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【drug-news】衍生于Rb2/p130的小分子可治疗癌症
Public release date: 20-Mar-2007
Small molecule derived from Rb2/p130 could act as cancer therapeutic
A small molecule derived from the spacer domain of the tumor-suppressor gene Rb2/p130 has demonstrated the ability to inhibit tumor growth in vivo and could be developed into an anti-cancer therapeutic, according to researchers at Temple University's Sbarro Institute for Cancer Research and Molecular Medicine.
The researchers reported their findings, "A small molecule based on the pRb2/p130 spacer domain leads to inhibition of cdk2 activity, cell cycle arrest and tumor growth reduction in vivo," in the March 22 issue of the journal Oncogene (http://www.nature.com/onc). Rb2/p130 was discovered in the early 1990s by Antonio Giordano, director of the Sbarro Institute (http://www.shro.org) and the Center for Biotechnology in Temple's College of Science and Technology, who headed the study.
The researchers discovered that within Rb2/p130's spacer domain--a sequence of 212 amino acids located in the pocket or middle section of the gene--was a small portion that resembled an amino-acidic sequence contained in the protein p21, which acts as a cdk (cyclin dependent kinase) inhibitor. Cdks play a critical role in cell cycle regulation.
"What we tested was the ability of the Rb2/p130 spacer region to inhibit the kinase activity of cdk2, which is the same kinase p21 inhibits," said Giordano, one of the study's lead authors. "And to our surprise, it happened." The researchers then set about trying to reduce the spacer domain's 212 amino acids down to the smallest sequence that would still produce the same functionality as p21, explained Giordano.
"We thought we could narrow down the spacer region that contains the protein-like motif to a small portion that could be delivered as a small molecule or peptide," Giordano said.
They discovered a 39 amino-acid-long sequence, which they named Spa310. The molecule that was synthetically produced in the laboratory was introduced into mice that had been injected with tumor cells.
"Tumor growth was inhibited and the tumors began to reduce in size until they disappeared," Giordano said.
Giordano said because of the intrinsic nature of the compound, it can be easily reproduced as a biological drug in large quantities and does not require potentially dangerous means of delivery like viruses, as do most gene therapies; therefore Spa310 has a good chance to succeed as an anti-cancer therapy. For these reasons, he believes it may be easier to get approval for clinical trials.
"Fifteen years after discovering Rb2/p130, our research and hard work has led us to the discovery of this small molecule, which is a step forward in cancer research and a big step toward a cancer treatment," he said. 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 一种源于肿瘤抑制基因Rb2/p130的小分子多肽可治疗癌症
A small molecule derived from the spacer domain of the tumor-suppressor gene Rb2/p130 has demonstrated the ability to inhibit tumor growth in vivo and could be developed into an anti-cancer therapeutic, according to researchers at Temple University's Sbarro Institute for Cancer Research and Molecular Medicine.
据Temple大学Sbarro癌症研究与分子医学研究所的研究人员说，一种源于肿瘤抑制基因Rb2/p130间隔区的小分子多肽显示出在体抑制肿瘤生长的能力，有望开发成一种抗癌药。
The researchers reported their findings, "A small molecule based on the pRb2/p130 spacer domain leads to inhibition of cdk2 activity, cell cycle arrest and tumor growth reduction in vivo," in the March 22 issue of the journal Oncogene (http://www.nature.com/onc). Rb2/p130 was discovered in the early 1990s by Antonio Giordano, director of the Sbarro Institute (http://www.shro.org) and the Center for Biotechnology in 's College of Science and Technology, who headed the study.
在3月22号癌基因（Oncogene，http://www.nature.com/onc）杂志上研究者报告说，一种源于Rb2/p130间隔区的小分子在体内引起cdk2激酶活性的抑制和细胞周期停滞并抑制肿瘤生长。Rb2/p130是由Sbarro研究所(http://www.shro.org)和Temple科学技术学院生物技术中心主任Antonio Giordano在上个世纪90年代早期发现的。
The researchers discovered that within Rb2/p130's spacer domain--a sequence of 212 amino acids located in the pocket or middle section of the gene--was a small portion that resembled an amino-acidic sequence contained in the protein p21, which acts as a cdk (cyclin dependent kinase) inhibitor. Cdks play a critical role in cell cycle regulation.
研究者发现Rb2/p130间隔区即位于基因中部或“口袋部位” 的一段编码212个氨基酸的序列与p21蛋白（一种细胞周期依赖的蛋白激酶抑制剂，细胞周期依赖的蛋白激酶在细胞周期调节中起关键作用。）内的小部分序列相似。
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作者:admin@医学,生命科学 2011-01-18 17:14
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