FS23 binds to the N-terminal domain of human Hsp90: A novel small inhibitor for Hsp90

分类： 物理学 >> 核物理学 提交时间： 2023-06-18 合作期刊: 《Nuclear Science and Techniques》

LI Jian SHI Feng CHEN Dan-Qi CAO Hui-Ling XIONG Bing SHEN Jing-Kang HE Jian-Hua

摘要： The N-terminal domain of heat shock protein 90 (Hsp90N) is responsible for the catalytic activity of Hsp90. The reported inhibitors of Hsp90 bind to this domain and would inhibit tumor growth and progression. Here, we synthesized FS23, a small molecule inhibitor of hsp90 and collected X-ray diffraction data of the complex crystal of Hsp90-FS23. High resolution X-ray crystallography shows that FS23 interacted with Hsp90N at the nucleotide binding cleft, and this suggests that FS23 may complete with nucleotides to bind to Hsp90N. The crystal structure and the interaction between Hsp90N and FS23 suggest a rational basis for the design of novel antitumor drugs.

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