Compositions and methods for the treatment of hepatitis C virus infection

Reference Number: K 01-30

Inventors: Todd, Scott C.; Baures, Paul W.

Owner: Kansas State University Research Foundation

USPTO Link: 7208628

Invention Summary

Current therapy for Hepatitis C virus (HCV) infection involves the use of general immune modulator, a-interferon, in combination with ribavirin. There therapy has limited efficacy. New small molecule therapeutics for the treatment of HCV infection are needed. The interaction of human CD81 (the cellular receptor for HCV-E2) protein and the HCV envelope protein (E2) is believed to be important in the infectivity of HCV. Additionally, binding of HCV-E2 to CD81 on T cells alters the T cell function which may enable HCV to manipulate or evade immune response and persist in the patient for many years.

Advantages

• Several small molecules synthesized at Kansas State University have been found to block binding of HCV-E2 to CD81 on human cell lines

• These novel molecules may act as peptidomimetics of CD81 to disrupt interactions between HCV-E2 and CD81, thereby inhibiting binding of the virus to the cellular receptor

• The best inhibitor to date has an approximate IC 50 value 45mM in the in vitro assay

• It is expected that further variation of this structure will improve its affinity and solubility characteristics

• The scaffolds used for the development of the compounds are relatively simple to prepare, have predictable conformations and are amphiphilic in order to aid solubility in both water and cell membranes

• An additional application of the invention is the use of these scaffolds as a general proteomimetic scaffold for studying other protein-protein interactions