Description:
Novel Compounds and Methods of Use for
the Treatment and Prevention of Cancer via Inhibition of the K-Ras Pathway
Background:
The Ras protein family members belong to a class of proteins called small GTPases and when activated by incoming signals, it subsequently switches on other genes involved in cell growth, differentiation, and survival. As a result, mutations in the ras genes can lead to production of permanently activated Ras proteins and ultimately lead to cancer. Localization of K-ras to the plasma membrane is required for the activation of downstream effector pathways. Fendiline hydrochloride has been identified as a specific inhibitor of plasma membrane localization of K-Ras. Therefore, Fendiline and Fendiline derivatives may potentially have utility as K-Ras-specific anticancer therapeutics.
Market:
Mutations that permanently activate Ras are found in 20-25% of all human tumors and up to 90% in certain types of cancer, such as pancreatic cancer. The broad indications place a tremendous demand and market for novel compounds and methods to treat and prevent cancer by inhibition of the Ras pathway.
Technology Highlights:
Scientists at The University of Texas Health Science Center at Houston (UTHealth) have identified novel compounds, including derivatives of Fendiline, methods for their manufacture, and methods for their use, including for the treatment and prevention of cancer or other diseases. This technology:
· Describes novel compounds, including Fendiline derivatives, for the inhibition of K-Ras localization to the plasma membrane;
· Such novel compounds may be used for inhibiting the signal transduction from oncogenic K-Ras;
· Provides potential treatment methods based on these compounds, which may be used as therapies for cancer, such as leukemia, colorectal cancer, pancreatic cancer, and lung cancer; and
· Current compounds are selectively toxic to K-Ras transformed pancreatic, endometrial, colorectal and lung tumor cell lines. Mouse studies with human pancreatic and endometrial tumors are planned and/or are in progress.
IP Status:
PCT application filed.
License Available:
World-wide; exclusive or non-exclusive
Researchers:
Drs. John F. Hancock and Dharini van der Hoeven