Ontology highlight
ABSTRACT:
SUBMITTER: Matsuno K
PROVIDER: S-EPMC4007973 | biostudies-literature | 2010 Nov
REPOSITORIES: biostudies-literature
Matsuno Kenji K Masuda Yoshiaki Y Uehara Yutaka Y Sato Hiroshi H Muroya Ayumu A Takahashi Osamu O Yokotagawa Takane T Furuya Toshio T Okawara Tadashi T Otsuka Masami M Ogo Naohisa N Ashizawa Tadashi T Oshita Chie C Tai Sachiko S Ishii Hidee H Akiyama Yasuto Y Asai Akira A
ACS medicinal chemistry letters 20100713 8
The signal transducer and activator of transcription 3 (STAT3) is considered to be an attractive therapeutic target for oncology drug development. We identified a N-[2-(1,3,4-oxadiazolyl)]-4-quinolinecarboxamide derivative, STX-0119, as a novel STAT3 dimerization inhibitor by a virtual screen using a customized version of the DOCK4 program with the crystal structure of STAT3. In addition, we used in vitro cell-based assays such as the luciferase reporter gene assay and the fluorescence resonance ...[more]