Affiliation: Wake Forest University School of Medicine
- Fatty acid synthase inhibitors: new directions for oncologySteven J Kridel
Wake Forest University School of Medicine, Department of Cancer Biology, Medical Center Boulevard, Winston Salem, North Carolina 27157, USA
Expert Opin Investig Drugs 16:1817-29. 2007..This review outlines the preclinical development of FASN inhibitors, their antitumor effects and the strategies underway to develop novel inhibitors...
- Dietary fat-gene interactions in cancerYong Q Chen
Cancer Biology, Wake Forest University School of Medicine, Medical Center Blvd, Winston Salem, NC 27157, USA
Cancer Metastasis Rev 26:535-51. 2007..The purpose of this review is to present a more cohesive view of dietary fat-gene interactions, and outline a working hypothesis of the intricate connection between fat, genes and cancer...
- Fatty acid synthase activity in tumor cellsJoy L Little
Department of Cancer Biology and Comprehensive Cancer Center, Wake Forest University of Medicine, Winston Salem, NC 27157, USA
Subcell Biochem 49:169-94. 2008..Pharmacological blockade of FASN activity has identified a pleiotropic role for FASN in mediating aspects of proliferation, growth and survival. As a result, a clearer understanding of the role of FASN in tumor cells has been developed...
- Crystal structure of the thioesterase domain of human fatty acid synthase inhibited by OrlistatCharles W Pemble
Center for Structural Biology and Department of Biochemistry, Wake Forest University School of Medicine, Medical Center Boulevard, Winston Salem, North Carolina 27157, USA
Nat Struct Mol Biol 14:704-9. 2007..Our findings provide a foundation for the development of new cancer drugs that target FAS...
- Disruption of crosstalk between the fatty acid synthesis and proteasome pathways enhances unfolded protein response signaling and cell deathJoy L Little
Department of Cancer Biology, Comprehensive Cancer Center, Wake Forest University School of Medicine, Medical Center Boulevard, Winston Salem, NC, USA
Mol Cancer Ther 7:3816-24. 2008..Combined, the data support the concept that the UPR balance between adaptive to stress signaling can be exploited to mediate increased cell death and suggests novel applications of FASN inhibitors for clinical use...
- Inhibition of fatty acid synthase induces endoplasmic reticulum stress in tumor cellsJoy L Little
Department of Cancer Biology, Comprehensive Cancer Center, Wake Forest University School of Medicine, Winston Salem, NC 27157, USA
Cancer Res 67:1262-9. 2007..These results provide the first evidence that FAS inhibitors induce ER stress and establish an important mechanistic link between FAS activity and ER function...
- S-nitrosylation of matrix metalloproteinases: signaling pathway to neuronal cell deathZezong Gu
Center for Neuroscience and Aging, Program in Cell Adhesion and Extracellular Matrix Biology, The Burnham Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Science 297:1186-90. 2002..These findings suggest a potential extracellular proteolysis pathway to neuronal cell death in which S-nitrosylation activates MMPs, and further oxidation results in a stable posttranslational modification with pathological activity...
- Orlistat is a novel inhibitor of fatty acid synthase with antitumor activitySteven J Kridel
Cancer Research Center, The Burnham Institute, 10901 North Torrey Pines Road, La Jolla, CA 92037, USA
Cancer Res 64:2070-5. 2004..By virtue of its ability to inhibit fatty acid synthase, Orlistat halts tumor cell proliferation, induces tumor cell apoptosis, and inhibits the growth of PC-3 tumors in nude mice...
- 1-11C-acetate as a PET radiopharmaceutical for imaging fatty acid synthase expression in prostate cancerAmy L Vavere
Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
J Nucl Med 49:327-34. 2008..Fatty acid synthase (FAS) has been found to be overexpressed in prostate carcinomas, as well as other cancers, and it is possible that imaging with 1-(11)C-acetate could be a marker for its expression...
- Fatty acid synthase inhibitors and prostate cancerSteven J Kridel; Fiscal Year: 2010..The proposed crystal structures will be instrumental to the rational design of analogs of orlistat with improved target specificity, bioavailability, and pharmacokinetics for the treatment of a variety of cancers. ..