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新药研究中的组合技术Ⅰ.肽化学库 被引量:1
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作者 刘刚 《中国药物化学杂志》 CAS CSCD 1995年第4期303-310,共8页
新药研究中的组合技术Ⅰ.肽化学库刘刚(军事医学科学院毒物药物研究所,北京100850)最大限度地筛选化合物的数量及不断产生结构上各异的化合物,以期首先找到具有药效作用的先导化合物是当今世界上各大医药公司及研究所正在努... 新药研究中的组合技术Ⅰ.肽化学库刘刚(军事医学科学院毒物药物研究所,北京100850)最大限度地筛选化合物的数量及不断产生结构上各异的化合物,以期首先找到具有药效作用的先导化合物是当今世界上各大医药公司及研究所正在努力的一个重要课题。在新药开发过程中... 展开更多
关键词 新药研究 类药物 组合化学 肽化学库 合成
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从组合化学肽库中筛选亲和配基 被引量:4
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作者 方灿良 赵睿 +3 位作者 刘阳 余晓 熊少祥 刘国诠 《高等学校化学学报》 SCIE EI CAS CSCD 北大核心 2003年第1期52-54,共3页
A new method for the rapid and efficient screening of affinity ligands to biological targets is reported. The fusion peptide of influenza virus A was used as the model target and immobilized on the PGMA beads. Antisen... A new method for the rapid and efficient screening of affinity ligands to biological targets is reported. The fusion peptide of influenza virus A was used as the model target and immobilized on the PGMA beads. Antisense peptide YRSKQA of fusion peptide was chosen as the lead compound. The special positional scanning peptide libraries were designed based on YRSKQA and synthesized by utilizing solid phase peptide synthesis manually. The libraries were YRSKQX, YRSKXA, YRSXQA, YRXKQA, YXSKQA and XRSKQA, where X represented 18 L-amino acids(except for Cys and Trp). Each library was screened by affinity chromatography. The eluates from the fusion peptide affinity column were collected and analyzed by RP-HPLC and MS, respectively, in order to determine the kind of X at each position. After the preferred residues of six positions were decided, the two preferred peptide sequences, GRGKHK and TRGKHK, were obtained. The dissociation constants of GRGKHK, TRGKHK and YRSKQA, were 3.35×10 -6, 5.24×10 -6 and 1.15×10 -5 mol·L -1, respectively. The preferred peptides showed the higher affinity binding to immobilized fusion peptide than the lead peptide. 展开更多
关键词 组合化学 亲和配基 解离常数 固相 合成 亲和色谱
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组合化学在新药研究中的应用
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作者 吴鸣虎 杨诗玉 《咸宁师专学报》 2000年第6期50-54,共5页
综述了组合化学在新药研究中的应用 ,着重介绍了小分子库。
关键词 组合化学 药物先导化合物 肽化学库 有机小分子化学 快速筛选
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抗肿瘤小分子多肽的研究进展 被引量:7
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作者 张冉 劳兴珍 郑珩 《氨基酸和生物资源》 CAS 2012年第4期42-46,共5页
抗肿瘤小分子多肽具有分子量小、低毒性、高活性、易于穿透肿瘤细胞等特点,一些抗肿瘤小分子多肽已进入临床研究,成为肿瘤药物研发的新热点。本文从抗肿瘤小分子多肽的不同来源途径、结构改造及生物活性等方面,对其近年来的研究进展作... 抗肿瘤小分子多肽具有分子量小、低毒性、高活性、易于穿透肿瘤细胞等特点,一些抗肿瘤小分子多肽已进入临床研究,成为肿瘤药物研发的新热点。本文从抗肿瘤小分子多肽的不同来源途径、结构改造及生物活性等方面,对其近年来的研究进展作简要概述。 展开更多
关键词 抗肿瘤 小分子多 噬菌体 化学合成
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Rational design and functional evolution of targeted peptides for bioanalytical applications 被引量:1
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作者 Yanyan Huang Yulong Jin Rui Zhao 《Science China Chemistry》 SCIE EI CAS CSCD 2016年第10期1250-1257,共8页
The complicated, highly dynamic and diverse nature of biosystems brings great challenges to the specific analysis of molecular processes of interest. Nature provides antibodies for the specific recognition of antigens... The complicated, highly dynamic and diverse nature of biosystems brings great challenges to the specific analysis of molecular processes of interest. Nature provides antibodies for the specific recognition of antigens, which is a straight-forward way for targeted analysis. However, there are still limitations during the practical applications due to the big size of the antibodies, which accelerate the discovery of small molecular probes. Peptides built from various optional building blocks and easily achieved by chemical synthetic approaches with predictable conformations, are versatile and can act as tailor-made targeting vehicles.In this mini review, we summarize the recent developments in the discovery of novel peptides for bioanalytical and biomedical applications. Progresses in peptide-library design and selection strategies are presented. Recent achievements in the peptide-guided detection, imaging and disease treatment are also focused. 展开更多
关键词 PEPTIDE DESIGN SCREENING targeted analysis biomedical applications
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