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61.
Bianchi M Adur J Takizawa S Saida K Casco VH 《Biochemical and biophysical research communications》2012,417(4):1113-1118
The endothelin system consists of three ligands (ET-1, ET-2 and ET-3) and at least two receptors (ETA and ETB). In mice ET-2 counterpart is a peptide originally called "vasoactive intestinal contractor" (VIC) for this reason, this peptide is frequently named ET-2/VIC. In intestinal villi, fibroblasts-like cells express endothelin's receptors and response to ET-1 and ET-3 peptides, changing their cellular shape. Several functions have been attributed to these peptides in the "architecture" maintenance of intestinal villi acting over sub-epithelial fibroblasts. Despite this, ET-2/VIC has not been analyzed in depth. In this work we show the intestine gene expression and immunolocalization of ET-1, ET-2 and the ETA and ETB receptors from duodenum to rectus and in the villus-crypt axis in mice, allowing a complete analysis of their functions. While ET-1 is expressed uniformly, ET-2 had a particular distribution, being higher at the bottom of the villi of duodenum, ileum and jejunum and reverting this pattern in the crypts of colon and rectus, where the higher expression was at the top. We postulated that ET-2 would act in a cooperative manner with ET-1, giving to the villus the straight enough to withstand mechanical stress. 相似文献
62.
Yoneda Y Kawajiri S Sugimura M Osanai K Kito F Ota E Mimura T 《Bioorganic & medicinal chemistry letters》2001,11(19):2663-2666
We synthesized diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists with non-hypotensive activity. Compound 10c showed selective Ca(2+)-permeable AMPA receptor antagonist activity and neuroprotective effects in transient global ischemia models in gerbils. 相似文献
63.
Li J Isozaki K Okada K Matsushima A Nose T Costa T Shimohigashi Y 《Bioorganic & medicinal chemistry》2008,16(5):2635-2644
Nociceptin is an endogenous agonist ligand of the ORL1 (opioid receptor-like 1) receptor, and its antagonist is a potential target of therapeutics for analgesic and antineuropathy drugs. Ac-RYYRIK-NH(2) is a hexapeptide isolated from the peptide library as an antagonist that inhibits the nociceptin activities mediated through ORL1. However, the structural elements required for this antagonist activity are still indeterminate. In the present study, we evaluated the importance of the acetyl-methyl group in receptor binding and activation, examining the peptides acyl-RYYRIK-NH(2), where acyl (R-CO) possesses a series of alkyl groups, R=C(n)H(2n+1) (n=0-5). The isovaleryl derivative with the C(4)H(9) (=(CH(3))(2)CHCH(2)-) group was found to reveal a high receptor-binding affinity and a strong antagonist nature. This peptide achieved a primary goal of eliminating the agonist activity of Ac-RYYRIK-NH(2) and producing pure antagonist activity. 相似文献
64.
Kaname Isozaki Hidehiko Fukahori Takeshi Honda Naoto Shirasu Kazushi Okada Takeru Nose Kazuyasu Sakaguchi Yasuyuki Shimohigashi 《International journal of peptide research and therapeutics》2003,10(5-6):511-522
The S-3-nitro-2-pyridinesulfenyl (SNpys) group in an affinity ligand can bind to a free thiol group of a cysteine residue in a
target receptor molecule, forming a disulfide bond via the thiol-disulfide exchange reaction. SNpys-containing Leu-enkephalin
analogues of [-Ala2, Leu5]-enkephalyl-Cys(Npys)6 and [-Ala2,Leu(CH2SNpys)5]enkephalin, and dynorphin A analogues of [-Ala2,Cys(Npys)12]dynorphin A-(1-13) amide and [-Ala2,Cys(Npys)8]dynorphin A-(1-9) amide have been found to affinity-label all of the δ, μ (rat brain), and κ (guinea pig brain) opioid receptor subtypes. In this study, using these chemically synthesized SNpys-containing analogues,
we attempted to identify the analogues that affinity-label the cysteine residue at position 60 of the δ opioid receptor. We first established the assay procedure, principally based on the receptor binding assay to use COS-7 cells
expressing the δ opioid receptor. Then, using a mutant δ receptor with the Cys60→Ala substitution, we assayed the SNpys-containing analogues for their specific affinity-labeling. [-Ala2,Cys(Npys)12]dynorphin A-(1-13) amide was found to have drastically reduced labeling activity for this mutant receptor as compared to
its activity for the wild-type δ receptor. Other analogues exhibited almost the same activity for both the wild-type and mutant δ receptors. These results indicate that the δ-Cys60 residue has a free thiol group, which is labeled by [-Ala2,Cys(Npys)12]dynorphin A-(1-13) amide. 相似文献
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68.
Loss of tubulin during cold treatment of cultured carrot cells 总被引:1,自引:0,他引:1
When carrot cells, Daucus carota L. cv. Kintoki, in suspension culture were chilled on ice, more than 90% of the cortical microtubules disappeared within an hour. Colchicine-binding activity in the soluble extract decreased gradually during the prolonged cold treatment and after 4 days reached a minimum level. In SDS-polyacrylamide gel electrophoretograms of the cold-treated cell extracts, the bands corresponding to tubulin subunits disappeared, whereas most of the other protein bands remained. The level of tubulin was restored within a day after the cells were returned to 267deg;C. The relative ratio of the two major β-tubulin isoforms was reversed during the cold treatment, indicating that the cold sensitivity of tubulin differs according to its molecular species. When the cells were returned to 26°C, the ratio was restored to the original state within 24 h. 相似文献
69.
Hiroya Obama Tadashi Kaname Akiharu Sudou Toyoko Yanagida Shinya Ikematsu Masayuki Ozawa Hiroki Yoshida Reiji Kannagi Ken-Ichi Yamamura Takashi Muramatsu 《Glycoconjugate journal》1995,12(6):795-801
cDNA of human -1,3/4-fucosyltransferase (Fuc-TIII) was placed under the control of the chicken -actin promoter and cytomegalovirus enhancer, then introduced into male pronuclei of fertilized mouse eggs. A transgenic mouse line thus obtained exhibited enhanced expression of Lex (4C9) antigen in endothelial cells located in the glomerulus, sinusoidal capillaries of the liver and capillaries of the heart. Furthermore, in the transgenic mice, sialyl dimeric Lex (FH6) and sialyl Lea (2D3), antigens were strongly expressed in the glomerular endothelial cells. 相似文献
70.
AGR,an Agravitropic Locus of Arabidopsis thaliana, Encodes a Novel Membrane-Protein Family Member 总被引:4,自引:0,他引:4
Utsuno Kaname; Shikanai Toshiharu; Yamada Yasuyuki; Hashimoto Takashi 《Plant & cell physiology》1998,39(10):1111-1118
Mutations in the Agr locus of Arabidopsis thaliana impair theroot gravitropic response. Root growth of agr mutants is moderatelyresistant to ethylene and to an auxin transport inhibitor. Verticallyplaced agr roots grow into agar medium containing IAA or naphthalene-1-aceticacid, but not into medium containing 2,4-D. Positional cloningshowed that AGR encodes a root-specific member of a novel membrane-proteinfamily with limited homology to bacterial transporters. (Received September 4, 1998; Accepted September 21, 1998) 相似文献