New Cancer Drug Targets Lipid Chemical Messengers

Researchers have created a new cancer drug that targets lipid chemical messengers. As it stands, more than half of human cancers have abnormally unregulated chemical signals related to lipid metabolism that are controlled during tumor formation. However, many health officials still are not completely certain how they function.

In these findings, researchers at the Laboratory Medicine of the Perelman School of Medicine, University of Pennsylvania, describe a newly discovered oncogenic protein that promotes cancer by targeting pathways.

"Lipid second messengers play cardinal roles in relaying and amplifying signals from outside the cell to its interior and outer membrane. One of the best known lipid second messengers is PIP3, which relays signals from hundreds of membrane receptors, including many oncogenic receptors, on the cell surface to PIP3-binding proteins in the cell's interior, which control cell growth, differentiation, migration, transformation, and death," the researchers note, in a new release. 

Researchers noted that drugs targeting PIP3 may be effective for treating a variety of diseases, including cancer and certain inflammatory disorders. TIPE3 belongs to a newly described family of proteins and is a risk factor for the aforementioned issues, though its mechanisms are still relatively unknown.

TIPE3 is the transfer protein of the second messenger PIP3 and it is hijacked by cancer cells to cause runaway cell division.

The high-resolution crystal structure of TIPE3 shows a large cavity that captures and transfers PIP3 and its chemical precursor PIP2 to increase their presence on the inner membrane of the cell. This promotes activation of downstream PIP3 effectors that cause cancer.

"These findings explain why normal cells can control their lipid signals but cancer cells can't, a phenomenon widely recognized, but poorly understood," researchers concluded. "Therefore, TIPE3 may represent a new therapeutic target for treating malignant diseases."

More information regarding the findings can be seen via the journal Cancer Cell.