线性聚酰胺以非寻常的 1:1 模式结合抑制热休克转录因子结合。
Inhibition of heat shock transcription factor binding by a linear polyamide binding in an unusual 1:1 mode.
机构信息
Department of Chemistry, Washington University, St. Louis, MO 63130, USA.
出版信息
Chembiochem. 2012 Jan 2;13(1):97-104. doi: 10.1002/cbic.201100524. Epub 2011 Dec 1.
Abstract
Heat shock proteins (HSPs) are known to protect cells from heat, oxidative stress, and the cytotoxic effects of drugs, and thus can enhance cancer cell survival. As a result, HSPs are a newly emerging class of protein targets for chemotherapy. Among the various HSPs, the HSP70 family is the most highly conserved and prevalent. Herein we describe the development of a β-alanine rich linear polyamide that binds the GGA heat shock elements (HSEs) 3 and 4 in the HSP70 promoter in an unusual 1:1 mode and inhibits heat shock transcription factor 1 (HSF1) binding in vitro.
摘要
热休克蛋白（HSPs）已知可保护细胞免受热、氧化应激和药物的细胞毒性作用，从而增强癌细胞的存活能力。因此，HSPs 是化疗的一个新兴的蛋白质靶标类别。在各种 HSPs 中，HSP70 家族是最保守和普遍的。本文描述了一种富含β-丙氨酸的线性聚酰胺的开发，该聚酰胺以不寻常的 1:1 模式结合 HSP70 启动子中的 GGA 热休克元件（HSEs）3 和 4，并抑制体外热休克转录因子 1（HSF1）结合。
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