Accession Number : ADA540961


Title :   Inhibitors of Fatty Acid Synthase for Prostate Cancer


Descriptive Note : Annual rept. 1 May 2009-30 Apr 2010


Corporate Author : WAKE FOREST UNIV WINSTON-SALEM NC SCHOOL OF HEALTH SCIENCES


Personal Author(s) : Kridel, Steven J


Full Text : https://apps.dtic.mil/dtic/tr/fulltext/u2/a540961.pdf


Report Date : 31 May 2010


Pagination or Media Count : 44


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.


Descriptors :   *DRUGS , *PROSTATE CANCER , *FATTY ACIDS , *SYNTHASES , INHIBITORS , QUINONES , POSITRON EMISSION TOMOGRAPHY , LIPID METABOLISM , OPTIMIZATION , TABLES(DATA) , IN VITRO ANALYSIS , NEOPLASMS , AZOLES


Subject Categories : Biochemistry
      Medicine and Medical Research
      Pharmacology


Distribution Statement : APPROVED FOR PUBLIC RELEASE