Researchers at the University of California, Davis have developed novel proteins for the inhibition of IGF2 signaling without adversely affecting glucose metabolism.
The insulin receptor (IR) exists in two isoforms: the ‘B’ isoform (IR-B) which only binds to insulin and is a critical regulator of glucose metabolism, and the ‘A’ isoform (IR-A) which recognizes both insulin and insulin-like growth factor-2 (IGF2). Aberrant IGF2 has been implicated in many cancers, and binds insulin-like growth factor-1 receptor (IGF1R) in addition to IR-A. In cells with a high IR-A/IGF1R ratio, production of IGF2 stimulates unregulated cell growth.
IR-A is a therapeutic target in cancer, and efforts have been made to produce inhibitors of IGF2 signaling that selectively target IR-A, as inhibitors of IR-B are expected to adversely affect glucose metabolism. Unfortunately, currently available kinase inhibitors do not distinguish IGF1R, IR-A, and IR-B. Additionally, available anti-IGF1R antibodies do not block IR-A or IR-B.
Researchers at the University of California, Davis have developed novel proteins for inhibiting IGF2 signaling. These inhibitors modulate IGF1R and IR-A activity without affecting IR-B activity. These proteins are expected to serve as both drug discovery tools and therapeutic agents to aid in the treatment of a number of hyperproliferative and inflammatory diseases.
Patent Pending
IGF2, inhibitors, cancer, oncology, isoform, theraphy, drug discovery, autoimmune, hypervasularization, fibrosis