Girish Mahajan (Editor)

Cysmethynil

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Cysmethynil

Cysmethynil is a compound that was reported to be responsible for the uninhibited cell growth, one of the main characteristics of cancer. Since it is a recently discovered compound, there are still animal experiments taking place to prove its efficiency. Researchers are trying to see if they can use this compound as an anti-cancer drug and since many cancers share the same characteristics, the drug would be able to help treat different types of cancers. It is a substituted indole with toluene, a tertiary amine, and a primary amide substituents. The structure has three hydrogen bond acceptors.

Reactions/Uses

Cysmethynil reacts to inhibit Icmt, which plays in key role for the Ras protein. Ras is one of the components in the cell that is responsible for controlling cell growth. Certain mutations in Ras can leave it in the "on" configuration, such that uncontrolled cell growth results. Ras gets methylated by the Icmt enzyme, a signal that allows Ras to go to its destination (plasma membrane) that can lead to uncontrolled growth. Icmt can be inhibited from adding the methyl group, inactivating Ras such that it no longer sends a signal to the cell to have uncontrolled growth. Cysmethynil is the compound that knocks out Icmt so that it can no longer function, and this in turn prevents Ras from signaling the cell. The compound was tested out in xenograft mice that had multiple human tumors, and the result was reduced tumor burden. Treatment from this compound causes autophagy in the cell and results in cell death. Research done on prostate cancer cells has demonstrated that cysmethynil inhibits Icmt such that the cell is stuck in the G1 phase, and this leads to the autophagic cell death.

References

Cysmethynil Wikipedia