US Patent:
20130039854, Feb 14, 2013
Inventors:
Jean C. SHIH - Beverly Hills CA, US
Leland CHUNG - Los Angeles CA, US
Haiyen E. ZHAU - Los Angeles CA, US
Boyang Jason WU - Los Angeles CA, US
Bogdan Z. OLENYUK - Sierra Madre CA, US
Assignee:
UNIVERSITY OF SOUTHERN CALIFORNIA - Los Angeles CA
International Classification:
A61K 31/405
C07D 319/18
C07D 311/36
C07D 311/54
A61K 31/381
A61K 31/357
A61K 31/352
A61K 31/366
A61K 31/7088
A61K 31/713
A61K 31/404
C07D 209/14
C07D 409/14
C12N 9/99
C12Q 1/26
A61K 49/00
G01N 33/574
C12Q 1/68
A61P 35/00
C07D 333/28
US Classification:
424 91, 549 78, 549362, 549403, 549285, 514438, 514452, 514456, 514414, 514 44 A, 548455, 435184, 435 25, 435 74, 435 612
Abstract:
A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.