Product name
Piperidone derivatives strongly inhibiting HIV replicationSummary
New substances specifically inhibit deoxyhypusine hydroxylase involved in HIV and HTLV replication and show in vitro activity in CML and trypanosomiasisOrganization name
Ascenion GmbHProfile
Challenge
An estimated 39.5 million people are living with HIV, the retrovirus causing AIDS, and 2.9 million people died of AIDS-related illnesses in 2006 (source: WHO). Current antiretroviral therapies primarily rely on virus enzyme inhibitors and molecules that inhibit virus-cell fusion. The Highly Active Anti-Retroviral Therapy (HAART) is based on a combination of these different drug classes. Although HAART significantly improved morbidity and mortality of HIV-patients, long-term treatment often is accompanied by severe side effects in patients and development of highly resistant HIVstrains. Therefore novel therapy options, especially for patients with multiple HAART-resistant HIV strains have to be developed.
Technology
An alternative target for antiretroviral therapy is the biosynthesis of the eukaryotic initiation factor 5A (eIF-5A). eIF-5A is an essential cofactor of the HIV regulatory protein Rev and the HTLV protein Rex which are important for replication of the respective retroviruses. The biological activity of eIF-5A depends on a posttranslational modification of a single specific lysine that is transformed into the unusual amino acid hypusine. The formation of hypusine is a two-step process involving the enzyme deoxyhypusine hydroxylase (DOHH). The inventors synthesized new substances that specifically target DOHH and that have very low cytotoxic effects. The inventors were able to show that these DOHH-inhibitors strongly inhibit virus replication.
Commercial Opportunity
These new substances can be developed as new active agents for the treatment of HIV-1 and HTLV infections. The technology is offered for co-development or licensing. Developmental Status So far, DOHH via the new substances have been shown to have beneficial effects in vitro data are available. Additional therapeutic fields in which inhibition ofin vitro is the treatment of Chronic Myeloid Leukemia (CML) and trypanosomiasis.
Patent Situation
A priority establishing European patent application was filed in 2007.
Contact
Ascenion
Dr. Hinrich Habeck
habeck(at)ascenion.de
About Ascenion
Ascenion is the exclusive partner of 12 life-science institutes in the Helmholtz and Leibniz Associations and of one Medical School, and coordinates technology transfer for the German National Genome Research Network. They currently market around 600 technologies, together with a varied range of research materials, e.g. antibodies, animal models and vectors.
Description File
Piperidone_derivatives_for_treatment_of_HIV_and_HTLV_infections_and_of_Chro...
print this page
