Dimeric small molecule potentiators of apoptosis

USRE46129E1 · kind E1 · reissue

Assignee

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

Inventors

• Patrick G. Harran · Dallas, US
• Xiaodong Wang · Zhejiang, CN
• Jef DeBrabander · Flower Mound, US
• Lin Li · 安丰镇, CN
• Ranny Mathew Thomas · Dallas, US
• Hidetaka Suzuki · Dallas, US

Key dates

• Filing date: Jan 10, 2014
• Grant date: Aug 30, 2016
• Expiry date: Jan 10, 2034

Classification

• Technology area (CPC —): General

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 compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.