Spinal cord injury is a severe clinical problem, and research searching activity molecular that can promote spinal cord injury repairing is very prevalent. Mst3b can promote repair of damaged peripheral nerves and the optic nerve, but has been rarely reported in spinal cord injury research. Through detecting its expression in different periods of injured spinal cord, we found that the expression of Mst3b was significantly upregulated in injured spinal cord neurons.
View Article and Find Full Text PDFACS Med Chem Lett
January 2014
A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (RORγt) inverse agonists was discovered through agonist/inverse agonist conversion. The level of RORγt inhibition can be enhanced by modulating the conformational disruption of H12 in RORγt LBD. Linker exploration and rational design led to the discovery of more potent indole-based RORγt inverse agonists.
View Article and Find Full Text PDFBackground: A fundamental issue in systems biology is how to design simplified mathematical models for describing the dynamics of complex biochemical reaction systems. Among them, a key question is how to use simplified reactions to describe the chemical events of multi-step reactions that are ubiquitous in biochemistry and biophysics. To address this issue, a widely used approach in literature is to use one-step reaction to represent the multi-step chemical events.
View Article and Find Full Text PDFBackground: ClC-3 channel/antiporter plays a critical role in a variety of cellular activities. ClC-3 has been detected in the ileum and colon.
Objective: To determine the functions of ClC-3 in the gastrointestinal tract.
Novel series of N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides were discovered as potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitors. SAR studies of the RORγt HTS hit 6a led to identification of thiazole ketone amide 8h and thiophene ketone amide 9g with high binding affinity and inhibitory activity of Th17 cell differentiation. Compound 8h showed in vivo efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models via oral administration.
View Article and Find Full Text PDFGlioma is among the ten most common causes of cancer-related death and has no effective treatment for it, so we are trying to find a new target for anticancer treatment. This study investigates the different expression of SRPK1 as a novel protein in glioma, which can influence tumor cells biological characteristics in normoxic and hypoxic environment. The expression levels of SRPK1 protein in glioma cell lines transfected with siSRPK1 or not were examined using immunofluorescence, RT-PCR and Western blot analysis, respectively.
View Article and Find Full Text PDFA stimuli-responsive supramolecular polymer network was constructed by the orthogonal assembly of metal-ligand interactions and host-guest interactions.
View Article and Find Full Text PDFAlpha6beta2 nicotinic acetylcholine receptors (nAChRs) are potential therapeutic targets for the treatment of several neuropsychiatric diseases, including addiction and Parkinson's disease. Alpha-conotoxin (α-CTx) TxIB is a uniquely selective ligand, which blocks α6/α3β2β3 nAChRs only, but does not block the other subtypes. Therefore, α-CTx TxIB is a valuable therapeutic candidate peptide.
View Article and Find Full Text PDFIntroduction: The Xeroderma pigmentosum group D (XPD, also referred to as excision repair cross complementing gene 2, ERCC2) is one of key genes involved in nucleotide excision repair and two potentially functional polymorphisms of XPD (Asp312Asn and Lys751Gln) have been widely investigated in various cancers including prostate cancer. However, the results were conflicting rather than conclusive.
Aims: Thus, we conducted a meta-analysis to evaluate the associations between these two polymorphisms of XPD and the risk of prostate cancer.
Objective: To evaluate the efficacy and safety of antenatal ambroxol as a preventive therapeutic of respiratory distress syndrome (RDS) in preterm infants.
Methods: Randomized controlled trials of antenatal ambroxol treatment for RDS in preterm infants published up to March 2012 were downloaded from the Cochrane Library, PubMed, EMBASE, Science Citation Index, and Google Scholar databases. Data were evaluated for homogeneity and analyzed by the Cochrane Collaboration's RevMan software.
Recent evidence suggested that ClC-3 channel/antiporter is involved in regulation of nuclear factor (NF)-κB activation. However, the mechanism explaining how ClC-3 modulates NF-κB signaling is not well understood. We hypothesized that ClC-3-dependent alteration of intracellular chloride concentration ([Cl(-)](i)) underlies the effect of ClC-3 on NF-κB activity in endothelial cells.
View Article and Find Full Text PDFEvid Based Complement Alternat Med
November 2011
The fucoidanase from Fusarium sp. (LD8) was obtained by solid-state fermentation. The fermented solid medium was extracted by citric acid buffer, and the extracts were precipitated by acetone and purified by Sephadex G-100 successively.
View Article and Find Full Text PDFDopamine (DA) profoundly modulates excitatory synaptic transmission and synaptic plasticity in the brain. In the present study the effects of SKF83959, the selective agonist of phosphatidylinositol (PI)-linked D(1) -like receptor, on the excitatory synaptic transmission were investigated in rat hippocampus. SKF83959 (10-100 μM) reversibly suppressed the field excitatory postsynaptic potential (fEPSP) elicited by stimulating the Schaffer's collateral-commissural fibers in CA1 area of hippocampal slices.
View Article and Find Full Text PDFA series of new aporphine analogues (aporlogues) were prepared from appropriate aporphine precursors and arylpiperazines using the Click reaction protocol. These compounds displayed good to high affinity at the D(3) receptor, low or no affinity at the D(1) and D(2) receptors. Compounds 7f and 11c stood out as the most potent at the D(3) receptor among our newly synthesized aporlogues with K(i) values of 2.
View Article and Find Full Text PDFZhejiang Da Xue Xue Bao Yi Xue Ban
July 2010
Objective: To construct, express and identify the recombinant plasmid pcDNA3.1(+)/sflk1-IFN-gamma encoding bifunctional protein sflk1-IFN-gamma (soluble fetal liver kinase 1 and interferon-gamma).
Methods: sflk1 and IFN-gamma gene fragments were cloned by RT-PCR, and then inserted into pcDNA3.
A series of new aporphine analogues were synthesized and pharmacologically evaluated. 11-Allyloxy-(17), 11-propargyloxy-(20), and dihydrofuro-(19) aporphines displayed the highest affinity at the 5-HT(1A) receptor with K(i) values of 12.0, 14.
View Article and Find Full Text PDFNan Fang Yi Ke Da Xue Xue Bao
October 2009
Objective: To investigate the effects of combined use of low-dose hydroxyurea (HU) and sodium butyrate (NaB) on the expression of 7 globin genes (zeta, alpha, epsilon, Ggamma, Agamma, delta, and beta) in human erythroid progenitor cells.
Methods: Human erythroid progenitor cells were cultured using a two-step liquid culture system and treated with HU and NaB either alone or in combination. The inhibitory effects of the agents on the cell growth were monitored with trypan blue exclusion assay, and the changes in the mRNA of the 7 globin genes were detected using RT-PCR.
The beta-agarase gene agaA, cloned from a marine bacterium, Pseudoalteromonas sp. CY24, consists of 1,359 nucleotides encoding 453 amino acids in a sequence corresponding to a catalytic domain of glycosyl hydrolase family 16 (GH16) and a carbohydrate-binding module type 13 (CBM13). The recombinant enzyme is an endo-type agarase that hydrolyzes beta-1,4-linkages of agarose, yielding neoagarotetraose and neoagarohexaose as the predominant products.
View Article and Find Full Text PDFFucoidanase was isolated and purified from marine fungus LD8 by solid state fermentation, extraction with citric acid buffer, acetone precipitatation and column chromatography on Sephadex G-100. A single band on PAGE shows that pretty pure fucoidanase has been obtained. FT-IR spectra and its derivation, self-deconvolution and curve-fitting methods were used to analyze the secondary structure of the fucoidanase.
View Article and Find Full Text PDFObjective: To investigate the anti-metastatic effect of vascular endothelial growth factor receptor 2 extracellular domain gene-modified dendritic cell (DC-sVEGFR-2) vaccination.
Methods: Dendritic cells (DC) were electroporated with pcDNA3. 1/sVEGFR-2 plasmid DNA.
The neuropeptide vasoactive intestinal peptide (VIP), released within lymphoid organs from nerve terminals and/or immune cells, plays a significant anti-inflammatory role. It was reported that VIP can induce regulatory dendritic cells (DCs) and promote Th2-type responses. However, the regulatory effect of VIP on the migration and expression of chemokine receptors by DC is mostly unknown.
View Article and Find Full Text PDFDi Yi Jun Yi Da Xue Xue Bao
August 2005
Objective: To construct recombinant eukaryotic expression plasmid pcDNA3.1(+)-mtDNA for investigation of mutations in the D-loop region of mitochondrial DNA in human colorectal carcinoma.
Methods: The D-loop region of 3 colorectal carcinoma cell lines (SW480, LoVo, and HT29) were amplified by PCR and sequenced.