Asymmetric synthesis of 4'-alpha-alkylcarbovir derivatives

Asymmetric synthesis of 4'-alpha-alkylcarbovir derivatives 3 were achieved based on Sakai's asymmetric alkylation of beta-keto esters. The key carbocyclic intermediate 12 was synthesized from 6 via an eleven-step sequence. Coupling of 12 with 2-amino-6-chloropurine followed by desilylation and subsequent hydrolysis gave the target compounds 3 in moderate yields.     

Efficient third-harmonic generation of a picosecond laser pulsewith time delay

A new configuration based on the polarization-mismatching scheme with time delay for efficient frequency tripling conversion is proposed in this paper. The calculated results showed that the requirement for the efficient frequency tripling conversion of a 1-ps laser pulse is not only the optimization of peak intensity of the second-harmonic pulse, but also the optimization of the pulse duration ratio and temporal difference between the o-polarization second-harmonic pulse and the e-polarization first-harmonic pulse due to group-velocity mismatch among the interacting pulses. With the proposed scheme the group velocity mismatch can be compensated. Overall energy conversion efficiency increases from 55% to 75% under the optimized conditions at the intensity of 6 GW/cm². The temporal shape of the third-harmonic pulse with 1 ps pulse duration has no subpulses. The optimization of the efficient frequency tripling conversion for intensities of over 75 GW/cm² is also described. The results showed that the maximum tripling energy conversion efficiency is close to 80% with the optimized doubler and tripler     

Superconductivity in the tetragonal phase of La1.9Bi0.1CuO4+δ annealed under high oxygen pressure

We have investigated the relation between the crystal structure and superconductivity in La_1.9Bi_0.1CuO_4+δ , in which the phase separation observed in La₂CuO_4+δ is suppressed. A phase diagram in theT?δ plane is given for La_1.9Bi_0.1CuO_4+δ with excess oxygen. For very smallδ values, the crystal structure is orthorhombic, and an orthorhombic-tetragonal phase transition occurs markedly atδ ～ 0.03 in the measured temperature range between 13 and 293 K. Superconductivity is observed in the range of 0.04<δ<0.11. This is clear evidence thathigh-T _c superconductivity also appears in the tetragonal phase.     

The significance of urinary N-acetyl-beta-D-glucosaminidase for predicting early stage diabetic nephropathy

We studied urinary N-acetyl-beta-D-glucosaminidase (NAG) in the early stage of diabetic nephropathy in 27 non-insulin-dependent diabetes mellitus (NIDDM) patients with a microalbumin level below 20 mg on 24-hour urine sample. Microalbumin and NAG excretion were measured in 24-hour urine samples collected on three separate occasions within seven days of admission. Creatinine clearance was determined simultaneously. There was a significant negative correlation between the creatinine clearance and 24-hour urinary NAG (r = -0.38, p < 0.05). Elevation of urinary NAG may indicate decreased renal function during early stage NIDDM nephropathy.     

Insights into multistep phosphorelay from the crystal structure of the C-terminal HPt domain of ArcB

The histidine-containing phosphotransfer (HPt) domain is a novel protein module with an active histidine residue that mediates phosphotransfer reactions in the two-component signaling systems. A multistep phosphorelay involving the HPt domain has been suggested for these signaling pathways. The crystal structure of the HPt domain of the anaerobic sensor kinase ArcB has been determined at 2.06 A resolution. The domain consists of six alpha helices containing a four-helix bundle-folding. The pattern of sequence similarity of the HPt domains of ArcB and components in other signaling systems can be interpreted in light of the three-dimensional structure and supports the conclusion that the HPt domains have a common structural motif both in prokaryotes and eukaryotes.     

Preparation of SiC particles coated with alumina hydrate: Effect of reaction condition on particle coalescence

Alumina-hydrate-coated SiC particles were prepared via a homogeneous precipitation method using urea, and the conditions for uniform coating and less coalescence of the particles were investigated. Coalescence of coated particles could be said to occur by collision and agglomeration followed by deposition of alumina hydrate on the agglomerated particles. Coalescence of coated particles was suppressed by use of low reaction temperature, low concentration of aluminium sulfate, high concentration of urea, intensive stirring, and a flow reactor.     

Immunohistochemical demonstration of 3,2''-dimethyl-4-aminobiphenyl DNA adduct formation in various organs of Syrian golden hamsters

We attempted to purify endogenous growth factors of chick embryonal retinal pigment epithelial cells from bovine neural retina. Ammonium sulfate precipitation, gel filtration, and anion exchange column chromatography were used. Though only partially purification, bovine retinal extract had two effects, growth and transformation, on chick embryonal pigment epithelial cells. We think that these purified factors may be novel from the estimation of their molecular weight by gel filtration.     

Characterization of a cartilage-derived 66-kDa protein (RGD-CAP/beta ig-h3) that binds to collagen

Malignant human gliomas are the most common forms of primary tumors in the central nerve system. Due to their location and invasive nature, treatment so far has been mainly palliative. Thus, understanding the molecular detail of tumor transformation and progression is crucial for developing effective therapeutic strategy for this fetal tumor. Among the genetic alternations found in these tumors, p53 inactivation and PDGF/PDGFR activation represent the early events, and the loss of chromosome 10 and gene amplification and rearrangement of EGFR represent the late events. Studies with both glioma cell lines and primary tumor tissues have strongly suggested that TGF-alpha and EGFR function as an important autocrine loop in supporting proliferation of human glioma, especially in high grade glioma, since elevated TGF-alpha expression is also found in these high grade tumors. Furthermore, down regulation of the expression of TGF-alpha by antisense constructs has been shown to inhibit several types of human tumor cell growth including glioma. Other means of therapeutic approaches using this autocrine loop as a target also include the use of monoclonal antibodies and their cytotoxic conjugated. Considerable understanding of the EGFR-mediated signal transduction pathways has become available recently, which including GRB2/mSOS1 mediated MAP kinase activation; JAK/STATs pathway; PLC-gamma pathway. However, much work still needs to be done before a specific component of these pathways can be applied for effective control of tumor growth in the clinic.