Ontology highlight
ABSTRACT:
SUBMITTER: Miklossy G
PROVIDER: S-EPMC4834983 | biostudies-literature | 2015 Oct
REPOSITORIES: biostudies-literature
Miklossy Gabriella G Youn Ui Joung UJ Yue Peibin P Zhang Mingming M Chen Chih-Hong CH Hilliard Tyvette S TS Paladino David D Li Yifei Y Choi Justin J Sarkaria Jann N JN Kawakami Joel K JK Wongwiwatthananukit Supakit S Chen Yuan Y Sun Dianqing D Chang Leng Chee LC Turkson James J
Journal of medicinal chemistry 20150917 19
We report that hirsutinolide series, 6, 7, 10, 11, 20, and 22, and the semisynthetic analogues, 30, 31, 33, and 36, inhibit constitutively active signal transducer and activator of transcription (Stat)3 and malignant glioma phenotype. A position 13 lipophilic ester group is required for activity. Molecular modeling and nuclear magnetic resonance structural analyses reveal direct hirsutinolide:Stat3 binding. One-hour treatment of cells with 6 and 22 also upregulated importin subunit α-2 levels an ...[more]