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Proposal of Dual Inhibitor Targeting ATPase Domains of Topoisomerase II and. Heat Shock Protein 90

Title
Proposal of Dual Inhibitor Targeting ATPase Domains of Topoisomerase II and. Heat Shock Protein 90
Authors
Jun, Kyu-YeonKwon, Youngjoo
Ewha Authors
권영주
SCOPUS Author ID
권영주scopus
Issue Date
2016
Journal Title
BIOMOLECULES & THERAPEUTICS
ISSN
1976-9148JCR Link2005-4483JCR Link
Citation
vol. 24, no. 5, pp. 453 - 468
Keywords
Topoisomerase IIHeat shock protein 90Molecular docking studyDesign of dual inhibitor
Publisher
KOREAN SOC APPLIED PHARMACOLOGY
Indexed
SCIE; SCOPUS WOS scopus
Abstract
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.
DOI
10.4062/biomolther.2016.168
Appears in Collections:
약학대학 > 약학과 > Journal papers
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