The University of Texas System

Genelabs Technologies, Inc.

Yan Kwok

Kirk E Fry

Laurence H Hurley

Thomas W Bruice

Sean Michael Kerwin

Albert W Tam

Cynthia A Edwards

Qingping Zeng

Megan E Laurance

Douglas B Starr

Moon Young Lim

Jongsik Gam

The present invention provides molecular switch system methods and compositions for use in regulatable gene expression. The system includes a nucleic acid construct which has a DNA response sequence for a transcriptional regulatory protein operably linked to a promoter, a compound binding sequence in the vicinity of the DNA response sequence, a transgene under the control of the promoter; and a DNA binding compound. In some cases, the molecular switch system further includes a nucleic acid sequence encoding a transcriptional regulatory protein operably linked to a second promoter. The invention further provides a method for screening compounds for the ability to function in the molecular switch system and thereby regulate gene expression.

DNA binding compound-mediated molecular switch system

The present invention discloses a novel quinobenzoxazine self-assembly complex on DNA and on the topoisomerase II-DNA complex. The related model is used to design a new series of quinobenzoxazines, pyridobenzophenoxazines, pyrridonaphthophenoxazines, and other related compounds that may exhibit anticancer or antibiotic activity. The anticancer activity of these compounds is thought to operate via stabilization of the topoisomerase II-DNA complex and/or interaction with G-quadruplexes, while the antibiotic activity of these compounds derives from their ability to inhibit gyrase, the bacterial type II topoisomerase.

Synthesis of quinobenzoxazine analogues with topoisomerase II and quadruplex interactions for use as antineoplastic agents

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Sunnyvale, CA, United States of America

Yan Kwok