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自从1996年蛋白酶抑制剂(PI)被使用到高效抗逆转录病毒治疗(HAART)中以来,HIV携带者的发病率和艾滋病患者的死亡率被大大降低。至今经美国FDA批准上市的蛋白酶抑制剂已有11种,其中多种药物被列为美国和欧洲HIV治疗指南的一线治疗方案。然而我国在这方面的报道还不足,因此,本文对HAART,蛋白酶抑制剂的发展史和海外临床应用现状作一综述。 相似文献
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Jing Fu Chongchong Tian Mengtao Xing Xinzhi Wang Hongli Guo Lixin Sun Lan Sun Zhenzhou Jiang Luyong Zhang 《Biomedicine & Pharmacotherapy》2014
KU004 is a newly synthesized compound which has been demonstrated possessing potent anti-cancer activities through targeting the highly-expressed protein HER2 on the surface of the cells. In this study, we investigated the potential roles of KU004 in the induced-cell cycle arrest in human breast cancer SK-BR-3 cells. KU004 could not only inhibit the proliferation of SK-BR-3 in a concentration-dependent manner but also induce G1 phase arrest in SK-BR-3 cells. The western blot results showed KU004 decreased the expression of cyclin D, CDK-4, p-Rb708/780, and up-regulated the p21. In order to verify whether KU004 takes the anti-tumor effect thought the regulation of PI3K/Akt pathway, we used western blot to detect the expression of protein Akt, Her2, p-Akt and p-Her2. Our results shown that after KU004 treatment, the amount of p-Akt and p-Her2 decreased but the total amount of Akt and Her2 remained unchanged. In conclusion, these results provide a framework for further exploration of KU004 as a novel chemotherapeutic for human breast tumors by modulating PI3K/Akt pathway. 相似文献
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Meijuan Wu Zhenzhou Jiang Huaqin Duan Lixin Sun Shuang Zhang Mi Chen Yun Wang Qin Gao Yuming Song Xiong Zhu Luyong Zhang 《Biomedicine & Pharmacotherapy》2013
Deoxypodophyllotoxin (DPT), a naturally occurring microtubule destabilizer, inhibits tubulin polymerization and causes cell cycle arrest at G2/M phase in tumor cells. However, the anti-tumor effect and specific mechanism of DPT in non-small cell lung cancer (NSCLC) are still poorly understood. In this study, we determined the anti-tumor effect and potential mechanism of DPT in the NSCLC cell line, NCI-H460 (H460). First, we demonstrated that DPT significantly inhibits the proliferation of H460 cells in vitro and the growth of H460 xenografts in vivo. In further studies, DPT triggered necroptosis in H460 cells with the following characteristics: (I) necrotic cell death morphology; (II) autophagy; (III) loss of plasma membrane integrity; (IV) loss of mitochondria membrane potential; (V) elevation of reactive oxygen species levels; and (VI) specific inhibition of necroptosis via a small molecule, necrostatin-1. This study also revealed that DPT has a similar effect towards the drug-sensitive cancer cell line, H460, and the drug-resistant cell line, H460/Bcl-xL. To our knowledge, this is the first report to document the induction of necroptosis by a microtubule-targeting agent to circumvent cancer drug resistance, thereby providing a new potential choice for clinical cancer therapy, especially drug-resistant cancer therapy. 相似文献
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光动力治疗是一种新型非侵入性治疗手段,其原理是光敏剂经激光触发后将能量转移至氧气,生成具有细胞毒性的单线态氧,从而诱导肿瘤细胞发生凋亡或坏死。作为一种氧依赖性治疗方式,光动力治疗的抗肿瘤效果明显受限于实体瘤的乏氧微环境。因此,逆转并改善肿瘤组织的缺氧情况可显著增强光动力治疗效果。本文重点讨论纳米递送系统介导的肿瘤增氧策略的研究进展,包括氧气直接递送策略、酶催化产氧递送策略、响应型材料原位产氧递送策略和微生物体供氧递送策略,以提高光动力治疗抗肿瘤效果,为进一步研究增氧型光动力治疗纳米给药系统提供了新思路和新方案。 相似文献
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SIM010603 is a structurally novel, oral, multi-targeted receptor tyrosine kinase inhibitor. This study investigated the anti-angiogenic and anti-tumor effects of SIM010603. 相似文献10.