US Patent:
20050080102, Apr 14, 2005
Inventors:
Saul Rosenberg - Grayslake IL, US
Shi Ng - Libertyville IL, US
James Kofron - Bristol WI, US
Haichao Zhang - Lake Bluff IL, US
Xuejun Jiang - New York NY, US
Xiaodong Wang - Dallas TX, US
International Classification:
A61K031/44
C07D213/28
G01N033/574
US Classification:
514277000, 546339000, 435007230
Abstract:
The subject invention relates to a novel small molecule, referred to as alpha-(trichloromethyl)-4-Pyridineethanol (PETCM), as well as to uses thereof. PETCM was identified and isolated by high throughput screening and is an activator of caspase-3. Using PETCM in combination with biochemical fractionation, a novel pathway that regulates mitochondria-initiated caspase activation was also identified. This pathway comprises tumor suppressor PHAP proteins and oncoprotein prothymosin-alpha. PETCM relieves prothymosin-alpha inhibition and allows apoptosome to form at a physiological concentration of dATP.