Dimeric small molecule potentiators of apoptosis

US7638544B2 · kind B2 · utility

Assignee

• The Board of Regents of the University of Texas System · US

Inventors

• Patrick G. Harran · Dallas, US
• Xiaodong Wang · Zhejiang, CN
• Jef K. De Brabander · Dallas, US
• Lin Li · 安丰镇, CN
• Ranny Mathew Thomas · Dallas, US
• Hidetaka Suzuki · Dallas, US

Key dates

• Filing date: Dec 17, 2007
• Grant date: Dec 29, 2009
• Expiry date: Dec 17, 2027

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K5/06034
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of the dimeric mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.