Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
Basic Information
ID: ALA1141505
Journal: Bioorg Med Chem Lett
Title: Conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin, for Hsp90 inhibitory activity.
Authors: Onodera H, Kaneko M, Takahashi Y, Uochi Y, Funahashi J, Nakashima T, Soga S, Suzuki M, Ikeda S, Yamashita Y, Rahayu ES, Kanda Y, Ichimura M.
Abstract: Hsp90 is an attractive chemotherapeutic target because it is essential to maturation of multiple oncogenes. We describe the conformational significance of EH21A1-A4, phenolic derivatives of geldanamycin isolated from Streptomyces sp. Their native free structures are similar to the active form of geldanamycin bound to Hsp90 protein. Their conformational character is a probable reason for their high-affinity binding. Lack of toxic benzoquinone in EH21A1-A4 also adds to their potential as lead compounds for anti-tumor drugs.
CiteXplore: 18243703
DOI: 10.1016/j.bmcl.2008.01.072
Patent ID: ┄