Farnesyltransferase inhibitor

Farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the intention of preventing its action. Farnesyltransferase is an enzyme that plays a key role in cell signaling, and its dysregulation has been implicated in the development of several types of cancer.

Mechanism of Action

Farnesyltransferase inhibitors work by blocking the action of the enzyme protein farnesyltransferase. This enzyme is responsible for the post-translational modification of a variety of proteins through a process known as prenylation. Prenylation involves the addition of a farnesyl group to the protein, which allows it to anchor to cell membranes and participate in cell signaling processes.

In many cancers, certain proteins are overactive or present in excessive amounts, leading to uncontrolled cell growth and division. By inhibiting farnesyltransferase, these drugs aim to prevent the prenylation and subsequent activation of these proteins, thereby halting the growth of cancer cells.

Clinical Use

Farnesyltransferase inhibitors are currently in the experimental stages of development and have not yet been approved for use in humans. However, they have shown promise in preclinical trials for the treatment of a variety of cancers, including lung cancer, breast cancer, and pancreatic cancer.

Potential Side Effects

As with all drugs, farnesyltransferase inhibitors have the potential to cause side effects. These may include nausea, vomiting, diarrhea, and fatigue. More serious side effects may include liver damage and blood clotting disorders.

Future Directions

Research is ongoing to further understand the role of farnesyltransferase in cancer and to develop more effective and selective inhibitors of this enzyme. It is hoped that these drugs may eventually provide a new approach to cancer treatment, particularly for cancers that are currently resistant to other forms of therapy.

See Also

• Protein prenylation
• Cancer drug discovery and development
• Enzyme inhibitor

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