Disconnection between the early onset anorectic effects by C75 and hypothalamic fatty acid synthase inhibition in rodents

European Journal of Pharmacology

Volumn 511, Issue 1, 2005, Pages 31-41

  Rohrbach, Kenneth W ^a   Han, Songping ^a   Gan, Jinping ^a   O'Tanyi, Eva J ^a   Zhang, Hongwei ^a   Chi, Cecilia L ^a   Taub, Rebecca ^a,b   Largent, Brian L ^a   Cheng, Dong ^a  

^a BRISTOL MYERS SQUIBB   (United States)

^b HOFFMANN LA ROCHE INC   (United States)

Author keywords

Appetite suppression; C75; Fatty acid synthase; Obesity

Indexed keywords

3 CARBOXY 4 OCTYL 2 METHYLENEBUTYROLACTONE; C 75; FATTY ACID SYNTHASE; FENFLURAMINE; GAMMA BUTYROLACTONE DERIVATIVE; PHENTERMINE; PROTEIN C FOS; SIBUTRAMINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANOREXIA; APPETITE; AREA POSTREMA; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; ENZYME ACTIVITY; ENZYME INHIBITION; FOOD INTAKE; HYPOTHALAMUS; IC 50; IN VITRO STUDY; IN VIVO STUDY; INHIBITION KINETICS; MALE; MEASUREMENT; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; QUANTITATIVE ANALYSIS; RAT; RAT STRAIN; RODENT;

EID: 15044351299     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2005.01.034     Document Type: Article

References (28)

1. U. Andersson, K. Filipsson, C.R. Abbott, A. Woods, K. Smith, S.R. Bloom, D. Carling, and C.J. Small AMP-activated protein kinase plays a role in the control of food intake J. Biol. Chem. 279 2004 12005 12008
2. M.J. Arslanian, and S.J. Wakil Fatty acid synthase from chicken liver Methods Enzymol. 35 1975 59 65
3. D. Cheng, R.L. Meegalla, B. He, D.A. Cromley, J.T. Billheimer, and P.R. Young Human acyl-CoA: diacylglycerol acyltransferase is a tetrameric protein Biochem. J. 359 2001 707 714
4. D.J. Clegg, M.D. Wortman, S.C. Benoit, C.C. McOsker, and R.J. Seeley Comparison of central and peripheral administration of C75 on food intake, body weight, and conditioned taste aversion Diabetes 51 2002 3196 3201
5. J.M. Friedman Obesity in the new millennium Nature 404 2000 632 634
6. J.M. Fritschy, C.G. Frondoza, and R. Grzanna Differential effects of reserpine on brainstem catecholaminergic neurons revealed by Fos protein immunohistochemistry Brain Res. 562 1991 48 56
7. S. Gao, and M.D. Lane Effect of the anorectic fatty acid synthase inhibitor C75 on neuronal activity in the hypothalamus and brainstem Proc. Natl. Acad. Sci. U. S. A. 100 2003 5628 5633
8. D.G. Hardie, and D. Carling The AMP-activated protein kinase-fuel gauge of the mammalian cell? Eur. J. Biochem. 246 1997 259 273
9. L.K. Heisler, M.A. Cowley, L.H. Tecott, W. Low, M.J. Fan, J.L. Smart, M. Rubinstein, J.B. Tatro, J.N. Marcus, H. Holstege, C.E. Lee, R.D. Cone, and J.K. Elmquist Activation of central melanocortin pathways by fenfluramine Science 297 2002 609 611
10. Z. Hu, S.H. Cha, S. Chohnan, and M.D. Lane Hypothalamic malonyl-CoA as a mediator of feeding behavior Proc. Natl. Acad. Sci. U. S. A. 100 2003 12624 12629
11. E.K. Kim, I. Miller, S. Aja, L.E. Landree, M. Pinn, J. McFadden, F.P. Kuhajda, T.H. Moran, and G.V. Ronnett C75, a fatty acid synthase inhibitor, reduces food intake via hypothalamic AMP-activated protein kinase J. Biol. Chem. 279 2004 3817 3827
12. F.P. Kuhajda, E.S. Pizer, J.N. Li, N.S. Mani, G.L. Frehywot, and C.A. Townsend Synthesis and antitumor activity of an inhibitor of fatty acid synthase Proc. Natl. Acad. Sci. U. S. A. 97 2000 3450 3454
13. M.V. Kumar, T. Shimokawa, T.R. Nagy, and M.D. Lane Differential effects of a centrally acting fatty acid synthase inhibitor in lean and obese mice Proc. Natl. Acad. Sci. U. S. A. 99 2002 1921 1925
14. O. Lammert, N. Grunnet, P. Faber, K.S. Bjornsbo, J. Dich, L.O. Larsen, R.A. Neese, M.K. Hellerstein, and B. Quistorff Effects of isoenergetic overfeeding of either carbohydrate or fat in young men Br. J. Nutr. 84 2000 233 245
15. L.E. Landree, A.L. Hanlon, D.W. Strong, G. Rumbaugh, I.M. Miller, J.N. Thupari, E.C. Connolly, R.L. Huganir, C. Richardson, L.A. Witters, F.P. Kuhajda, and G.V. Ronnett C75, a fatty acid synthase inhibitor, modulates AMP-activated protein kinase to alter neuronal energy metabolism J. Biol. Chem. 279 2004 3817 3827
16. T.C. Linn Purification and crystallization of rat liver fatty acid synthetase Arch. Biochem. Biophys. 209 1981 613 619
17. T.M. Loftus, D.E. Jaworsky, G.L. Frehywot, C.A. Townsend, G.V. Ronnett, M.D. Lane, and F.P. Kuhajda Reduced food intake and body weight in mice treated with fatty acid synthase inhibitors Science 288 2000 2379 2381
18. R.L. Meegalla, J.T. Billheimer, and D. Cheng Concerted elevation of acyl-coenzyme A: diacylglycerol acyltransferase (DGAT) activity through independent stimulation of mRNA expression of DGAT1 and DGAT2 by carbohydrate and insulin Biochem. Biophys. Res. Commun. 298 2002 317 323
19. I. Miller, G.V. Ronnett, T.H. Moran, and S. Aja Anorexigenic C75 alters c-Fos in mouse hypothalamic and hindbrain subnuclei NeuroReport 15 2004 925 929
20. Y. Minokoshi, T. Alquier, N. Furukawa, Y.B. Kim, A. Lee, B. Xue, J. Mu, F. Foufelle, P. Ferre, M.J. Birnbaum, B.J. Stuck, and B.B. Kahn AMP-kinase regulates food intake by responding to hormonal and nutrient signals in the hypothalamus Nature 428 2004 569 574
21. N.B. Ruderman, A.K. Saha, D. Vavvas, and L.A. Witters Malonyl-CoA, fuel sensing, and insulin resistance Am. J. Physiol. 276 1999 E1 E18
22. T. Shimokawa, M.V. Kumar, and M.D. Lane Effect of a fatty acid synthase inhibitor on food intake and expression of hypothalamic neuropeptides Proc. Natl. Acad. Sci. U. S. A. 99 2002 66 71
23. 2O Am. J. Physiol., Endocrinol Metabol. 286 2004 E577 E588
24. J. Swierczynski, E. Goyke, L. Wach, A. Pankiewicz, Z. Kochan, W. Adamonis, Z. Sledzinski, and Z. Aleksandrowicz Comparative study of the lipogenic potential of human and rat adipose tissue Metabolism 49 2000 594 599
25. K.A. Takahashi, J.L. Smart, H. Liu, and R.D. Cone The anorexigenic fatty acid synthase inhibitor, C75, is a nonspecific neuronal activator Endocrinology 145 2004 184 193
26. J.N. Thupari, L.E. Landree, G.V. Ronnett, and F.P. Kuhajda C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity Proc. Natl. Acad. Sci. U. S. A. 99 2002 9498 9502
27. S.J. Wakil Fatty acid synthase, a proficient multifunctional enzyme Biochemistry 28 1989 4523 4530
28. M.D. Wortman, D. Clegg, D.J. D'Alessio, S.C. Woods, and R.J. Seeley C75 inhibits food intake by increasing CNS glucose metabolism Nat. Med. 9 2003 483 485