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CXCR4分子结构与作用原理揭开为治疗艾滋病和癌症提供了新方法
发布时间： 2010-10-09 | 作者：刘霞http://www.stdaily.com 2010年10月09日 来源： 科技日报
本报讯 据英国广播公司（BBC）10月8日报道，美国科学家在最新出版的《科学》杂志报告称，他们获得了CXCR4分子结构的图像，也了解了该分子的工作原理。研究显示，CXCR4分子同艾滋病病毒（HIV）感染和癌症扩散有关，该分子会帮助HIV进入细胞，因此，阻断该分子有望治疗艾滋病和癌症。但也有专家表示，还需要对CXCR4的活动进行更详尽的了解。
加州斯克利普斯研究所的雷蒙德·斯蒂芬斯领导的研究团队使用x射线结晶学方法获得了CXCR4分子的图像，也了解了该分子的工作原理。图像显示，CXCR4分子会亲密地成双成对出现。
斯蒂芬斯表示，CXCR4分子结构提供了理解GPCR如何传递信息的全新角度。这些图像展示了如何设计出调节CXCR4活动或者阻止HIV病毒进入细胞的化合物，通过这种方法得到的化合物可以另辟蹊径对付HIV或者癌症。
CXCR4分子是“G蛋白结合受体（GPCR）”家族中的一员，“G蛋白结合受体”的超家族群已经被证明是许多药物的药理作用靶点。CXCR4分子会越过细胞膜并且将外部环境的信号传送到内部，它们对细胞生长、荷尔蒙分泌以及光感等与组织发育有关的过程都可以起到控制作用。一般而言，CXCR4也有助于激活免疫系统并且刺激细胞运动，但是，当激活受体的信号没有被正确调制时，CXCR4会加速癌症的恶化和扩散。慈善组织NAM主要帮助艾滋病患者改善生活，该组织的资深编辑凯茨·艾尔科恩指出，HIV利用很多受体进入细胞，比如，大多数艾滋病患者最先感染的一个病毒使用名为CCR5的受体进入细胞，随着时间的推移，病毒可能会使用CXCR4进入细胞，至于其中的缘由，目前还是个谜。不过，已经有几家公司研发出了阻止CCR5受体的药物。
艾尔科恩表示，能够同时阻止CCR5和CXCR4的药物或许可以有效地治疗艾滋病和癌症。但是，由于CXCR4同很多正常的免疫系统功能有关，阻止CXCR4的活动所产生的可能后果还需要更好地了解。
英国癌症研究所高级信息官约瑟菲娜·奎里多强调，CXCR4同很多癌症的恶化以及扩散有关，解开这种分子的结构是设计出抗癌新药的关键一步。
Published: 2010-10-09 | On: Liu Xia http://www.stdaily.com 2010 年 10 月 09 日 Source: Science and Technology Daily
WASHINGTON According to the British Broadcasting Corporation (BBC) 10 月 8 reported in the latest issue of American Scientists, "Science" magazine reported that the molecular structure of their access to the CXCR4 an image, but also to understand the working principle of the molecule. Study, CXCR4 molecules with the AIDS virus (HIV) infection and the spread of cancer is related to the molecule will help HIV enter cells, so blocking the molecule is expected to treat AIDS and cancer. But some experts said, but also the activities of CXCR4 more detailed understanding.
Scripps Research Institute, California Raymond Stephens led the research team used x-ray crystallography was obtained by the image CXCR4 molecules, but also to understand the working principle of the molecule. Image display, CXCR4 molecules occur in pairs close to.
Stephens said, CXCR4 GPCR understanding the molecular structure provides a new perspective on how to transmit information. These images show how to regulate CXCR4 activities designed to prevent HIV virus from entering cells or compounds, compounds obtained by this method can be another way to deal with HIV or cancer.
CXCR4 molecules are "G protein coupled receptor (GPCR)" family member, "G protein coupled receptor," the super-family group has been shown to be targets for the pharmacological effects of many drugs. CXCR4 molecules across the cell membrane and will signal to the external environment inside their cells, such as hormone secretion, and light perception related to the development process and organization can play a controlling role. In general, CXCR4 also help activate the immune system and stimulate cell motility, but when the signal is not activated receptor correct modulation, CXCR4 will accelerate the deterioration and spread of cancer. NAM major charitable organizations to help improve the lives of AIDS patients, the organization's senior editor Katz said Al Cohen, HIV enters cells using a lot of receptors, for example, the majority of AIDS patients infected with a virus the first use of a receptor called CCR5 into the cell, over time, the virus may use CXCR4 to enter cells, as to why, is still a mystery. However, several companies have developed drugs to block CCR5 receptor.
Al Cohen said that while blocking CCR5 and CXCR4 to the drug may be effective in treating AIDS and cancer. However, because a lot of CXCR4 with the normal immune system function related to the activities of CXCR4 to prevent the possible consequences arising from a better understanding of needs.
Senior information officer at Cancer Research UK where more emphasis 约瑟菲娜奎, CXCR4, and with the spread of the deterioration of many cancers is related to solve the structure of this molecule is to design a key step in anti-cancer drugs.
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