Rae, C. , Babich, J. W. and Mairs, R. J. (2017) Differential in radiosensitizing potency of enantiomers of the fatty acid synthase inhibitor C75. Chirality, 29(1), pp. 10-13. (doi: 10.1002/chir.22668) (PMID:27901292) (PMCID:PMC5248592)
|
Text
132443.pdf - Published Version Available under License Creative Commons Attribution. 185kB |
Abstract
The elevated activity of fatty acid synthase has been reported in a number of cancer types. Inhibition of this enzyme has been demonstrated to induce cancer cell death and reduce tumor growth. In addition, the fatty acid synthase inhibitor drug C75 has been reported to synergistically enhance the cancer-killing ability of ionizing radiation. However, clinical use of C75 has been limited due to its producing weight loss, believed to be caused by alterations in the activity of carnitine palmitoyltransferase-1. C75 is administered in the form of a racemic mixture of (−) and (+) enantiomers that may differ in their regulation of fatty acid synthase and carnitine palmitoyltransferase-1. Therefore, we assessed the relative cancer-killing potency of different enantiomeric forms of C75 in prostate cancer cells. These results suggest that (−)-C75 is the more cytotoxic enantiomer and has greater radiosensitizing capacity than (+)-C75. These observations will stimulate the development of fatty acid synthase inhibitors that are selective for cancer cells and enhance the tumor-killing activity of ionizing radiation, while minimizing weight loss in cancer patients.
| Item Type: | Articles |
|---|---|
| Status: | Published |
| Refereed: | Yes |
| Glasgow Author(s) Enlighten ID: | Mairs, Professor Robert and Rae, Dr Colin |
| Authors: | Rae, C., Babich, J. W., and Mairs, R. J. |
| College/School: | College of Medical Veterinary and Life Sciences > School of Cancer Sciences |
| Journal Name: | Chirality |
| Publisher: | Wiley |
| ISSN: | 0899-0042 |
| ISSN (Online): | 1520-636X |
| Published Online: | 30 November 2016 |
| Copyright Holders: | Copyright © 2016 The Authors |
| First Published: | First published in Chirality 29(1): 10-13 |
| Publisher Policy: | Reproduced under a Creative Commons License |
University Staff: Request a correction | Enlighten Editors: Update this record
Altmetric
Altmetric