Related Experiment Videos
Current progress on farnesyl protein transferase inhibitors
Sheo B Singh1, Russell B Lingham
1Merck & Co Inc, PO Box 2000, Building RY80Y-355, Rahway, NJ 07065, USA. sheo_singh@merck.com
Current Opinion in Drug Discovery & Development
|April 3, 2002
Summary
Inhibiting farnesyl protein transferase (FPTase) shows promise for cancer treatment. While some FPTase inhibitors advance in clinical trials, many candidates have faced challenges, necessitating further research.
Area of Science:
- Oncology
- Biochemistry
- Drug Discovery
Background:
- Farnesyl protein transferase (FPTase) inhibition is a therapeutic strategy for cancer.
- A decade of preclinical research has yielded several FPTase inhibitors for clinical testing.
Purpose of the Study:
- To review clinical and preclinical data of FPTase inhibitors published in 2001.
- To discuss natural product inhibitors reported between 1998-2001.
- To summarize the historical development of FPTase inhibitors at Merck.
Main Methods:
- Literature review of clinical and preclinical data.
- Analysis of published studies on FPTase inhibitors.
- Historical account of drug discovery efforts.
Main Results:
- Several FPTase inhibitors are in Phase I, II, or III clinical trials.
- BMS-214662, R-115777, and Sch-66336 are the most advanced compounds.
- Initial results for advanced compounds are encouraging, but many candidates show limited clinical efficacy.
Conclusions:
- FPTase inhibition remains a key area in cancer drug development.
- Further research is needed to overcome challenges with FPTase inhibitor efficacy.
- Diverse chemical strategies, from small molecules to macrocycles, are being explored.