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【drug-news】新药物宣告可能预示灰指甲难治时代
Science Daily — A new mechanism to attack hard-to-treat fungal infections has been revealed by scientists from the biotech company Anacor Pharmaceuticals Inc., California, and the European Molecular Biology Laboratory [EMBL] outstation in Grenoble, France. In the current issue of Science they describe how a new compound kills fungal pathogens by blocking an enzyme crucial for their protein synthesis.
The human body is home to many different kinds of fungi. While the majority normally do not harm us, some fungi can cause unpleasant infections of skin, nails or lungs.
"We have discovered a new compound that has the potential to treat common chronic nail infections caused by fungi," says Dickon Alley, researcher at Anacor Pharmaceuticals. "The compound, called AN2690, kills fungi by blocking their ability to make proteins. It has been very successful in clinical trials." AN2690 interferes with an enzyme called leucyl-tRNA synthetase, which is involved in translation, one of the last steps in the process of turning a gene's DNA code into a protein.
The process begins when the cell makes an RNA version of the gene's code, called messenger RNA. Ribosomes, the cell's protein synthesis machinery, then translate the messenger RNA into protein by stitching together the amino acids in the order specified by the message. This requires the help of molecules called tRNAs, which link the code of the messenger RNA to the correct amino acid.
Leucyl-tRNA synthetase is one of a group of enzymes called aminoacyl-tRNA synthetases that attach the correct amino acid to each tRNA. Some of these enzymes have two main functional parts, or active sites: a site that links the amino acid to the tRNA, and a separate editing site that proofreads this process and removes wrongly added amino acids.
To find out how exactly AN2690 blocks leucyl-tRNA synthetase Stephen Cusack, Head of EMBL Grenoble, and his team generated crystals of the enzyme bound to tRNA in the presence of AN2690. Examining them with the high-intensity X-ray source at the European Synchrotron Radiation Facility, Cusack and his colleagues found that AN2690 sticks in the editing site of the enzyme where it makes a very strong bond to the end of the tRNA, trapping it on the enzyme.
This stops the enzyme working and thus blocks protein synthesis, killing the fungal cell. The mechanism crucially depends on a boron atom that is part of AN2690, which is needed to link the compound to the tRNA. It is the first time that scientists describe such a mechanism, suggesting boron containing compounds as a promising new class of drug candidates.
"Now that we know how AN2690 works, the same approach could be adapted to target other aminoacyl-tRNA synthetases with editing sites and also other pathogenic microbes," concludes Cusack. "We are now working towards finding related antibacterial compounds that could help counter the problem of antibiotic resistance."
http://www.sciencedaily.com/releases/2007/06/070622101043.htm 本人已认领该文编译，48小时后若未提交译文，请其他战友自由认领 New Compound Effectively Treats Fungal Infections
新型药物有效的治疗真菌感染
Science Daily — A new mechanism to attack hard-to-treat fungal infections has been revealed by scientists from the biotech company Anacor Pharmaceuticals Inc., California, and the European Molecular Biology Laboratory [EMBL] outstation in Grenoble, France. In the current issue of Science they describe how a new compound kills fungal pathogens by blocking an enzyme crucial for their protein synthesis.
科学每日—来自美国加里福尼亚Anacor药剂公司和法国格勒诺布尔的欧洲分子生物实验室的科学家们宣称找到了一种新的治疗顽固性真菌感染的方法。在最近一期科学杂志里，他们解释了这种新型复合物是如何通过抑制蛋白合成中的酶而杀死真菌病原体的。
The human body is home to many different kinds of fungi. While the majority normally do not harm us, some fungi can cause unpleasant infections of skin, nails or lungs.
人体是多种真菌的寄居处，但大多数对人体无害。一些真菌可以引起皮肤，指甲和肺部的感染。
"We have discovered a new compound that has the potential to treat common chronic nail infections caused by fungi," says Dickon Alley, researcher at Anacor Pharmaceuticals. "The compound, called AN2690, kills fungi by blocking their ability to make proteins. It has been very successful in clinical trials." AN2690 interferes with an enzyme called leucyl-tRNA synthetase, which is involved in translation, one of the last steps in the process of turning a gene's DNA code into a protein.
Anacor制药公司的Dickon Alley说“我们发现了一种可以治疗真菌引起的慢性指甲感染的新型复合物。”“这种被称作AN2690的复合物通过抑制蛋白合成而杀死真菌病原体，临床试验表明其作用很有效。”AN2690可以干扰亮胺酰tRNA合成酶。亮胺酰tRNA合成酶是翻译过程中的一种酶。翻译是指从DNA密码到蛋白质过程中的最后一步。
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作者:admin@医学,生命科学 2011-03-04 01:26
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