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IGF-1, human recombinant The inhibition of CYP activity by N
2021-07-27

The inhibition of CYP11β activity by NOR was 11- and 2.5-fold higher than those reported for the antifungal agents ketoconazole (IC50: 4.4μM) and clotrimozole (IC50: 1.0μM) (Fernandes and Porte, 2013). Furthermore, NOR was able to inhibit P450 aromatase activity in carp ovaries, although at a rather
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The use of recombinant ER and ER binding assays
2021-07-27

The use of recombinant ERα and ERβ binding assays offers a relatively inexpensive, rapid technique for screening compounds for potential direct ARCA EGFP mRNA receptor modulatory activity and understanding the mechanisms of existing herbal medicines. For background on the protein production system
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In addition to the ESIs identified that target both
2021-07-27

In addition to the ESIs identified that target both EPAC1 and EPAC2, ESI-05 and ESI-07 were identified as compounds that selectively antagonise EPAC2, displaying almost no inhibition of EPAC1 at concentrations up to 100μM [99]. Both compounds were effective inhibitors EPAC2 GEF activity towards Rap1
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br Materials and methods br Results and
2021-07-27

Materials and methods Results and discussion Concluding remarks Enzymatic production of bioactive 9-cis-11-trans-conjugated linoleic prostaglandin receptor is part of a detoxification mechanism against linoleic acid which is a toxic and stress factor for many lactic bacteria such as Lactob
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For most enolases fluoride acts
2021-07-27

For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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