Interaction of beta-lactam antibiotics with histidine residue of rat H+/peptide cotransporters, PEPT1 and PEPT2

Peptide transporters mediate the H+-coupled uphill transport of oligopeptides and peptide-like drugs such as beta-lactam antibiotics in the intestinal and renal brush-border membranes. Two H+/peptide cotransporters, PEPT1 and PEPT2, have been cloned and functionally characterized. In this study, we examined the interaction of the dipeptides and beta-lactam antibiotics with the histidine residue of rat PEPT1 and PEPT2 transfected into the renal epithelial cell line LLC-PK1. Diethylpyrocarbonate (DEPC), which is a histidine residue modifier, abolished the glycylsarcosine uptake by both transfectants. The DEPC-induced inhibition of glycylsarcosine uptake via PEPT1 or PEPT2 was attenuated by an excess of dipeptide or aminocephalosporin. In contrast, anionic cephalosporins without an alpha-amino group and bestatin, which is an antineoplastic drug with a beta-amino group, did not attenuate the DEPC-induced inactivation of PEPT1 and PEPT2. The DEPC inactivation of PEPT1 was almost prevented by various charged dipeptides, which suggests that the inability of the drugs without an alpha-amino group to prevent the DEPC inactivation was not due to their ionic charge. These findings suggest that the alpha-amino group of beta-lactam antibiotics interacts with the histidine residue of PEPT1 and PEPT2 and may be involved in the mechanism of substrate recognition by the peptide transporters.     

An analysis of the stress intensity factor of a crack perpendicular to the welding bead

Stress intensity factor of a crack perpendicular to the welding bead in a wide plate is analyzed as a plane problem of elasticity. The function which .simulates the residual stress distribution qualitatively is assumed. Crack analysis is performed by using the Muskhelishvili's stress function. Results are given in figures and table.     

Studies on the synthesis of proteinase inhibitors. II. Synthesis of cyclic nonapeptide fragments and analogs related to the reactive sites of soybean Bowman-Birk inhibitor

Several heterodetic cyclic nonapeptides modeled after the disulfide loops of Bowman-Birk inhibitor which involve either the anti-tryptic or anti-chymotryptic region have been synthesized by the conventional method. The inhibitory properties and the stabilities of these peptides toward trypsin and chymotrypsin, as well as the properties of dimers of the above nonapeptides, were examined.     

Two-dimensional multiarray formation of hepatocyte spheroids on a microfabricated PEG-brush surface

A two-dimensional microarray of ten thousand (100 x 100) hepatocyte heterospheroids, underlaid with endothelial cells, was successfully constructed with 100 microm spacing in an active area of 20 x 20 mm on microfabricated glass substrates that were coated with poly(ethylene glycol) brushes. Cocultivation of hepatocytes with endothelial cells was essential to stabilize hepatocyte viability and liver-specific functions, allowing us to obtain hepatocyte spheroids with a diameter of 100 microm, functioning as a miniaturized liver to secret albumin for at least one month. The most important feature of this study is that these substrates are defined to provide an unprecedented control of substrate properties for modulating cell behavior, employing both surface engineering and synthetic polymer chemistry. The spheroid array constructed here is highly useful as a platform of tissue and cell-based biosensors and detects a wide variety of clinically, pharmacologically, and toxicologically active compounds through a cellular physiological response.     

Fabrication of low-loss and wide-bandwidth v.a.d. optical fibres at 1.3 ?m wavelength

A low-loss and wide-bandwidth optical fibre in the long-wavelength region has been fabricated by the v.a.d. method. Loss at 1.3 ?m is 0.98 dB/km and 6 dB down bandwidth is 1600 MHz km at 1.26 ?m.     

Fourier synthesis image reconstruction by use of one-dimensional position-sensitive detectors

An improvement of Fourier synthesis optics for hard x-ray imaging is described, and the basic performance of the new optics is confirmed through numerical simulations. The original concept of the Fourier synthesis imager utilizes nonposition-sensitive hard x-ray detectors coupled to individual bigrid modulation collimators. The improved concept employs a one-dimensional position-sensitive detector (such as a CdTe strip detector) instead of the second grid layer of each bigrid modulation collimator. This improves the imaging performance in several respects over the original design. One performance improvement is a two-fold increase in the average transmission, from 1/4 to 1/2. The second merit is that both the sine and cosine components can be derived from a single grid-detector module, and hence the number of imaging modules can be halved. Furthermore, it provides information along the depth direction simultaneously. This in turn enables a three-dimensional imaging hard x-ray microscope for medical diagnostics, incorporating radioactive tracers. A conceptual design of such a microscope is presented, designed to provide a field of view of 4 mm and a spatial resolution of 400 microm.     

Electrochemical protein chip with arrayed immunosensors with antibodies immobilized in a plasma-polymerized film

An electrochemical protein chip was microfabricated. A thin-film three-electrode system, including an array of 36 platinum working electrodes, a set of thin-film Ag/AgCl electrodes, and platinum auxiliary electrodes, was integrated on a glass substrate. Capture antibodies were immobilized in a 4.5-nm-thick double layer of a hexamethyldisiloxane plasma-polymerized film. Because of their highly cross-linked network structure, the capture antibodies could be firmly immobilized. No nonspecific adsorption was observed during a series of procedures to detect target proteins, and electrochemical cross talk between neighboring sites was negligible. The sandwich immunoassay was conducted on a single chip using model proteins, alpha-1-fetoprotein and beta2-microglobulin. A distinct current increase following the oxidation of hydrogen peroxide produced by the enzymatic reaction of glucose oxidase was observed, which indicates that the capture proteins could actually bind the target proteins. Two kinds of protein were detected independently on multiple sites with respective capture antibodies.     

Human and chimpanzee face recognition in chimpanzees (Pan troglodytes): Role of exposure and impact on categorical perception.

The respective influences of exposure and inborn neural networks on conspecific and nonconspecific face processing remain unclear. Although the importance of exposure in the development of object and face recognition in general is well documented, studies explicitly comparing face recognition across species showed a species-specific effect. For instance, laboratory monkeys exposed daily to human faces were better at discriminating monkeys than humans, suggesting that the role of exposure may not be the only factor affecting cross-species recognition. In the present study, the authors investigated conspecific and nonconspecific face recognition in chimpanzees (Pan troglodytes) from 2 primate centers that provided different exposure to chimpanzee and human faces. The authors showed that the chimpanzees from the center providing more exposure to human faces than to chimpanzee faces were better at discriminating human faces than they were at discriminating chimpanzee faces. The chimpanzees from the other center did not show the same effect. A computational simulation was developed to evaluate the average similarities among human pictures and among chimpanzee pictures. Both categories were comparable. Chimpanzees' scores were significantly correlated with the similarity coefficients. Overall, the results show that exposure is a critical determinant in conspecific and nonconspecific face recognition. (PsycINFO Database Record (c) 2010 APA, all rights reserved)     

Enhanced path smoothing based on conjugate gradient descent for firefighting robots in petrochemical complexes*

The firefighting robot system (FFRS) comprises several autonomous robots that can be deployed to fire disasters in petrochemical complexes. For autonomous navigation, the path planner should consider the robot constraints and characteristics. Specifically, three requirements should be satisfied for a path to be suitable for the FFRS. First, the path must satisfy the maximum curvature constraint. Second, it must be smooth for robots to easily execute the trajectory. Third, it must allow reaching the target location in a specific heading. We propose a path planner that provides smooth paths, satisfy the maximum curvature constraint, and allows a suitable robot heading. The path smoother is based on the conjugate gradient descent, and three approaches are proposed for this path planner to meet all the FFRS requirements. The effectiveness of these approaches is qualitatively and quantitatively evaluated by examining the generated paths. Finally, the path planner is applied to an actual robot to verify the suitability of the generated paths for the FFRS, and planning is applied to another type of robot to demonstrate the wide applicability of the proposed planner.