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KDDF-201312-06 Development of cancer therapeutics targeting mitochondrial TRAP1(Oncology, Chemical) [04.01.2014]

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Development and Market Objectives

To identify a lead compound from mitochondria-targeted TRAP1 inhibitors with a drug delivery mechanism.

Unmet Medical Need & Target Patients

Target patients:
Cancer patients with malignancies exhibiting a TRAP1 overexpression phenotype

Unmet medical needs:
-       Despite increases in cancer incidence due to an aging population, the development of effective anti-cancer drugs remains elusive
-       Anti-cancer drugs with noble mechanism of action are required for the treatment of patients who do not respond to conventional anticancer therapeutics and to overcomedrug resistance to conventional chemotherapy.
-       Novel therapeutics are required for combination treatment with conventional anticancer drugs.

Status

The inhibitor development program has been initiated lately and analysis protocols to examine target protein inhibition and action mechanism-of drugshave been established. In addition, high-resolution protein 3D structural informationhas been obtained from the inhibitor-TRAP1 co-crystals.
Design and synthesis of TRAP1 inhibitors are currently progressing in order to select a lead compound with outstanding safety and efficacy parameters.

Intellectual Property

Patents have already been filed for a first-in-class mitochondria-targeted TRAP1 inhibitor showing anticancer activities in vitro and in vivo. Ourdrug development program aims for not only an effective cancer drug but also a patentable drug that does not infringe any existing intellectual property 

Competitive Advantages

- First-in-class cancer drug development with novel mechanism of action delivering inhibitory compounds to the organelle
- Structure-based drug design, using high resolution protein crystal structures ofhuman TRAP1 protein complexed with its inhibitors
- A novel approach to increase drug efficacy by, incorporating both the target inhibitory moiety and drug delivery system to the relevant organelle.
- Drug combination with various  anti-cancer drugs currently used in clinic could synergistically enhance their therapeutic potential.

Indication

Cancer

Research Period

Feb, 2014 ~ Sep, 2015

Company

Ulsan National Institute of Science and Technology

Developmental Stage

Lead Generation

Additional Information

Contact Information

Contact
Address Company Name: Cancer Biology Laboratory, Department of Biological Sciences, UNIST.
WebSite Homepage: http://https://sites.google.com/site/mitomed/home Contact Person: Lee, Ji Eun
E-mail: peaceful@unist.ac.kr Contact: 82-52-217-2588

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