These analogs were found to be potent inhibitors of IGF-1-mediated cell signaling and cancer cell growth, providing more binding specificity with less likelihood of significant toxic effects.

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:

 

Preclinical

U.S. Provisional Application No. 61,040,203 filed 28 Mar 2008 (HHS Reference No. E-129-2008/0-US-01)

 

Inventors:

Nadya I. Tarasova and Sergey G. Tarasov (NCI)

 

 

Licensees Sought:

Available for exclusive and non-exclusive licensing.