(c) flickr & Matthew Crowley Photography
急速に増殖する癌細胞を死滅させる，革新的な方法が考案された。この方法を開発した研究班は，RAFという酵素の構造を変える薬剤を研究していたところ，RAFが増殖性の腫瘍の成長に重要であることを発見した。そして，RAFの形を変える薬剤が実際に腫瘍細胞を死滅させることを，動物実験やヒトの癌の組織を用いた実験で示した。RAFのような酵素を標的とする抗癌剤は既にあり，一般に酵素の活性部位に作用するが，この機序により標的酵素以外への望ましくない作用や耐性が生じる。新たな方法はRAFのみを標的にでき，耐性の可能性も低いという。（吉田素子）
New Way to Target -- And Kill -- Proliferating Tumors
UC San Diego researchers find surprising role for enzyme in tumor cell division and new drug to combat it
Researchers at the University of California, San Diego School of Medicine and the UC San Diego Moores Cancer Center have identified a new drug discovery approach enabling the destruction of the most highly proliferative tumors. The discovery, published in the November 13 online issue of the journal Nature Medicine, points to an effective, alternative method for killing fast-growing cancer cells without causing some of the negative effects of current therapies.
The scientists, led by David A. Cheresh, PhD, professor of pathology and associate director for translational research at the Moores Cancer Center, used an innovative chemical and biological approach to design a new class of drugs that arrests division in virtually all tumor cells by binding to and altering the structure of an enzyme called RAF.
RAF has been long-studied, but its role in cell division -- critical to cell proliferation and tumor growth -- was a surprise. “By designing a new class of drugs that changes the shape of RAF, we were able to reveal this previously undiscovered role for RAF in a wide range of highly proliferative tumors,” Cheresh said.
Current cancer drugs that target enzymes like RAF are generally designed to interact with the active site of the enzyme. Unfortunately, these drugs often lack specificity, Cheresh said. “They hit many different targets, meaning they can produce undesired side effects and induce dose-limiting toxicity.”
［単語和訳］
Proliferating：増殖している Tumors：腫瘍
researchers：研究者 enzyme：酵素 cell division：細胞分裂 combat：～と戦う
Cancer：癌 proliferative：増殖性の online：オンラインの points to：～を提示する fast-growing：増殖の速い therapies：治療
PhD：博士 pathology：病理学 translational research：トランスレーショナル・リサーチ innovative：革新的な biological：生物学的 virtually：実質的に arrests：停止させる
undiscovered：発見されていない a wide range of：広範囲の
interact with：～と相互作用する active site：活性部位 specificity：特異性 undesired：望ましくない side effects：副作用 induce：～を誘発する dose-limiting toxicity：用量制限毒性
