Product name
Small Molecule XIAP Inhibitor from Bavarian Patent AllianceSummary
Inhibitors increase etoposide-induced apoptosis fivefoldOrganization name
Bayerische Patentallianz GmbHProfile
Challenge
Apoptosis is a highly conserved process regulating the balance between cell death and proliferation for the maintenance of tissue homeostasis. Insufficient apoptosis can lead to the development and progression of cancer. Most chemotherapeutic drugs kill cancer cells by inducing apoptosis. Importantly, tumour cells which are capable of evading programmed cell death often become chemoresistant.
Inhibitor of apoptosis proteins (IAPs) are a group of antiapoptotic proteins that inhibit caspases, central players in the apoptotic cascade. XIAP, the most potent and well characterized member of the IAP family is an inhibitor of caspase-3, -7 and -9. Many human malignancies express elevated XIAP-levels thus leading to apoptosis resistance. Therefore, targeting XIAP is a promising strategy to overcome apoptosis resistance. In this context, small molecule XIAP inhibitors are attractive antitumor drug candidates.
Technology
Through virtual screening of commercially available databases several compounds were identified as novel XIAP inhibitors. These compounds, which showed no cytotoxicity on their own, were tested in a human leukaemia cell line stably overexpressing XIAP for their ability to overcome the cells’ chemoresistance.
The most effective molecules increased apoptosis-induction through the chemotherapeutic drug etoposide from approximately 10% to above 60% apoptotic cells. In order to develop the full therapeutic potential of our XIAP inhibitors, we currently work on the underlying apoptosis signalling mechanisms, NMR binding studies, and towards an in vivo proof of principle.
Commercial Opportunity
On behalf of the LMU the Bayerische Patentallianz GmbH offers an exclusive, worldwide patent license or the option in combination with a cooperation contract.
Developmental Status
In vitro
Patent Situation
Priority Year: 2007 EP
Contact
Bayerische Patentallianz GmbH
Dr. Ulrich Genschel
genschel(at)bayerischepatentallianz.de
About Bayerische Patentallianz
The Bavarian patent alliance supports scientists from Bavarian universities in the identification and evaluation of commercially interesting inventions and in the application and maintenance of patents. For industry partners, they offer an interesting portfolio of property rights and legal protection applications, and thus a source of new products and processes.
Description File
Small_Molecule_XIAP_Inhibitor__B64017_.pdf
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