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In this review we focus on
2021-09-24

In this review, we focus on the structure and function of the KDM4A protein, its role in cancer development, and the importance of this enzyme as a therapeutic target. For further review of the KDM4 family, see Shi et al., Whetstine et al., and Berry et al. , , . KDM4A protein structure and enzymol
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The manuscript provides mechanistic insights into the suppre
2021-09-23

The manuscript provides mechanistic insights into the suppression of EGFR, BCRP, PKM2, and other cancer biomarkers in response to pharmacological inhibition of GPR55 with MNF and CID (Fig. 7). Firstly, inactivation of ERK has been previously demonstrated following treatment of PANC-1 Vinpocetine sal
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Based on the role of NMDA receptors
2021-09-23

Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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In our study we evaluated adenovirus type Ad as a
2021-09-23

In our study we evaluated adenovirus type 5 (Ad5) as a vehicle for delivering Cre recombinase in conditional transgenic mouse based on the Cre-loxP system, in order to achieve GlyT1 gene modulation in a specific thalamic region in the adult animal. GlyT1 is a sodium- and chloride-coupled glycine tra
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Next we designed substituents of
2021-09-23

Next, we designed substituents of the 6-position. Edge-to-face aromatic interaction between aromatic ring of ligand and Phe162B needed to be retained because the interaction seems to be important for tight binding. 3′-Position of the 6-phenyl group of directs to a hydrophilic space where W1 exists.
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7915 During the structural transition the FD the PHD and
2021-09-23

During the structural transition, the FD, the PHD and the TrD retain their tertiary structure. Nevertheless, they undergo large rearrangements in their relative orientation due to secondary changes in hinge segments (R1 to R5) which refold during the low-pH induced conformational change. Particularl
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br Material and methods br Results br Discussion
2021-09-23

Material and methods Results Discussion Neurosteroids capable of blocking the NMDAR channel attract a lot of attention as possible therapeutic agents for the treatment of neurodegenerative diseases. A large number of new mitotic inhibitor with different structures have been synthesized in
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ATP is essential for maintaining the ionic
2021-09-23

ATP is essential for maintaining the ionic balance of the lens (Michael and Bron, 2011). Without sufficient ATP there is an ionic imbalance due to Na+K+ATPase dysfunction. Previous studies have shown that rabbit lenses incubated ex vivo without glucose rapidly lost ATP in their lens epithelium and f
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br Introduction The alternative splicing of pre mRNA is esse
2021-09-23

Introduction The alternative splicing of pre-mRNA is essential for generating multiple matured mRNAs from a single gene by selectively removing introns. Neural 13148 mg show many examples of regulated alternative splicing events, which produce structural changes in proteins important for the deve
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In the present study we
2021-09-23

In the present study, we tested α-glucosidase and tyrosinase inhibitory effects of the methanol extract from lower stems and AZD1152-HQPA of Q. coccifera (1) as well as the isolated compounds [lyoniresinol-9-O-β-xylopyranoside (2) and lyoniresinol-9-O-β-glucopyranoside (3), cocciferoside (4), (-)-8
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We report on four affected children
2021-09-23

We report on four affected children from two unrelated consanguineous actin inhibitor with moderate to severe ID associated with epilepsy and variable neuropsychiatric features. Using whole-exome sequencing, we identified homozygous missense variants in SLC45A1 (OMIM: 605763), which codes for a neu
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The eradication of agonist activity in compound
2021-09-23

The eradication of agonist activity in compound was also confirmed in the ex vivo growth hormone (GH) release experiment conducted in isolated primary rat pituitary Mdivi 1 as shown in . Compound did not produce any noticeable GH secretion at up to 10μM concentration. It could also antagonize the st
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Ghrelin contains an n octanoylation
2021-09-23

Ghrelin contains an n-octanoylation at its Ser3 residue (Kojima et al., 1999). While des-acyl ghrelin is found in high concentrations in the blood, only the lipidated form is active at GHSR (Bednarek et al., 2000). We previously showed that ghrelin interacts with the membrane via its lipid modificat
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br Financial support This work was
2021-09-22

Financial support This work was supported by Fondation pour la Recherche Médicale (Equipe labellisée, DEQ20150331724), Inserm, University of Lille, and Agence Nationale pour la Recherche (ANR-10-LBEX-46 and ANR-10-INBS-08; ProFI project, “Infrastructures Nationales en Biologie et Santé”; “Investi
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In terms of cytotoxicity studies
2021-09-22

In terms of cytotoxicity studies under two-dimensional cell culture conditions, only two of the above-mentioned publications with liposomal formulations of tyrosine kinase inhibitors reported viability data as compared to respective free drugs. On the one hand, liposomal gefitinib exerted strongly r
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