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S Ao

Publications and source records attributed to S Ao.

9 recordsLinked to original sources

Identification and characterization of a novel human cDNA encoding a 21 kDa pRb-associated protein.

The retinoblastoma protein (pRb) functions as a critical master regulator in cell cycle regulation, which is an important cell-regulatory process, through its interaction with various cellular proteins. Using the C-terminus of human pRb and the yeast two-hybrid system, a novel protein named RBP21 that contains 187 amino acid residues with a calculated molecular weight of 21 kDa was identified as a pRb-binding protein. Sequence analysis indicates that RBP21 shares homology with other retinoblastoma-binding proteins in the pRb-binding motif LxCxE at the C-terminal region. In vitro specific interaction between pRb and RBP21 was confirmed using in vitro translation products. When overexpressed in COS-7 cells, RBP21 could co-immunoprecipitate with pRb. This interaction requires the LxCxE motif of RBP21 and the entire pocket region of pRb. Each point mutation of the conserved amino acid residues in pRb-binding motif of RBP21 abolished its specific interaction with pRb. RH mapping result showed that this novel gene was mapped to chromosome region 15q21.1-21.3. Northern blot analysis suggested that RBP21 was widely expressed in various human tissues and cancer cell lines. When expressed in HeLa cells as a green fluorescent protein fusion, RBP21 was distributed throughout the cell.

Adenovirus E1A Proteins↗

Regulation of the yeast transcriptional factor PHO2 activity by phosphorylation.

The induction of yeast Saccharomyces cerevisiae gene PHO5 expression is mediated by transcriptional factors PHO2 and PHO4. PHO4 protein has been reported to be phosphorylated and inactivated by a cyclin-CDK (cyclin-dependent kinase) complex, PHO80-PHO85. We report here that PHO2 can also be phosphorylated. A Ser-230 to Ala mutation in the consensus sequence (SPIK) recognized by cdc2/CDC28-related kinase in PHO2 protein led to complete loss of its ability to activate the transcription of PHO5 gene. Further investigation showed that the Pro-231 to Ser mutation inactivated PHO2 protein as well, whereas the Ser-230 to Asp mutation did not affect PHO2 activity. Since the PHO2 Asp-230 mutant mimics Ser-230-phosphorylated PHO2, we postulate that only phosphorylated PHO2 protein could activate the transcription of PHO5 gene. Two hybrid assays showed that yeast CDC28 could interact with PHO2. CDC28 immunoprecipitate derived from the YPH499 strain grown under low phosphate conditions phosphorylated GST-PHO2 in vitro. A phosphate switch regulates the transcriptional activation activity of PHO2, and mutations of the (SPIK) site affect the transcriptional activation activity of PHO2 and the interaction between PHO2 and PHO4. BIAcore(R) analysis indicated that the negative charge in residue 230 of PHO2 was sufficient to help PHO2 interact with PHO4 in vitro.

Acid Phosphatase↗

RBP95, a novel leucine zipper protein, binds to the retinoblastoma protein.

We recently identified a novel cDNA encoding a retinoblastoma protein (pRb)-associated protein. It was named RBP95, which was composed of 838 amino acid residues with a calculated molecular size of 94,789 Da. Northern blot analysis showed a single mRNA of about 4. 5 kb ubiquitously expressed in human tissues. RH mapping results showed that RBP95 is mapped to chromosome region 16p11.2-11.1. Sequence analysis indicated that RBP95 contains a conserved pRb-binding motif LXCXE. Interaction between pRb and RBP95 was confirmed in vivo and in vitro. This interaction requires the LXCXE motif of RBP95 and the entire pocket region of pRb. Each point-mutant of the conserved amino acid residues in pRb-binding motif of RBP95 would destroy its interaction with pRb. RBP95 also contains a basic region leucine zipper and could homodimerize through its leucine zipper region. RBP95 was located in the nucleus with a special pattern when expressed as a GFP fusion in HeLa cells. All these findings suggested that RBP95, a new member of pRb-associated protein, may function as a regulation factor in the process of RNA polymerase II-mediated transcription and/or transcriptional processing.

Amino Acid Sequence↗

Human SOX11, an upregulated gene during the neural differentiation, has a long 3' untranslated region.

To obtain essential genes for neuronal development, we have performed a molecular indexing method using a human teratocarcinoma cell line, NTera-2. We isolated a cDNA fragment, designated B18, as an upregulated gene during the neural differentiation. From the complete cDNA sequence of B18 it was revealed that this cDNA was the human SOX11 gene. While a previous report has determined only a approximately 2 kb of the SOX11 cDNA including the entire open reading frame, our full length cDNA was 8743 bp possessing a long 3' untranslated region. Human SOX11 cDNA was mapped to chromosome region 2p25.3 between markers AFMA070WC9 and WI-1412 by radiation hybrid mapping.

3' Untranslated Regions↗

[Studies on the cloning, expression and function of the yeast PHO 80 gene].

Through in situ hybridization, a 4.2 kb Pst I-BamH I fragment was obtained from S. cerevisiae gene library. The cloned fragment contained 1100 bp upstream sequence and 879 bp coding sequence of the PHO80 gene. Coding region of PHO80 gene was substituted with URA3 gene and used as donor to transform YPH499 to URA3. A pho80 mutant resulted from deletion of the chromosomal counterpart in PHO80 was obtained. In vivo functional study of the PHO80 gene indicated that PHO80 was a negative regulator in the Pi-repressible acid phosphatase system including the structural genes PHO5 and PHO11 and the regulatory gene PHO81, whereas the expression of PHO4 or PHO85 was independent of PHO80. The coding region of PHO80 was fused in frame with LacZ and beta-galactosidase activities in various cells was determined. The results Showed that the PHO80 gene was expressed at a low level and suppressed by itself and PHO85.

Acid Phosphatase↗

Preparation and a structure-function analysis of human ciliary neurotrophic factor.

Ciliary neurotrophic factor (CNTF) is a trophic protein that promotes survival and/or differentiation of a variety of neuronal cell types including sensory, sympathetic, and motor neurons. CNTF, leukemia inhibitory factor (LIF), interleukin-6 (IL-6) and oncostatin M (OSM) share a predicted common helical framework and partially identical receptor components. In this study, we present the preparation and structure--functional analysis of recombinant human CNTF. The human CNTF gene was expressed under the control of the PL promoter in Escherichia coli, and the mutants were constructed by insertion, deletion and site-directed mutagenesis. The recombinant proteins were purified from bacteria via DEAE A-50 and Sephacryl S-200 chromatography, and their survival promoting activities were determined using cultures of embryonic chick dorsal root ganglion (DRG) neurons. Insertion at position 23 with APGL, or at position 79 with PRGA, or substitution of 162L163Q for PIDG resulted in proteins with no neurotrophic activity. However, insertion at position 186 with PRGI did not alter human CNTF activity. Deletion of the carboxy-terminal amino acid 186-200 did not reduce the biological activity, but elimination of the amino acid 162-186 abolished the activity. The mutant substituting of 17 Cys for Ser was found to display a biological activity equivalent to that of the wild type. Our data provided experimental confirmation for the structural prediction of CNTF.

Amino Acid Sequence↗

Pharmacological profile of FR139317, a novel, potent endothelin ETA receptor antagonist.

The effects of FR139317 on the cardiovascular system were investigated in cultured cells, isolated organs and whole animals. FR139317 inhibited the specific binding of [125]endothelin(ET)-1 to porcine aortic microsomes in a concentration-dependent, monophasic fashion with an IC50 of 0.53 nM. In contrast, FR139317 showed low affinity for [125I]ET-1 specific binding sites in porcine kidney (IC50, 4.7 microM). In isolated rabbit aorta, FR139317 shifted the ET-1-induced concentration-contractile response curve to the right with a pA2 value of 7.2 and lacked agonist activity. A single (i.v.) bolus dose of FR139317 completely inhibited the pressor response to ET-1 in vivo, but had no effect on the initial depressor response in conscious normotensive rats. These data indicate that FR139317 is a potent, highly specific ETA receptor antagonist. In addition, FR139317 also inhibited ET-1 induced [3H]thymidine incorporation in cultured vascular smooth muscle cells from rat aorta (IC50, 4.1 nM), suggesting that ET-1-induced mitogenesis is mediated only by the ETA receptor. FR139317 could become a useful tool for investigating the physiological and pharmacological actions of ET.

Animals↗

Characterization of a novel aldose reductase inhibitor, FR74366, and its effects on diabetic cataract and neuropathy in the rat.

FR74366 (FK366) ([3-(4-bromo-2-fluorobenzyl)-7-chloro-2,4-dioxo-1,2,3,4- tetrahydroquinazolin-1-yl] acetic acid) is a chemically novel aldose reductase (AR) inhibitor. It exhibited a highly potent, reversible, and mixed type inhibition of partially purified AR from the rat sciatic nerve (IC50 = 3.6 nmol/L) and rat lens (IC50 = 4.4 nmol/L). FR74366 inhibited sorbitol accumulation in the isolated human erythrocyte (IC50 = 1.6 mumol/L), rat lens (IC50 = 39 mumol/L), and rat sciatic nerve (IC50 = 17 mumol/L) incubated with high glucose concentrations. The oral administration of FR74366 to streptozotocin (STZ)-induced diabetic rats for 2 weeks decreased sorbitol levels (ED50 = 3.7 mg/kg for sciatic nerve, 23 mg/kg for lens, 52 mg/kg for retina, and 62 mg/kg for renal cortex). Administration of FR74366 to diabetic rats for 17 weeks delayed cataract formation and admixture of 0.028% FR74366 in the diet completely inhibited the cataract formation. Moreover, the recovery of reduced motor nerve conduction velocity by FR74366 in diabetic rats was demonstrated in prevention and reversal experiments. This recovery effect correlated well with reduction of accumulated sorbitol and fructose levels and normalization of decreased myoinositol levels. The duration and tissue specificity of inhibitory effects of FR74366 on sorbitol accumulation also correlated well with the levels of FR74366 in various tissues of diabetic rats. These data indicate that both decreases in tissue sorbitol levels and improvement of functional defects reflect FR74366 levels in tissue rather than plasma in diabetic rats. These results, taken together, suggest that FR74366, which is currently undergoing clinical trials in Japan and the United States, will be a useful therapeutic agent for diabetic complications.

Aldehyde Reductase↗

Effect of instillation of aldose reductase inhibitor FR74366 on diabetic cataract.

The authors investigate the effect of aldose reductase inhibitor FR74366 on diabetic cataract. Streptozocin (STZ)-induced diabetic rats were treated with eye drops of FR74366 (0.03%, 0.1%, and 0.3%) for 16 weeks. Lenses were examined using a slit lamp, and the score of lens opacity was determined on a scale of from 0 (normal lens) to 4 (matured nuclear cataract). Diabetic placebo control rats developed lens opacity linearly, beginning at 3 weeks and reaching a maximum at 8 weeks after STZ injection. Instillation of FR74366 to diabetic rats delayed the cataract formation and inhibited lens sorbitol accumulation in a dose-dependent manner. At 16 weeks after STZ injection, the score of lens opacity was more than 3 (diffuse central opacities) in diabetic placebo control rats, whereas it was less than 2 (peripheral vesicles and cortical opacities) and the lenses remained clear in animals treated with 0.3% of FR74366. Measurement of tissue drug concentrations indicated that FR74366 penetrated into the lens, where its levels were increased in a dose- and time-dependent manner. These three parameters (score of lens opacity and sorbitol and FR74366 levels) were well correlated with each other. Instillation of FR74366 also reduced the sorbitol levels in the retina. However, the sorbitol levels in the sciatic nerve and renal cortex were not changed by instillation of FR74366. Instillation or oral administration of FR74366 has not shown serious side effects in animal toxicity studies. These results suggested that instillation of FR74366 may be a useful therapeutic agent against diabetic cataract and retinopathy.

Administration, Topical↗