New enzyme inhibitor may lead to drug against cancer

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Washington, May 16 : Scientists at The Wistar Institute have developed a new type of enzyme inhibitor that can deactivate proteins called phosphatidyl-inositol-3-kinases (PI3Ks), which are crucial to cancer development.

The researchers have revealed that they created the new inhibitor 'E5' by combining natural organic atoms with the metal Ruthenium.

They tested the effectiveness of E5 using cell cultures of melanoma, a type of skin cancer.

Dr. Ronen Marmorstein, a professor in the Gene Expression and Regulation Program at the institute, said that melanoma was used as a model system for the study because the signalling pathway regulated by PI3K is highly mutated in melanoma.

He said that the study showed the new agent to be effective in inhibiting the growth of cells.

Further studies in three-dimensional cultures of melanoma cells showed the agent also prevented melanoma cell invasion, he added.

According to him, these findings indicate that small-molecule inhibitors can be designed to target a biochemical pathway that plays a key role in cancer development.

Marmorstein has revealed that the PI3K family of kinases includes four types-alpha, beta, delta and gamma-each of which is associated with particular biological pathways and performs various functions in the cell.

Some of the PI3K types are associated with cancer, while others are not.

The trick to building inhibitors with low side effects and toxicity is to create inhibitors that knock out the troublesome isoforms without disrupting the other types, Marmorstein says.

The study has been published in the journal ACS Chemical Biology.

ANI

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