Innovation

Lysine-Spermine Conjugates: Hydrophobic Polyamine Amides As Potent Lipopolysaccharide Sequestrants

University of Kansas
posted on 01/12/2006

The invention is the use of lysine-spermine conjugates in the treatment of sepsis

Suggested Uses

Treatment of sepsis. Adjunctive treatment of microbial infections.

Innovation Details
 

Detailed Description

Lipopolysaccharides (LPS), otherwise termed 'endotoxins', are outer-membrane constituents of Gram-negative bacteria. Lipopolysaccharides play a key role in the pathogenesis of 'Septic Shock', a major cause of mortality in the critically ill patient. Therapeutic options aimed at limiting downstream systemic inflammatory processes by targeting lipopolysaccharide do not exist at the present time. We have defined the pharmacophore necessary for small molecules to specifically bind and neutralize LPS and, using animal models of sepsis, have shown that the sequestration of circulatory LPS by small molecules is a therapeutically viable strategy. In this invention, the interactions of a focused library of lysine-spermine conjugates with lipopolysaccharide (LPS) have been characterized. Lysine-spermine conjugates with the alpha-amino terminus of the lysinyl moiety derivatized with long-chain aliphatic hydrophobic substituents in acyl or alkyl linkage bind and neutralize bacterial lipopolysaccharides, and may be of use in the prevention or treatment of endotoxic shock states.

File Number: KUCR # 2005 FY 11 

Other Information: *State of Development* Available for license.


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