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【技术产业】将绿色海藻转变为抗肿瘤黄金药物

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http://www.ns.umich.edu/htdocs/releases/story.php?id=3088

Turning green gunk to gold, anti-cancer gold
ANN ARBOR, Mich.—Combining synthetic chemistry techniques with a knowledge of the properties and actions of enzymes, scientists have been able to produce an exciting class of anti-cancer drugs originally isolated from blue-green algae.

This accomplishment is expected to make it possible to produce enough of the promising drugs for use in clinical trials.

In a study featured on the cover of the January issue of the journal ACS Chemical Biology, a scientific team lead by University of Michigan Life Sciences Institute Research Professor David H. Sherman and researcher Zachary Q. Beck found the trick to turning the green gunk into gold—cancer fighting gold.

"It was simply too difficult to use the native blue-green algae for high-level production using traditional fermentation approaches," said Sherman. But the compound, called cryptophycin 1, held so much promise as an anti-cancer drug that organic chemists got busy trying to find ways to make a synthetic form of the compound in large enough quantities for clinical trials.

Developing an efficient synthetic route to natural product compounds and their analogs is often an essential step in drug development. With drugs such as penicillin and tetracycline, it can easily be done, but cryptophycins present more of a challenge. Sherman's team realized that with all cryptophycins, the most difficult step came very late in the synthesis, at the point at which a key part called an epoxide—a highly strained, three-membered ring oxygen-containing group, crucial for the drug's anti-cancer activity—becomes attached to the molecule.

The epoxide group can be attached in two configurations, designated as alpha and beta. Scientists have known for several years that the beta configuration was absolutely required for the anti-cancer properties of the drug, but were unable to devise efficient synthetic strategies that favored that configuration.

Sherman's team accomplished this by isolating the entire set of biosynthetic genes and key enzymes and developing a new, efficient method to manufacture the broad class of cryptophycin natural products, including important analogs with clinical potential. This included characterization of an enzyme, cytochrome P450, that always introduces the epoxide in the desired beta configuration.

Sherman, who is also the John G. Searle Professor of Medicinal Chemistry in the College of Pharmacy, believes that this approach will allow effective new cryptophycin analogs with low levels of side effects to be created for clinical trials.

"This issue represented an exciting target that offered not only an interesting scientific problem, but the potential to do something of practical importance in creating a promising anti-cancer drug," he said.

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2007-01-09 23:05 浏览 : 681 回复 : 2

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sunyongjun 编辑于 2007-01-09 23:09

• 盆腔肿物，少见病例，病理出来了，请你诊断

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2007-01-09 23:11

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Turning green gunk to gold, anti-cancer gold
将绿色海藻转变为抗肿瘤黄金药物

ANN ARBOR, Mich.—Combining synthetic chemistry techniques with a knowledge of the properties and actions of enzymes, scientists have been able to produce an exciting class of anti-cancer drugs originally isolated from blue-green algae.

密西根大学安娜堡分校.--结合合成化学技术和酶的性质及活性的认识，科学家已经能够制造出一类激动人心的抗癌药物，它最初是从蓝藻里分离出来的。

This accomplishment is expected to make it possible to produce enough of the promising drugs for use in clinical trials.

这个成果被期待有可能制造很有前途的药物用于临床试验

In a study featured on the cover of the January issue of the journal ACS Chemical Biology, a scientific team lead by University of Michigan Life Sciences Institute Research Professor David H. Sherman and researcher Zachary Q. Beck found the trick to turning the green gunk into gold—cancer fighting gold.

美国化学学会的化学生物学期刊今年一月版报道了一个研究，由密歇根大学生命科学研究所教授David H. Sherman和研究员Zachary Q. Beck领导的科学小组发现了把这种绿色黏性物质转化为抗癌黄金药物的技术。

"It was simply too difficult to use the native blue-green algae for high-level production using traditional fermentation approaches," said Sherman. But the compound, called cryptophycin 1, held so much promise as an anti-cancer drug that organic chemists got busy trying to find ways to make a synthetic form of the compound in large enough quantities for clinical trials.

Sherman说：利用传统的发酵方法很难利用这种天然的蓝藻作为高标准的产品，但它含有的cryptophycin 1这种化合物，很有希望成为一个抗癌药物，以至于有机化学家们正致力于在足够多的蓝藻中设法发现这种复合物的合成剂型用于临床试验。

Developing an efficient synthetic route to natural product compounds and their analogs is often an essential step in drug development. With drugs such as penicillin and tetracycline, it can easily be done, but cryptophycins present more of a challenge. Sherman's team realized that with all cryptophycins, the most difficult step came very late in the synthesis, at the point at which a key part called an epoxide—a highly strained, three-membered ring oxygen-containing group, crucial for the drug's anti-cancer activity—becomes attached to the molecule.

发展一种自然产物复合物以及类似物的有效合成途径在药物研制过程中经常是必需的步骤。例如盘尼西林和四环素这些药物容易研制；但cryptophycins目前还是个挑战。Sherman's 小组了解所有的cryptophycins，在合成最后最困难的一步，指向的一个关键部分是把一个环氧化物附加到分子上----这是一个大的可塑性，三元环氧的封闭基团，对于药物的抗癌活性有决定性作用。

The epoxide group can be attached in two configurations, designated as alpha and beta. Scientists have known for several years that the beta configuration was absolutely required for the anti-cancer properties of the drug, but were unable to devise efficient synthetic strategies that favored that configuration.

这个环氧基群能够被附加到两种构型, 命名为α和β。几年前科学家已经知道β-构型对于药物的抗癌特性来说是绝对必需的，但不能发明有效的合成策略得到这种构型。

Sherman's team accomplished this by isolating the entire set of biosynthetic genes and key enzymes and developing a new, efficient method to manufacture the broad class of cryptophycin natural products, including important analogs with clinical potential. This included characterization of an enzyme, cytochrome P450, that always introduces the epoxide in the desired beta configuration.

通过分离整个生物合成的基因组和关键酶，Sherman's 团队完成这个任务，并发展了一种全新有效的方法制造这一大类cryptophycin自然产物，包括重要的有临床潜力的同型物。还有细胞色素P450这个酶的鉴定，经常在想得到β-构型时引入这个环氧化物。

Sherman, who is also the John G. Searle Professor of Medicinal Chemistry in the College of Pharmacy, believes that this approach will allow effective new cryptophycin analogs with low levels of side effects to be created for clinical trials.

Sherman,也是John G. Searle药学院的药物化学教授，他相信这个进展可以制造出新的高效、低毒的cryptophycin类似物用于临床试验。

"This issue represented an exciting target that offered not only an interesting scientific problem, but the potential to do something of practical importance in creating a promising anti-cancer drug," he said.

他说，这个问题描绘了令人兴奋的目标，不仅提供有趣的科学难题，而且在发明一种有前途的抗癌药物时还有去做一些重要实践的可能性。

2007-01-10 19:35

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神农编辑于 2007-01-10 21:02

• 【心电旋律 27】青年男性心肌梗死背后的真凶！

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http://www.ns.umich.edu/htdocs/releases/story.php?id=3088

绿色海藻可作抗肿瘤黄金药物

密西根大学安娜堡分校1月8日消息称，应用合成化学技术及对酶的性质及活性的认识，科学家已经能够制造出一类令人激动的抗癌药物，它最初是从蓝藻里分离出来的。这一成果有望成为制造很有前途的药物用于临床试验。

美国化学学会的《化学生物学》今年一月刊报道了一项研究，由密歇根大学生命科学研究所教授David H. Sherman和研究员Zachary Q. Beck领导的科学小组，发现了将这种绿色黏性物质转化为抗癌黄金药物的技术。

Sherman说道，利用传统的发酵方法很难利用这种天然的蓝藻作为高标准的产品，但它含有的cryptophycin 1这种化合物，极有希望成为抗癌药物，以至于有机化学家们正致力于在足够多的蓝藻中设法发现这种复合物的合成剂型用于临床试验。

发展一种自然产物复合物以及类似物的有效合成途径在药物研制过程中经常是必需的步骤。例如盘尼西林和四环素这些药物容易研制；但cryptophycins目前还是个挑战。Sherman's 小组了解所有的cryptophycins，在合成最后最困难的一步，指向的一个关键部分是把一个环氧化物附加到分子上----这是一个大的可塑性，三元环氧的封闭基团，对于药物的抗癌活性有决定性作用。

这个环氧基群能够被附加到两种构型, 命名为α和β。几年前科学家已经知道β-构型对于药物的抗癌特性来说是绝对必需的，但未能找到有效的合成方法得到这种构型。

通过分离整个生物合成的基因组和关键酶，Sherman's 团队完成了该任务，并发展了一种全新有效的方法制造这一大类cryptophycin自然产物，包括重要的有临床潜力的同型物。

Sherman，也是John G. Searle药学院的药物化学教授，他相信这个进展可以制造出新的高效、低毒的cryptophycin类似物用于临床试验。

2007-01-10 22:55

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• 盆腔肿物，少见病例，病理出来了，请你诊断

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