Thomas G Rowe

US Patent:

8623854, Jan 7, 2014

Filed:

Jun 13, 2011

Appl. No.:

13/159016

Inventors:

Daniel M. Sullivan - Tampa FL, US
Joel G. Turner - Tampa FL, US
Thomas C. Rowe - Gainesville FL, US
David A. Ostrov - Gainesville FL, US

Assignee:

H. Lee Moffitt Cancer Center and Research Institute, Inc. - Tampa FL
University of Florida Research Foundation, Inc. - Gainesville FL

International Classification:

A01N 43/00
A61K 31/33
A01N 57/00
A61K 31/66
A01N 43/66
A61K 31/53
A01N 43/50
A61K 31/415

US Classification:

514183, 514124, 514244, 514245, 514401

Abstract:

A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase IIα and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo IIα have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.