蛋白酶体19S调节颗粒的类肽抑制剂的鉴定。
Identification of a peptoid inhibitor of the proteasome 19S regulatory particle.
作者信息
Lim Hyun-Suk, Archer Chase T, Kodadek Thomas
机构信息
Division of Translational Research, Department of Internal Medicine, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, Texas 75390-9185, USA.
出版信息
J Am Chem Soc. 2007 Jun 27;129(25):7750-1. doi: 10.1021/ja072027p. Epub 2007 May 31.
Abstract
The first chemical inhibitor of the 19S Regulatory Particle (RP) of the proteasome is described. The molecule was identified by screening a library of nucleoside-capped peptoids for binding to the yeast 26S proteasome in a crude extract. The hit was resynthesized and shown to block 19S RP-mediated protein unfolding in vitro and proteasome-mediated turnover of p27 in HeLa cells.
摘要
本文描述了蛋白酶体19S调节颗粒（RP）的首个化学抑制剂。该分子是通过筛选核苷封端的类肽文库，以寻找能与粗提物中的酵母26S蛋白酶体结合的物质而鉴定出来的。对筛选出的活性物质进行了重新合成，并证明其在体外可阻断19S RP介导的蛋白质解折叠，在HeLa细胞中可阻断蛋白酶体介导的p27周转。
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