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Accession Number ADA570535
Title Inhibitors of Fatty Acid Synthase for Prostate Cancer.
Publication Date May 2012
Media Count 18p
Personal Author S. J. Kridel
Abstract The purpose of this proposal was to develop and optimize chemical scaffolds as potential inhibitors of fatty acid synthase (FASN), specifically the thioesterase (TE) domain. This line of investigation was based on a series of observation by many groups, including ours, that FASN represents a valuable drug target. It isoverexpressed in prostate cancer and appears to be required for tumor cells to survive. Through an iterative scheme of in silico design, activity-based screening and structural analyses we identified a series of novel pharmacophores with the ability to inhibit the thioesterase domain of FASN. This proposal had three specific aims. They were (1) To optimize compounds through structure-based design, chemical syntheses and in vitro testing, (2) To determine the toxicological and pharmacokinetic properties of the most promising analog(s), and (3) To test the efficacy of the analog(s) in mouse xenograft models of human prostate cancer. Here we summarize the findings by our group during the course of the research proposal.
Keywords Drugs
Fatty acids
Inhibitors
Prostate cancer
Synthases
Thioesterase


 
Source Agency Non Paid ADAS
NTIS Subject Category 57A - Anatomy
57S - Physiology
57E - Clinical Medicine
Corporate Author Wake Forest Coll., Winston-Salem, NC.
Document Type Technical report
Title Note Annual rept. 1 May 2011-30 Apr 2012.
NTIS Issue Number 1315
Contract Number W81XWH-09-1-0204

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