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1.
MOTOYOSHI NOMIZU YOSHIMASA INAGAKI TAKEYOSHI YAMASHITA AKO OHKUBO AKIRA OTAKA NOBUTAKA FUJII PETER P. ROLLER HARUAKI YAJIMA 《Chemical biology & drug design》1991,37(2):145-152
A new two-step deprotection/cleavage procedure for t-butoxycarbonyl (Boc) based solid phase peptide synthesis is reported. First the protective groups are removed from 4-(oxymethyl)-phenylacetamidomethyl (PAM) resin attached peptide with the weak hard acid, trimethylsilyl bromide-thioanisole/trifluoroacetic acid (TFA). In the second step, the peptide is cleaved from the resin with a stronger hard acid such as trimethylsilvl trifluoromethanesulfonate in TFA or with HF. The method is also shown to deformylate Nin-formyltryptophan moiety efficiently. The usefulness of this procedure for practical solid phase peptide synthesis is demonstrated by comparison with other deprotection methods in the synthesis of urotensin II and human endothelin. 相似文献
2.
In order to investigate the validity of the hypothesis that acid-soluble peptides (ASP) in urinary excreta can be applied as an index of the protein catabolism of the whole body, we measured the urinary excretion of ASP in 46 normal children and in 18 children with Duchenne muscular dystrophy (DMD), in which continuous breakdown of skeletal muscle protein is presumed. The mean value of ASP in the children with DMD was significantly higher than that in normal controls. The concentration of ASP was correlated with that of 3-methylhistidine (3MH), which has been proposed as an index of muscle breakdown. This finding indicates that urinary ASP reflects the catabolism of body proteins. No correlation was observed between the concentration of ASP and that of 1-methylhistidine (1MH), which is used as an objective index of meat and fish ingestion. After the administration of bestatin, an inhibitor of leucine aminopeptidase, for 9 months, the urinary ASP concentration of children with DMD increased markedly. This increase is thought to have been directly caused by the bestatin itself. Urinary ASP is therefore apparently a more conveniently applied index of protein catabolism than is urinary 3MH, which requires the application of several restrictions. However, it should not be applied when the effect of bestatin administration is evident. 相似文献
3.
MOTOYOSHI NOMIZU TAKANORI IWAKI TAKEYOSHI YAMASHITA YOSHIMASA INAGAKI KATSUHIKO ASANO MIKI AKAMATSU TOSHIO FUJITA 《Chemical biology & drug design》1993,42(3):216-226
One hundred Suc-X-Y-Ala-pNA peptides (SUC: succinyl, pNA: p-nitroanilide, X, Y: Gly, Ala, Val, Leu, Ile, Phe, Pro, x-aminobutyric acid, norvaline, norleucine) were synthesized and their reaction constants with porcine pancreatic elastase (Km, Kcat and Kcat/Km) were determined. These reaction constants were quantitatively analyzed using the Free–Wilson/Fujita–Ban method. The contribution of amino acid side chains to the reaction constants Km, Kcat and Kcat/Km), expressed logarithmically, was found to be additive. On the other hand, 19 elastase inhibitors of the general formula CF3CO-X-Y-Ala-pNA (X,Y: ten amino acids) were synthesized, and their inhibition constants were compared with the Michaelis constant for the corresponding substrates and analyzed using free-energy-related substituent constants. In the analysis of amino acid side chains in the Y position, the Ki value of the inhibitor was generally correlated to the Km value of the substrate, which corresponded to the inhibitor, thus confirming the validity of the equation This study may serve as a prototypical approach to unraveling structure–activity relationships of peptide substrates and inhibitors of medicinal or agricultural importance. 相似文献
4.
TAKAKURA KINTOMO; MIKI YOSHIMASA; KUBO OSAMI; OGAWA NOBUKO; MATSUTANI MASAO; SANO KEIJI 《Japanese journal of clinical oncology》1972,2(2):109-120
New methods of adjuvant immunotherapy were introduced for thetreatment of malignant brain tumors. Allogeneic bone marrowcell transfusion or local intratumoral infusion of allogeneicor autologous peripheral white blood cells were conducted on18 patients having malignant glioma, after ordinary treatmentof operation, radiation or chemotherapy. The survival rate ofthese patients was significantly prolonged when compared withthe rate normally expected. No side effects were noted. Morphologicalchanges of cells in the cerebrospinal fluid taken from the intratumoralcavity, before and after infusion of peripheral white bloodcells, were studied. Cytolysis and phagocytosis of tumor cellsby macrophages were observed. Suppressive mechanism of immunologicallycompetent cells on glioma cells was partly studied, cytologicallyin vitro. 相似文献
5.
SATOSHI KOYAMA TAKESHI INOUE TAKAO TARAL KOICHI TAKIMOTO MASAYUKI KATO KIYOTAKA ITO MASHAHIRO NEYA JIRO SEKI YUJI KOBAYASHI YOSHIMASA KYOGOKU KEIZO YOSHIDA 《Chemical biology & drug design》1994,43(4):332-336
AP-811 is a derivative of the Phe8-Ile15 region of atrial natriuretic peptide (ANP) and is one of the smallest linear ligands for ANP receptors. The binding and agonist activities of AP-811 have been compared with those of other ANP analogs for the ANP-A and ANP-C receptors. AP–811 binds with a high binding affinity to and is a strong agonist for the ANP-C receptor, indicating that the binding and agonist sites for this receptor are the same or near each other in the ANP sequence. In contrast, AP-811 showed no agonistic effect for the ANP-A receptor, although it could bind to this receptor. Comparing the biological activities of AP-811 with those of other ANP analogs, we propose that the binding and agonist sites for the ANP-A receptor may consist of separate regions of ANP. In conclusion, AP-811 is the smallest C-receptor-selective agonist. 相似文献
6.
JUN‐ICHI OKADA Ph.D. TERUYOSHI SASAKI M.Sc. TAKUMI WASHIO M.Sc. HIROSHI YAMASHITA M.D. Ph.D. TARO KARIYA M.D. YASUSHI IMAI M.D. Ph.D. MACHIKO NAKAGAWA M.Sc. YOSHIMASA KADOOKA Ph.D. RYOZO NAGAI M.D. Ph.D. TOSHIAKI HISADA Ph.D. SEIRYO SUGIURA M.D. Ph.D. 《Pacing and clinical electrophysiology : PACE》2013,36(3):309-321
7.
This study was designed to determine precisely the radiosensitive period in the development of ICR mouse embryos during which external malformations and growth retardation tend to occur. Female and male mice were placed together for only three hours to allow fairly precise identification of the time of conception. The pregnant mice were divided into 31 groups, which were irradiated in turn with 1.5 Gy gamma radiation at 6-hour intervals during the period of organogenesis. They were then observed on day 18 of gestation. Items recorded were intrauterine death, external malformations, sex ratio and fetal body weight. Death of the embryo/fetus, especially death in the early period of organogenesis, was most frequent in mice irradiated between days 6.75 and 8.25 of gestation, but there was no statistically significant difference in the frequency of early- and late-period deaths between irradiated and control groups. The types and frequencies of external malformations observed differed according to the exposure period. The most highly sensitive period for each malformation lasted no more than 12 hours. Reduction of fetal body weight was a good indicator of radiation effects, and was observed mostly in the groups irradiated between days 9.75 and 11.00 of gestation. The sex ratio was not affected by the period in which irradiation was performed. 相似文献
8.
TETSUYA OGINO MASAYASU INOUE YUKIO ANDO MICHIYASU AWAI HIROSHI MAEDA YOSHIMASA MORINO 《Chemical biology & drug design》1988,32(2):153-159
Protection of organisms from oxidative stress is one of the major prerequisites for aerobic life. Since intravenously injected Cu++/Zn++ -type superoxide dismutase (SOD) rapidly undergoes renal glomerular filtration and appears in urine in its intact form, its clinical use as a scavenger for superoxide radicals has been highly limited. To test whether reversible interaction of SOD with plasma albumin might decrease the rate of disappearance of the enzyme from the circulation, the lysyl residues of the human erythrocyte-type enzyme were covalently linked with poly-(styrene-co-maleic acid) butyl ester (SMA) via amide linkage. Affinity chromatographic analysis by an albumin-Sepharose column revealed that the enzyme samples labeled with SMA (SMA-SOD) tightly bound to the column, while unmodified SOD was eluted in the unbound fractions. SMA-SOD bound to the column could be eluted by the buffer solution containing 0.1% sodium dodecylsulfate. In vivo analysis revealed that intravenously administered SMA-SOD circulated bound to albumin with an extremely long half-life (6 h), while unmodified SOD rapidly underwent renal glomerular filtration with a plasma half-life of 4min. Thus, SMA-SOD may effectively dismutate superoxide radicals in the circulation. 相似文献
9.
10.
YOSHIMASA SHISHIBA YASUNORI OZAWA TAEKO SHIMIZU NATSUKO OHTSUKI 《Clinical endocrinology》1982,17(3):207-212
LATS has already been shown to be neutralized by an unknown antigenic substance in human thyroid tissue. This antigen has been presumed to be a TSH receptor. To examine this hypothesis, we sought to determine whether SH reagents capable of altering the characteristics of TSH receptors in thyroidal crude membrane fractions caused an alteration in the LATS neutralization activity of the same fraction. Diamide (10?3m ) which was shown to enhance 125I-TSH binding to TSH receptors by increasing the binding affinity of the receptor, significantly increased the neutralization of LATS by the crude membrane fraction. Dithiothreitol (10?3m ) which was shown to inhibit 125I-TSH binding by decreasing the affinity of the receptor, significantly decreased the neutralization of LATS by the fraction. This indicates that TSH receptors and the thyroidal factor capable of neutralizing LATS share a common property in terms of the effects of SH reagents and is compatible with the idea that the LATS neutralizing activity of thyroidal crude membrane fraction is due to binding by the TSH receptor or its fragments. 相似文献