| Inhibitors of Fatty Acid Synthase for Prostate Cancer |
MAY 2011 |
13 pages |
| Authors:
Steven J. Kridel; Jeffrey W. Schmitt; W. T. Lowther; WAKE FOREST UNIV WINSTON-SALEM NC
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 | Fatty acid synthase (FASN), the enzyme that synthesizes fatty acid in cells, is overexpressed 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 ... |
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| Inhibitors of Fatty Acid Synthase for Prostate Cancer |
31 MAY 2010 |
44 pages |
| Authors:
Steven J. Kridel; WAKE FOREST UNIV WINSTON-SALEM NC SCHOOL OF HEALTH SCIENCES
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| 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 ... |
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| Fatty Acid Synthase Inhibitors Engage the Cell Death Program Through the Endoplasmic Reticulum |
DEC 2007 |
106 pages |
| Authors:
Steven J. Kridel; WAKE FOREST UNIV WINSTON-SALEM NC SCHOOL OF HEALTH SCIENCES
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| Fatty acid synthase (FAS), the enzyme that synthesizes the 16-carbon fatty acid palmitate, in highly expressed in prostate cancer. Because of a corresponding lack of expression in normal prostate, FAS is an attractive drug target. We have described the endoplasmic reticulum (ER) stress response as a critical mediator of the anti-tumor effects of FAS inhibitors. In this report we also describe a novel connection between the FAS pathway and the ... |
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| Inhibition of Fatty Acid Synthase in Prostate Cancer by Orlistat, a Novel Therapeutic |
NOV 2007 |
66 pages |
| Authors:
Steven J. Kridel; WAKE FOREST UNIV WINSTON-SALEM NC SCHOOL OF HEALTH SCIENCES
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| The basic premise of this proposal was based on two important findings. The first was the discovery that fatty acid synthase (FAS) is overexpressed in prostate cancer as well as in many other cancers. FAS is the enzyme that catalyzes the synthesis of fatty acid from the precursors acetyl-CoA and malonyl-CoA. The fatty acids are then utilized for subsequent phospholipid synthesis and membrane biogenesis. A body of literature has demonstrated ... |
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| Inhibition of Fatty Acid Synthase in Prostate Cancer by Olristat, a Novel Therapeutic |
NOV 2006 |
54 pages |
| Authors:
Steven J. Kridel; WAKE FOREST UNIV WINSTON-SALEM NC SCHOOL OF HEALTH SCIENCES
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| The overall goal of this project 5 to understand the anti-tumor effects of FAS inhibitors. We have followed up on our previous findings by further evaluating the role of ER stress in tumor cells treated with FAS inhibitors. Our results suggest that ER stress may initiate the cell death program when FAS is inhibited in prostate tumor cell lines. Moreover, the data also suggest that the ER may sense fatty ... |
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