Inhibitors of Fatty Acid Synthase for Prostate Cancer
Abstract
Fatty acid synthase (FASN), the enzyme that synthesizes fatty acid in cells, is over-expressed in prostate cancer and a potential therapeutic target. We have identified several novel chemical scaffolds with potential to inhibit FASN. An extensive series of anti-FASN pharmacophores has been synthesized and characterized for their ability to inhibit recombinant FASN, FASN activity in tumor cells, and to kill prostate cancer cell lines. The best inhibitors have increased potency over other FASN inhibitors, including orlistat, the prototype FASN thioesterase inhibitor. The current studies represent a significant advancement of the development of FASN inhibitors and moves a step closer to translating FASN inhibitors into the clinic.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 31, 2010
- Accession Number
- ADA540961
Entities
People
- Steven J. Kridel
Organizations
- Wake Forest University