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2004年12月31日

【期刊论文】抗HIV-1活性的大环多胺类化合物与RNA的识别作用及其对细胞凋亡的影响*

杨铭, 郝美荣), 杨铭)**, 卜显和)

生物化学与生物物理进展,2002,29(2):211~216,-0001,():

-1年11月30日

摘要

研究了具有抗HIV-1活性的大环多胺类化合物与RNA的识别作用,以及其对cos-7细胞凋亡的影响,以进一步探讨其抗HIV-1的作用机理。实验采用琼脂糖凝胶电泳方法,观察化合物与RNA的识别作用;通过流式细胞计数法探讨其对cos-7细胞凋亡的影响;运用计算机分子模型,从理论上Docking计算化合物与TAR RNA结合的可能性。结果表明,大环多胺类化合物MP-1、MP-2和MP-3不仅具有断裂RNA的作用,并可抑制Tat-RNA的相互作用,还可影响cos-7细胞亚二倍体的含量;理论化学计算数据与实验结果基本一致。这一结果提示化合物的抗HIV-1活性可能通过作用于病毒基因组RNA而发挥作用,是多靶作用的结果。

HIV-1,, 大环多胺,, 凋亡,, Docking

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2005年06月16日

【期刊论文】Synthesis of unimolecularly circular G-quadruplexes as prospective molecular probes

杨铭, Tianyan Zhou, , Guoshu Chen, Yifan Wang, Qiang Zhang, Ming Yang and Tianhu Li, *

Nucleic Acids Research, 2004, Vol. 32, No.21,-0001,():

-1年11月30日

摘要

Synthesis of unimolecularly circular G-quadruplex has been accomplished for the first time during our investigation on the template basis of G-quadruplex through chemical ligations of guanine-rich linear sequencesofoligodeoxyribonucleotides. Theuniqueness of this newly designed circularization course is its self-recognition and self-templating on the scale of individual strand of zligodeoxyribonucleotide in which the same linear sequence serves both as a template and as a substrate simultaneously. The results from our exonuclease and DNAse hydrolysis studies confirm that there is indeed absence of open termini within the structure of the identified circular product. Our subsequent investigation on the loopsize effect indicates that the unimolecularly circular G-uadruplex possessing two or more thymine nucleotides within their connecting loops is readily attainable, while the linear sequence with a single thymine nucleotide between guanine tracts is not a proper precursor for our ligation reaction. In addition, conformation dependency of the circularization course as well as the effects of alkali ions, pH values and concentration of potassium ions on the circularization reaction are examined during our investigation. The implication of our current studies and possible application of the obtained unimolecularly circular G-quadruplex in certain biological processes are also discussed in this report.

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2004年12月31日

【期刊论文】Synthesis, crystal structure, antitumor activity and DNA-binding study on the Mn(Ⅱ) complex of 2H-5-hydroxy-1, 2, 5-oxadiazo[3, 4-f]1,10-phenanthroline

杨铭, Zhi-Dong Xu a, He Liu b, Su-Long Xiao a, Ming Yang a, *, Xian-He Bu b

Journal of Inorganic Biochemistry 90(2002)79-84,-0001,():

-1年11月30日

摘要

The complex [Mn(L)(NO3)2(H2O2)] (1) (L=2H-5-hydroxy-1, 2, 5-oxadiazo[3, 4-f]1,10-phenanthroline) was synthesized and characterized by elemental analysis, IR and UV. The crystal and molecular structure of 1 was determined by single-crystal X-ray diffraction; crystal data: light yellow, monoclinic, space group P21/n, Z=4, a=7.432(2)

Mn(, Ⅱ), complex, 2H-5-Hydroxy-1,, 2,, 5-oxadiazo[3,, 4-f]1,, 10-phenanthroline, Crystal structure, Antitumor activity, DNA-binding interaction

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2004年12月31日

【期刊论文】人免疫缺陷病毒-1整合酶及其抑制剂的研究进展

杨铭, 肖苏龙综述, 杨铭审校

Foreign Medical Sciences Section on Pharmacy 2002 Jun; 29(3),-0001,():

-1年11月30日

摘要

整合酶(integrase)对于人免疫缺陷病毒(HIV)-1逆转录病毒的复制来说是必不可少的,因而成为抗艾滋病(AIDS)药物设计的一个理性的靶点。最近文献报道了大量具有抗整合酶活性的化合物,当前最大的挑战就是如何将这些作用于整合酶靶点的先导化合物转变成为临床上有效的抗AIDS药物。

艾滋病, 整合酶, 整合酶抑制剂

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2005年06月16日

【期刊论文】Synthesis, Biological Evaluation and DNA Binding Properties of Novel Bleomycin Analogues

杨铭, Zhi-Dong Xu, Min Wang, Su-Long Xiao, Chun-Li Liu, and Ming Yang*

Bioorganic & Medicinal Chemistry Letters 13 (2003) 2595-2599,-0001,():

-1年11月30日

摘要

Aseries of bleomycin analogues was prepared with a facile synthetic method. All the compounds were shown to display significant antitumor activity against HeLa and BGC-823 cell lines in vitro. The binding properties with CT-DNAand cleavage efficiency to pBR322 DNAwere investigated, the results indicate that there is a positive relationship between DNAcleavage efficiency and the binding affinity to DNA, and the antitumor activity of the bleomycin analogues is enhanced as the hydrophobicity of the C-terminus substituent side chain increased.

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  • 杨铭 邀请

    北京大学,北京

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