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排序方式: 共有342条查询结果,搜索用时 531 毫秒
71.
Kazumasa Hirata Supanee Duangteraprecha Etsuko Morihara Motoyasu Honda Tomohiro Akagi Masuo Nakae Hiroshi Katayama Kazuhisa Miyamoto 《Biotechnology letters》1997,19(1):53-57
Vinblastine (VLB) is an antineoplastic agent contained in leaves of Catharanthus roseus. One-pot synthesis of VLB from vindoline and catharanthine, biosynthetic precursors in the plant, was achieved under biomimetic conditions. FMN-mediated coupling of vindoline and catharanthine under irradiation with near-ultraviolet light was followed by NAD(P)H-mediated direct conversion of the coupling product to VLB in the dark. The yield of VLB was governed by the level of NAD(P)H added, and the highest yield was obtained by incubation with 10 mM NAD(P)H for 5 h. It is postulated, as one concept of VLB biosynthesis, that similar non-enzymic VLB synthesis may occur in the plant leaves. 相似文献
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Pituitary adenylate cyclase activating polypeptide provokes cultured rat chromaffin cells to secrete adrenaline. 总被引:7,自引:0,他引:7
T Watanabe Y Masuo H Matsumoto N Suzuki T Ohtaki Y Masuda C Kitada M Tsuda M Fujino 《Biochemical and biophysical research communications》1992,182(1):403-411
Pituitary adenylate cyclase activating polypeptide (PACAP) provoked the rat chromaffin cells to secrete adrenaline. Within 20 min, the amount of adrenaline secreted by PACAP (10(-8) M) was as much as that caused by acetylcholine (10(-4) M). PACAP, but not acetylcholine, induced a long-term (over 120 min) increase in secretion of adrenaline. PACAP also activated adenylate cyclase and elevated cytosolic Ca2+ concentration. Furthermore, we found immunoreactive PACAP and PACAP binding sites in the rat adrenal medulla. These results suggest that PACAP has an important role in stimulating secretion of adrenaline in the adrenal medulla. 相似文献
74.
A novel proapoptotic gene PANO encodes a post-translational modulator of the tumor suppressor p14ARF
The protein p14ARF is a known tumor suppressor protein controlling cell proliferation and survival, which mainly localizes in nucleoli. However, the regulatory mechanisms that govern its activity or expression remain unclear. Here, we report that a novel proapoptotic nucleolar protein, PANO, modulates the expression and activity of p14ARF in HeLa cells. Overexpression of PANO enhances the stability of p14ARF protein by protecting it from degradation, resulting in an increase in p14ARF expression levels. Overexpression of PANO also induces apoptosis under low serum conditions. This effect is dependent on the nucleolar localization of PANO and inhibited by knocking-down p14ARF. Alternatively, PANO siRNA treated cells exhibit a reduction in p14ARF protein levels. In addition, ectopic expression of PANO suppresses the tumorigenicity of HeLa cells in nude mice. These results indicate that PANO is a new apoptosis-inducing gene by modulating the tumor suppressor protein, p14ARF, and may itself be a new candidate tumor suppressor gene. 相似文献
75.
Yamamoto S Tomita N Suzuki Y Suzaki T Kaku T Hara T Yamaoka M Kanzaki N Hasuoka A Baba A Ito M 《Bioorganic & medicinal chemistry》2012,20(7):2338-2352
A series of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole compounds B were designed, synthesized, and evaluated for their potential as new-generation androgen receptor (AR) antagonists therapeutically effective against castration-resistant prostate cancer (CRPC). Introduction of a bulky amide substituent (R(2)) to the terminal aryl ring of the 4-arylmethyl group favored the reduction of agonistic activity and improved the pharmacokinetic (PK) properties. Similarly, introduction of a bulky substituent in the 4-aryloxy derivatives also resulted in improved PK properties. Compounds 28 h and 44b exhibited potent antitumor effects against a CRPC model of LNCaP-hr cell line in a mouse xenograft model. On the contrary, bicalutamide showed only partial suppression of tumor growth. These results suggest that the novel pyrazole derivatives are new-generation AR antagonists, different from the 'first-generation' antagonists such as bicalutamide in a CRPC treatment model. 相似文献
76.
Terabayashi Y Shimizu M Kitazume T Masuo S Fujii T Takaya N 《Applied microbiology and biotechnology》2012,93(1):305-317
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Satoshi Niizuma Masao Tsukazaki Hitomi Suda Takeshi Murata Jun Ohwada Sawako Ozawa Hiroshi Fukuda Chikako Murasaki Masami Kohchi Kenji Morikami Kiyoshi Yoshinari Mika Endo Masako Ura Hiromi Tanimura Yoko Miyazaki Tsuyoshi Takasuka Akira Kawashima Eitaro Nanba Kounosuke Nakano Kotaro Ogawa Nobuo Shimma 《Bioorganic & medicinal chemistry letters》2009,19(7):2018-2021
Novel hexacyclic camptothecin analogs containing cyclic amidine, urea, or thiourea moiety were designed and synthesized based on the proposed 3D-structure of the topoisomerase I (Topo I)/DNA/camptothecin ternary complex. The analogs were prepared from 9-nitrocamptothecin via 7,9-diaminocamptothecin derivatives as a key intermediate. Among them, 7c exhibited in vivo antitumor activities superior to CPT-11 in human cancer xenograft models in mice at their maximum tolerated doses though its in vitro antiproliferative activity was comparable to SN-38 against corresponding cell lines. 相似文献
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