Proposal of Dual Inhibitor Targeting ATPase Domains of Topoisomerase II and. Heat Shock Protein 90
- 주제(키워드) Topoisomerase II , Heat shock protein 90 , Molecular docking study , Design of dual inhibitor
- 등재 SCIE, SCOPUS
- 발행기관 KOREAN SOC APPLIED PHARMACOLOGY
- 발행년도 2016
- 총서유형 Journal
- URI http://www.dcollection.net/handler/ewha/000000140115
- 본문언어 영어
- Published As http://dx.doi.org/10.4062/biomolther.2016.168
초록/요약
There is a conserved ATPase domain in topoisomerase II (topo II) and heat shock protein 90 (Hsp90) which belong to the GHKL (gyrase, Hsp90, histidine kinase, and MutL) family. The inhibitors that target each of topo II and Hsp90 are intensively studied as anti-cancer drugs since they play very important roles in cell proliferation and survival. Therefore the development of dual targeting anti-cancer drugs for topo II and Hsp90 is suggested to be a promising area. The topo II and Hsp90 inhibitors, known to bind to their ATP binding site, were searched. All the inhibitors investigated were docked to both topo II and Hsp90. Four candidate compounds as possible dual inhibitors were selected by analyzing the molecular docking study. The pharmacophore model of dual inhibitors for topo II and Hsp90 were generated and the design of novel dual inhibitor was proposed.
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