Synthetic Analogs of Juxtamembrane Domain of IGF-1 Receptor as Anti-Cancer Agents
Description of Invention:
Insulin-like growth factor receptor type one (IGF-1R), part of the receptor tyrosine kinase (RTKs) family, is integral to cancer cell growth and metastasis. Juxtamembrane domains (JM) of RTKs are located in the cytoplasm between the transmembrane and kinase domains. JMs play a crucial role in the inhibition of the regulation of receptor activity. Studies on other small molecules tyrosine kinase inhibitors (TKIs) indicate non-specific binding with the insulin receptor which has high homology with IGF-1R.
The current invention describes synthetic analogs of IGF-1R JM which were found to be potent inhibitors of IGF-1-mediated cell signaling and cancer cell growth. These analogs provide more binding specificity with less likelihood of significant toxic effects.
Applications and Modality:
New inhibitors can be used to treat many types of tumors.
IGR-1R inhibition may be useful as an anti-aging agent.
IGR-1R plays an inhibitory role in regulation of skin development and differentiation. IGF-1R inhibitors may have revitalizing and rejuvenating effect on skin and may stimulate wound healing.
Market:
An estimated 1,444,920 new cancer diagnoses in the U.S. in 2007.
600,000 deaths caused by cancer in the U.S. in 2006.
Cancer is the second leading cause of death in the U.S.
Cancer drug market will likely double to $50 billion in 2010 from $25 billion in 2006.
Development Status:
The technology is currently in the preclinical stage of development.