cerulenin

Summary

Summary: An epoxydodecadienamide isolated from several species, including ACREMONIUM, Acrocylindrum, and Helicoceras. It inhibits the biosynthesis of several lipids by interfering with enzyme function.

Top Publications

  1. Bills G, Platas G, Gams W. Conspecificity of the cerulenin and helvolic acid producing 'Cephalosporium caerulens', and the hypocrealean fungus Sarocladium oryzae. Mycol Res. 2004;108:1291-300 pubmed
    Fermentation processes for the biochemical reagents cerulenin and helvolic acid employ 'Cephalosporium caerulens,' an invalidly published designation that has been used for more than 40 years...
  2. Straub S, Sharp G. Inhibition of insulin secretion by cerulenin might be due to impaired glucose metabolism. Diabetes Metab Res Rev. 2007;23:146-51 pubmed
    b>Cerulenin, an inhibitor of protein acylation, has been used as a tool to study the potential role of protein acylation in a variety of activities in different cells, and in stimulus-secretion coupling in pancreatic islets and clonal beta-..
  3. Wang W, Zhao X, Wang H, Liang Y. Increased fatty acid synthase as a potential therapeutic target in multiple myeloma. J Zhejiang Univ Sci B. 2008;9:441-7 pubmed publisher
    ..To determine fatty acid synthase (FAS) expression in human multiple myeloma and verify its potential as a therapeutic target in multiple myeloma...
  4. Ronnett G, Kim E, Landree L, Tu Y. Fatty acid metabolism as a target for obesity treatment. Physiol Behav. 2005;85:25-35 pubmed
    ..Inhibition of FAS using cerulenin or synthetic FAS inhibitors such as C75 reduces food intake and induces profound reversible weight loss...
  5. Rastogi N, Goh K, Horgen L, Barrow W. Synergistic activities of antituberculous drugs with cerulenin and trans-cinnamic acid against Mycobacterium tuberculosis. FEMS Immunol Med Microbiol. 1998;21:149-57 pubmed
    ..In the present study, we investigated cerulenin and trans-cinnamic acid, which have recently been shown to augment the activity of various antibiotics against ..
  6. Makimura H, Mizuno T, Yang X, Silverstein J, Beasley J, Mobbs C. Cerulenin mimics effects of leptin on metabolic rate, food intake, and body weight independent of the melanocortin system, but unlike leptin, cerulenin fails to block neuroendocrine effects of fasting. Diabetes. 2001;50:733-9 pubmed
    b>Cerulenin and a related compound, C75, have recently been reported to reduce food intake and body weight independent of leptin through a mechanism hypothesized, like leptin, to involve hypothalamic nutrition-sensitive neurons...
  7. Shu I, Lindenberg D, Mizuno T, Roberts J, Mobbs C. The fatty acid synthase inhibitor cerulenin and feeding, like leptin, activate hypothalamic pro-opiomelanocortin (POMC) neurons. Brain Res. 2003;985:1-12 pubmed
    ..hypothesis, hypothalamic sections from mice that were fed or injected with the fatty acid synthase inhibitor cerulenin were examined for Fos (a marker for neuronal activation) and POMC product immunoreactivity and compared with ..
  8. Heiligtag S, Bredehorst R, David K. Key role of mitochondria in cerulenin-mediated apoptosis. Cell Death Differ. 2002;9:1017-25 pubmed
    b>Cerulenin, a fungal metabolite, is known to be a specific inhibitor of fatty acid synthase...
  9. Gaspar M, Aregullin M, Jesch S, Henry S. Inositol induces a profound alteration in the pattern and rate of synthesis and turnover of membrane lipids in Saccharomyces cerevisiae. J Biol Chem. 2006;281:22773-85 pubmed
    ..These results are discussed in relationship to transcriptional regulation known to be linked to lipid metabolism in yeast...

More Information

Publications90

  1. Akada R, Shimizu Y, Matsushita Y, Kawahata M, Hoshida H, Nishizawa Y. Use of a YAP1 overexpression cassette conferring specific resistance to cerulenin and cycloheximide as an efficient selectable marker in the yeast Saccharomyces cerevisiae. Yeast. 2002;19:17-28 pubmed
    ..Yeast cells containing PGKp-YAP1 were resistant to cycloheximide, a protein synthesis inhibitor, and also to cerulenin, a fatty acid synthesis inhibitor, but not to other drugs tested...
  2. Thupari J, Pinn M, Kuhajda F. Fatty acid synthase inhibition in human breast cancer cells leads to malonyl-CoA-induced inhibition of fatty acid oxidation and cytotoxicity. Biochem Biophys Res Commun. 2001;285:217-23 pubmed
    ..We have found that: [i] inhibition of FAS with cerulenin causes carnitine palmitoyltransferase-1 (CPT-1) inhibition and fatty acid oxidation inhibition in MCF-7 human ..
  3. Murata S, Yanagisawa K, Fukunaga K, Oda T, Kobayashi A, Sasaki R, et al. Fatty acid synthase inhibitor cerulenin suppresses liver metastasis of colon cancer in mice. Cancer Sci. 2010;101:1861-5 pubmed publisher
    ..Expression of FAS was evaluated in murine CRC cell lines Colon 26 and CMT 93. Cerulenin, a natural inhibitor of FAS, induced apoptosis in these cell lines...
  4. Slade R, Hunt D, Pochet M, Venema V, Hennigar R. Characterization and inhibition of fatty acid synthase in pediatric tumor cell lines. Anticancer Res. 2003;23:1235-43 pubmed
    ..Finally, the FAS inhibitor cerulenin was investigated for its ability to suppress tumor cell growth...
  5. Oskouian B, Saba J. YAP1 confers resistance to the fatty acid synthase inhibitor cerulenin through the transporter Flr1p in Saccharomyces cerevisiae. Mol Gen Genet. 1999;261:346-53 pubmed
    In this study, we utilized a genetic approach to identify genes which render yeast cells resistant to cerulenin (Cer), a potent and noncompetitive inhibitor of fatty acid synthase (FAS)...
  6. Jin Y, Li S, Zhao Z, An J, Kim R, Kim Y, et al. Carnitine palmitoyltransferase-1 (CPT-1) activity stimulation by cerulenin via sympathetic nervous system activation overrides cerulenin's peripheral effect. Endocrinology. 2004;145:3197-204 pubmed
    To clarify the paradoxic effects of cerulenin, namely its in vitro inhibitory effects on fat catabolism and its in vivo reduction of fat mass, we studied the in vivo and in vitro effects of cerulenin on carnitine palmitoyltransferase-1 (..
  7. Deepa P, Vandhana S, Krishnakumar S. Fatty acid synthase inhibition induces differential expression of genes involved in apoptosis and cell proliferation in ocular cancer cells. Nutr Cancer. 2013;65:311-6 pubmed publisher
    ..Differential gene expression in cultured retinoblastoma cells induced by cerulenin, a chemical inhibitor of FASN, was evaluated by cDNA microarray analysis...
  8. Kwok A, Wong J. Lipid biosynthesis and its coordination with cell cycle progression. Plant Cell Physiol. 2005;46:1973-86 pubmed
    ..Fatty acid synthesis and cellulose synthesis are apparently coupled to the cell cycle via independent pathways...
  9. Price A, Choi K, Heath R, Li Z, White S, Rock C. Inhibition of beta-ketoacyl-acyl carrier protein synthases by thiolactomycin and cerulenin. Structure and mechanism. J Biol Chem. 2001;276:6551-9 pubmed
    ..of type II fatty acid synthesis and are the targets for two natural products, thiolactomycin (TLM) and cerulenin. The high resolution structures of the FabB-TLM and FabB-cerulenin binary complexes were determined...
  10. Gabrielson E, Pinn M, Testa J, Kuhajda F. Increased fatty acid synthase is a therapeutic target in mesothelioma. Clin Cancer Res. 2001;7:153-7 pubmed
    ..These results suggest that FAS may be an effective target for pharmacological therapy in a high proportion of human mesotheliomas...
  11. Pizer E, Chrest F, DiGiuseppe J, Han W. Pharmacological inhibitors of mammalian fatty acid synthase suppress DNA replication and induce apoptosis in tumor cell lines. Cancer Res. 1998;58:4611-5 pubmed
    Pharmacological inhibitors of the anabolic enzyme, fatty acid synthase (FAS), including the natural product cerulenin and the novel compound c75, are selectively cytotoxic to cancer cells via induction of apoptosis, apparently related to ..
  12. Shiragami R, Murata S, Kosugi C, Tezuka T, Yamazaki M, Hirano A, et al. Enhanced antitumor activity of cerulenin combined with oxaliplatin in human colon cancer cells. Int J Oncol. 2013;43:431-8 pubmed publisher
    Fatty acid synthase is highly expressed in many types of human cancers. Cerulenin, a natural inhibitor of fatty acid synthase, induced apoptosis in the human colon cancer cell lines HCT116 and RKO...
  13. Ho T, Ho Y, Wong W, Chi Ming Chiu L, Wong Y, Eng Choon Ooi V. Fatty acid synthase inhibitors cerulenin and C75 retard growth and induce caspase-dependent apoptosis in human melanoma A-375 cells. Biomed Pharmacother. 2007;61:578-87 pubmed
    ..The growth-inhibitory effects of FAS inhibitors cerulenin and C75 were then investigated on these cancer cell lines, particularly the human melanoma A-375...
  14. Cheng G, Palanisamy A, Evans Z, Sutter A, Jin L, Singh I, et al. Cerulenin blockade of fatty acid synthase reverses hepatic steatosis in ob/ob mice. PLoS ONE. 2013;8:e75980 pubmed publisher
    ..The objective of this study was to investigate the effect of the fatty acid synthase inhibitor cerulenin on hepatic function in steatotic ob/ob mice...
  15. Menendez J, Vellon L, Mehmi I, Oza B, Ropero S, Colomer R, et al. Inhibition of fatty acid synthase (FAS) suppresses HER2/neu (erbB-2) oncogene overexpression in cancer cells. Proc Natl Acad Sci U S A. 2004;101:10715-20 pubmed
    ..Pharmacological FAS inhibitors cerulenin and C75 were found to suppress p185(HER2) oncoprotein expression and tyrosine-kinase activity in breast and ..
  16. DeJesus G, Bizzozero O. Effect of 2-fluoropalmitate, cerulenin and tunicamycin on the palmitoylation and intracellular translocation of myelin proteolipid protein. Neurochem Res. 2002;27:1669-75 pubmed
    ..3H]palmitate or [3H]leucine in the presence or absence of various concentrations of 2-fluoropalmitate (FP), cerulenin (CER), or tunicamycin (TM)...
  17. Dridi S, Ververken C, Hillgartner F, Arckens L, Lutgarde A, Van der Gucht E, et al. FAS inhibitor cerulenin reduces food intake and melanocortin receptor gene expression without modulating the other (an)orexigenic neuropeptides in chickens. Am J Physiol Regul Integr Comp Physiol. 2006;291:R138-47 pubmed
    b>Cerulenin, a natural fatty acid synthase (FAS) inhibitor, and its synthetic analog C75 are hypothesized to alter the metabolism of neurons in the hypothalamus that regulate ingestive behavior to cause a profound decrease of food intake ..
  18. Morita N, Nishida T, Tanaka M, Yano Y, Okuyama H. Enhancement of polyunsaturated fatty acid production by cerulenin treatment in polyunsaturated fatty acid-producing bacteria. Biotechnol Lett. 2005;27:389-93 pubmed
    ..5 microg cerulenin ml-1, an inhibitor for fatty acid biosynthesis, the cells grew normally, but the content of DHA in the total ..
  19. Schujman G, Choi K, Altabe S, Rock C, de Mendoza D. Response of Bacillus subtilis to cerulenin and acquisition of resistance. J Bacteriol. 2001;183:3032-40 pubmed
    b>Cerulenin is a fungal mycotoxin that potently inhibits fatty acid synthesis by covalent modification of the active site thiol of the chain-elongation subtypes of beta-ketoacyl-acyl carrier protein (ACP) synthases...
  20. Liu X, Shi Y, Giranda V, Luo Y. Inhibition of the phosphatidylinositol 3-kinase/Akt pathway sensitizes MDA-MB468 human breast cancer cells to cerulenin-induced apoptosis. Mol Cancer Ther. 2006;5:494-501 pubmed
    ..The specific fatty acid synthase inhibitor cerulenin can induce apoptosis in cancer cells...
  21. Jackowski S, Wang J, Baburina I. Activity of the phosphatidylcholine biosynthetic pathway modulates the distribution of fatty acids into glycerolipids in proliferating cells. Biochim Biophys Acta. 2000;1483:301-15 pubmed
    ..Cellular fatty acid synthesis was essential for membrane PL synthesis. Cerulenin inhibition of endogenous fatty acid synthesis also inhibited PtdCho synthesis, which was not relieved by ..
  22. Moche M, Schneider G, Edwards P, Dehesh K, Lindqvist Y. Structure of the complex between the antibiotic cerulenin and its target, beta-ketoacyl-acyl carrier protein synthase. J Biol Chem. 1999;274:6031-4 pubmed
    ..The crystal structure of the complex of the enzyme from Escherichia coli, and the fungal mycotoxin cerulenin reveals that the inhibitor is bound in a hydrophobic pocket formed at the dimer interface...
  23. Tirado Vélez J, Joumady I, Sáez Benito A, Cozar Castellano I, Perdomo G. Inhibition of fatty acid metabolism reduces human myeloma cells proliferation. PLoS ONE. 2012;7:e46484 pubmed publisher
    ..In conclusion, inhibition of fatty acid metabolism represents a potential therapeutic approach to treat human multiple myeloma...
  24. Schubert S, Barker K, Znaidi S, Schneider S, Dierolf F, Dunkel N, et al. Regulation of efflux pump expression and drug resistance by the transcription factors Mrr1, Upc2, and Cap1 in Candida albicans. Antimicrob Agents Chemother. 2011;55:2212-23 pubmed publisher
    ..albicans, but gain-of-function mutations in either of the two transcription factors can independently mediate efflux pump overexpression and drug resistance. ..
  25. Nishiuchi H, Tabira Y, Yamagishi K. A combination of flow cytometry and traditional screening using chemicals to isolate high glutathione-producing yeast mutants. Biosci Biotechnol Biochem. 2012;76:1085-90 pubmed
    ..Traditional screening using cerulenin resulted in similar findings, but a combination of both methods resulted in a 40% increase in the screening ..
  26. Santolla M, Lappano R, De Marco P, Pupo M, Vivacqua A, Sisci D, et al. G protein-coupled estrogen receptor mediates the up-regulation of fatty acid synthase induced by 17?-estradiol in cancer cells and cancer-associated fibroblasts. J Biol Chem. 2012;287:43234-45 pubmed publisher
    ..proliferative effects induced by E2 and G-1 in these cells involved FASN as the inhibitor of its activity, named cerulenin, abolished the growth response to both ligands...
  27. Yasumoto Y, Miyazaki H, Vaidyan L, Kagawa Y, Ebrahimi M, Yamamoto Y, et al. Inhibition of Fatty Acid Synthase Decreases Expression of Stemness Markers in Glioma Stem Cells. PLoS ONE. 2016;11:e0147717 pubmed publisher
    ..When GSCs were treated with 20 μM cerulenin, a pharmacological inhibitor of FASN, their proliferation and migration were significantly suppressed and de ..
  28. Heipieper H, de Bont J. Adaptation of Pseudomonas putida S12 to ethanol and toluene at the level of fatty acid composition of membranes. Appl Environ Microbiol. 1994;60:4440-4 pubmed
  29. Kangwan N, Kim Y, Han Y, Jeong M, Park J, Go E, et al. Sonic hedgehog inhibitors prevent colitis-associated cancer via orchestrated mechanisms of IL-6/gp130 inhibition, 15-PGDH induction, Bcl-2 abrogation, and tumorsphere inhibition. Oncotarget. 2016;7:7667-82 pubmed publisher
  30. Yamada S, Komatsu M, Sato Y, Yamauchi K, Aizawa T, Kojima I. Nutrient modulation of palmitoylated 24-kilodalton protein in rat pancreatic islets. Endocrinology. 2003;144:5232-41 pubmed
    ..of the 24-kDa doublet was preferentially attenuated also by the mitochondrial fuels and an acylation inhibitor, cerulenin. The half-life of the labeling of the doublet was apparently shorter (approximately 45 min) than that of other ..
  31. Zhu G, Marchewka M, Woods K, Upton S, Keithly J. Molecular analysis of a Type I fatty acid synthase in Cryptosporidium parvum. Mol Biochem Parasitol. 2000;105:253-60 pubmed
    ..That the discovery of CpFAS1 may provide a new biosynthetic pathway for drug development against cryptosporidiosis, is indicated by the efficacy of the FAS inhibitor cerulenin on the growth of C. parvum in vitro.
  32. Theodorou E, Theodorou M, Kyriakidis D. Involvement of the AtoSCDAEB regulon in the high molecular weight poly-(R)-3-hydroxybutyrate biosynthesis in phaCAB(+)Escherichia coli. Metab Eng. 2012;14:354-65 pubmed publisher
    ..The individual inhibition of ?-oxidation and mainly fatty-acid biosynthesis pathways by acrylic acid or cerulenin respectively, reduced PHB biosynthesis...
  33. Jeong N, Yoo Y. Cerulenin-induced apoptosis is mediated by disrupting the interaction between AIF and hexokinase II. Int J Oncol. 2012;40:1949-56 pubmed publisher
    ..We performed this study to examine the mechanism underlying apoptosis induced by cerulenin and with specific focus on its effect on HKII in ZR-75-1 human breast cancer cells...
  34. Nguyen L, Nosanchuk J. Lipid droplet formation protects against gluco/lipotoxicity in Candida parapsilosis: an essential role of fatty acid desaturase Ole1. Cell Cycle. 2011;10:3159-67 pubmed
    ..Thus, our results show that glucotoxicity is directly linked to lipotoxicity, which we demonstrate is mediated by mitochondrial function...
  35. Siggaard Andersen M, Kauppinen S, von Wettstein Knowles P. Primary structure of a cerulenin-binding beta-ketoacyl-[acyl carrier protein] synthase from barley chloroplasts. Proc Natl Acad Sci U S A. 1991;88:4114-8 pubmed
    The radioactively labeled beta-ketoacyl thioester synthase inhibitor [3H] cerulenin was used to tag three dimeric barely chloroplast proteins (alpha alpha, alpha beta, and beta beta) from the stromal fraction...
  36. Swinnen J, Heemers H, Van de Sande T, de Schrijver E, Brusselmans K, Heyns W, et al. Androgens, lipogenesis and prostate cancer. J Steroid Biochem Mol Biol. 2004;92:273-9 pubmed
  37. Siggaard Andersen M, Wissenbach M, Chuck J, Svendsen I, Olsen J, von Wettstein Knowles P. The fabJ-encoded beta-ketoacyl-[acyl carrier protein] synthase IV from Escherichia coli is sensitive to cerulenin and specific for short-chain substrates. Proc Natl Acad Sci U S A. 1994;91:11027-31 pubmed
    ..Escherichia coli by its ability to restore elongating activity to a protein extract which had been treated with cerulenin, a condensing enzyme-specific inhibitor...
  38. Zhang L, Foster K, Li Q, Martens J. S-acylation regulates Kv1.5 channel surface expression. Am J Physiol Cell Physiol. 2007;293:C152-61 pubmed
    ..Together, these results show that S-acylation can regulate steady-state expression of Kv1.5...
  39. Sanglard D, Ischer F, Monod M, Bille J. Susceptibilities of Candida albicans multidrug transporter mutants to various antifungal agents and other metabolic inhibitors. Antimicrob Agents Chemother. 1996;40:2300-5 pubmed
    ..The same mutant was slightly more susceptible than the wild type to nocodazole, cerulenin, and crystal violet but not to amphotericin B, nikkomycin Z, flucytosine, or pradimicin...
  40. Hughes D, Martel P, Kinlaw W, Eisenberg B. The synthetic triterpenoid CDDO-Im inhibits fatty acid synthase expression and has antiproliferative and proapoptotic effects in human liposarcoma cells. Cancer Invest. 2008;26:118-27 pubmed publisher
    ..effect in the LiSa-2 cell line, and simultaneous treatment with CDDO-Im and the fatty acid synthase inhibitor Cerulenin produced a synergistic cytotoxic effect...
  41. Van Bogaert I, Develter D, Soetaert W, Vandamme E. Cerulenin inhibits de novo sophorolipid synthesis of Candida bombicola. Biotechnol Lett. 2008;30:1829-32 pubmed publisher
    ..Fatty acid synthesis can be blocked by the antifungal agent cerulenin, an inhibitor if the fatty acid synthase (FAS) complex acting on the beta-ketoacyl thioester synthetase reaction...
  42. Abdel Ghany M, Sharp G, Straub S. Glucose stimulation of protein acylation in the pancreatic ?-cell. Life Sci. 2010;87:667-71 pubmed publisher
    ..b>Cerulenin, a classical inhibitor of protein acylation also substantially reduced the incorporation...
  43. Watanabe K, Yazawa K, Kondo K, Kawaguchi A. Fatty acid synthesis of an eicosapentaenoic acid-producing bacterium: de novo synthesis, chain elongation, and desaturation systems. J Biochem. 1997;122:467-73 pubmed
    ..Thus, Shewanella sp., strain SCRC-2738, has novel characteristics as to both fatty acid chain elongation and desaturation systems. ..
  44. Xu D, Sillaots S, Davison J, Hu W, Jiang B, Kauffman S, et al. Chemical genetic profiling and characterization of small-molecule compounds that affect the biosynthesis of unsaturated fatty acids in Candida albicans. J Biol Chem. 2009;284:19754-64 pubmed publisher
  45. Diwischek F, Morschhäuser J, Holzgrabe U. Cerulenin analogues as inhibitors of efflux pumps in drug-resistant Candida albicans. Arch Pharm (Weinheim). 2009;342:150-64 pubmed publisher
    ..The fatty acid synthesis inhibitor cerulenin and the structurally unrelated Golgi transport inhibitor brefeldin A are substrates for both types of efflux ..
  46. Ciana A, Achilli C, Hannoush R, Risso A, Balduini C, Minetti G. Freely turning over palmitate in erythrocyte membrane proteins is not responsible for the anchoring of lipid rafts to the spectrin skeleton: a study with bio-orthogonal chemical probes. Biochim Biophys Acta. 2013;1828:924-31 pubmed publisher
    ..2-bromopalmitate and cerulenin, two known palmitoylation inhibitors, completely inhibited p55 palmitoylation, and protein palmitoyl ..
  47. Bastos D, Paupert J, Maillard C, Seguin F, Carvalho M, Agostini M, et al. Effects of fatty acid synthase inhibitors on lymphatic vessels: an in vitro and in vivo study in a melanoma model. Lab Invest. 2017;97:194-206 pubmed publisher
    ..The effects of FASN inhibitors cerulenin and orlistat on the proliferation, apoptosis, and migration of human lymphatic endothelial cells (HDLEC) were ..
  48. Goblirsch B, Frias J, Wackett L, Wilmot C. Crystal structures of Xanthomonas campestris OleA reveal features that promote head-to-head condensation of two long-chain fatty acids. Biochemistry. 2012;51:4138-46 pubmed publisher
    ..The location of the fatty acid biosynthesis inhibitor, cerulenin, that possesses an alkyl chain length in the range of known OleA substrates, in conjunction with a single xenon ..
  49. Cheng H, Straub S, Sharp G. Protein acylation in the inhibition of insulin secretion by norepinephrine, somatostatin, galanin, and PGE2. Am J Physiol Endocrinol Metab. 2003;285:E287-94 pubmed
    ..In rat pancreatic islets, 2-bromopalmitate, cerulenin, and polyunsaturated fatty acids, all of which suppress protein acyltransferase activity, blocked the distal ..
  50. Katre G, Ajmera N, Zinjarde S, Ravikumar A. Mutants of Yarrowia lipolytica NCIM 3589 grown on waste cooking oil as a biofactory for biodiesel production. Microb Cell Fact. 2017;16:176 pubmed publisher
    ..using the alkylating agent, N- methyl-N'-nitro-N-nitrosoguanidine (MNNG) as well as an additional treatment with cerulenin, a fatty acid synthase inhibitor generated 800 mutants of Y...
  51. Shindiapina P, Barlowe C. Requirements for transitional endoplasmic reticulum site structure and function in Saccharomyces cerevisiae. Mol Biol Cell. 2010;21:1530-45 pubmed publisher
    ..We propose that tER site structures are stable elements that are assembled on an underlying protein and lipid scaffold. ..
  52. Trajtenberg F, Altabe S, Larrieux N, Ficarra F, de Mendoza D, Buschiazzo A, et al. Structural insights into bacterial resistance to cerulenin. FEBS J. 2014;281:2324-38 pubmed publisher
    b>Cerulenin is a fungal toxin that inhibits both eukaryotic and prokaryotic ketoacyl-acyl carrier protein synthases or condensing enzymes...
  53. Benisty R, Cohen A, Feldman A, Cohen Z, Porat N. Endogenous H2O2 produced by Streptococcus pneumoniae controls FabF activity. Biochim Biophys Acta. 2010;1801:1098-104 pubmed publisher
    ..By blocking FabF active site cysteine with cerulenin we show that the oxidized cysteine was the catalytic one...
  54. Mobbs C, Makimura H. Block the FAS, lose the fat. Nat Med. 2002;8:335-6 pubmed
  55. Zheng S, Gao J, Liu Z, Zhang X, Wu S, Weng B, et al. Downregulation of fatty acid synthase complex suppresses cell migration by targeting phosphor-AKT in bladder cancer. Mol Med Rep. 2016;13:1845-50 pubmed publisher
    ..Targeting FASN may represent a promising novel therapeutic strategy for BTCC. ..
  56. Chayakulkeeree M, Rude T, Toffaletti D, Perfect J. Fatty acid synthesis is essential for survival of Cryptococcus neoformans and a potential fungicidal target. Antimicrob Agents Chemother. 2007;51:3537-45 pubmed
    ..Furthermore, a subinhibitory dose of fluconazole showed anticryptococcal activity in vitro in the presence of cerulenin, a fatty acid synthase inhibitor...
  57. Gao S, Keung W, Serra D, Wang W, Carrasco P, Casals N, et al. Malonyl-CoA mediates leptin hypothalamic control of feeding independent of inhibition of CPT-1a. Am J Physiol Regul Integr Comp Physiol. 2011;301:R209-17 pubmed publisher
    ..However, the overexpression of this mutant did not affect the anorectic actions of leptin or central cerulenin for which an increase in Arc malonyl-CoA level is also required...
  58. Wanigasekera A, Hiraga K, Hamanaka N, Oda K. Purification and some properties of an inhibitor for a yeast pleiotropic drug resistant pump from Kitasatospora sp. E-420. Biosci Biotechnol Biochem. 2001;65:2353-7 pubmed
    ..purified inhibitor (molecular weight = 1,193 by FAB-MS) inhibited a Pdr5-mediated efflux of cycloheximide and cerulenin. The intracellular accumulation of a fluorescent dye, rhodamine 123, by the inhibitor was also confirmed...
  59. Hashimoto K, Kawasaki H, Akazawa K, Nakamura J, Asakura Y, Kudo T, et al. Changes in composition and content of mycolic acids in glutamate-overproducing Corynebacterium glutamicum. Biosci Biotechnol Biochem. 2006;70:22-30 pubmed
    ..by biotin limitation or by the supplementation of specific detergents, sublethal amounts of penicillin, or cerulenin. But, it remains unclear why these different treatments, which have different sites of primary action, produce ..
  60. Deepa P, Vandhana S, Jayanthi U, Krishnakumar S. Therapeutic and toxicologic evaluation of anti-lipogenic agents in cancer cells compared with non-neoplastic cells. Basic Clin Pharmacol Toxicol. 2012;110:494-503 pubmed publisher
    ..Here, three inhibitors targeting different domains of FASN--cerulenin, triclosan and orlistat--were evaluated for their anti-proliferative efficacy in ocular cancer, retinoblastoma (..
  61. Jeong N, Lee J, Yoo K, Oh S, Choe E, Lee H, et al. Fatty acid synthase inhibitor cerulenin inhibits topoisomerase I catalytic activity and augments SN-38-induced apoptosis. Apoptosis. 2013;18:226-37 pubmed publisher
    ..One of the most widely used inhibitors of FASN, cerulenin, is a natural product of Cephalosporium caerulens. Cerulenin is selectively toxic to human cancer cells in vitro...
  62. Hennigar R, Pochet M, Hunt D, Lukacher A, Venema V, Seal E, et al. Characterization of fatty acid synthase in cell lines derived from experimental mammary tumors. Biochim Biophys Acta. 1998;1392:85-100 pubmed
    ..Finally, cell lines were treated with the FAS inhibitor cerulenin: almost all breast cancer lines were growth inhibited at significantly lower amounts of drug than normal cell ..
  63. Pereira H, Rebello M. Inhibition of Mayaro virus replication by cerulenin in Aedes albopictus cells. Acta Virol. 1998;42:383-8 pubmed
    The antibiotic cerulenin, an inhibitor of lipid synthesis, was shown to suppress Mayaro virus replication in Aedes albopictus cells at non-cytotoxic doses...
  64. Lopez M, Varela L, Vazquez M, Rodriguez Cuenca S, González C, Velagapudi V, et al. Hypothalamic AMPK and fatty acid metabolism mediate thyroid regulation of energy balance. Nat Med. 2010;16:1001-8 pubmed publisher
    ..These effects are reversed by pharmacological blockade of the SNS. Thus, thyroid hormone-induced modulation of AMPK activity and lipid metabolism in the hypothalamus is a major regulator of whole-body energy homeostasis...
  65. Chohnan S, Furukawa H, Fujio T, Nishihara H, Takamura Y. Changes in the size and composition of intracellular pools of nonesterified coenzyme A and coenzyme A thioesters in aerobic and facultatively anaerobic bacteria. Appl Environ Microbiol. 1997;63:553-60 pubmed
    ..decrease in the amount of acetyl-CoA with a concomitant increase in the amount of CoASH, whereas the addition of cerulenin, a specific inhibitor of fatty acid synthase, triggered the intracellular accumulation of malonyl-CoA...
  66. Kotaka A, Sahara H, Hata Y. The construction and application of diploid sake yeast with a homozygous mutation in the FAS2 gene. J Biosci Bioeng. 2010;110:675-8 pubmed publisher
    In Japanese sake brewing, cerulenin-resistant sake yeasts produce elevated levels of ethyl caproate, an important flavor component. The FAS2 mutation FAS2-1250S of Saccharomyces cerevisiae generates a cerulenin-resistant phenotype...
  67. De Vos M, Lawrence D, Smith C. Cellular pharmacology of cerulenin analogs that inhibit protein palmitoylation. Biochem Pharmacol. 2001;62:985-95 pubmed
    ..We have described previously the synthesis of cerulenin analogs including cis-2,3-epoxy-4-oxononadecanamide (16C) and cis-2,3-epoxy-4-oxododecanamide (9C) that inhibit ..
  68. Yamada S, Komatsu M, Aizawa T, Sato Y, Yajima H, Yada T, et al. Time-dependent potentiation of the beta-cell is a Ca2+-independent phenomenon. J Endocrinol. 2002;172:345-54 pubmed
    ..However, cerulenin or tunicamycin, two inhibitors of protein acylation, eradicated TDP without affecting glucose metabolism...
  69. Koo A, Fulda M, Browse J, Ohlrogge J. Identification of a plastid acyl-acyl carrier protein synthetase in Arabidopsis and its role in the activation and elongation of exogenous fatty acids. Plant J. 2005;44:620-32 pubmed
    ..Laurate elongation was 85% inhibited by 50 microm cerulenin, an inhibitor of ketoacyl-acyl carrier protein (ACP) synthetase I/II...
  70. Menendez J, Ropero S, Mehmi I, Atlas E, Colomer R, Lupu R. Overexpression and hyperactivity of breast cancer-associated fatty acid synthase (oncogenic antigen-519) is insensitive to normal arachidonic fatty acid-induced suppression in lipogenic tissues but it is selectively inhibited by tumoricidal alpha-lin. Int J Oncol. 2004;24:1369-83 pubmed
    ..Interestingly, a long-term exposure to pharmacological inhibitors of FAS activity cerulenin [(2S,3R) 2,3-epoxy-4-oxo-7E,10E-dodecadienamide] or C75 also resulted in a significant reduction of FAS ..
  71. Hu N, Li Y, Zhao Y, Wang Q, You J, Zhang X, et al. A novel positive feedback loop involving FASN/p-ERK1/2/5-LOX/LTB4/FASN sustains high growth of breast cancer cells. Acta Pharmacol Sin. 2011;32:921-9 pubmed publisher
    ..To investigate the endogenous signaling pathways associated with high proliferation potential of breast cancer cells...
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    ..marina strain MP-1. When M. marina strain MP-1 was cultured in medium containing cerulenin, a fatty acid synthesis inhibitor, decreases in levels of middle-chain fatty acids and remarkable increases in ..
  73. Ter Beek A, Keijser B, Boorsma A, Zakrzewska A, Orij R, Smits G, et al. Transcriptome analysis of sorbic acid-stressed Bacillus subtilis reveals a nutrient limitation response and indicates plasma membrane remodeling. J Bacteriol. 2008;190:1751-61 pubmed
    ..This was further supported by the reduced sensitivity toward the fab inhibitor cerulenin upon sorbic acid stress...
  74. Zhao W, Kridel S, Thorburn A, Kooshki M, Little J, Hebbar S, et al. Fatty acid synthase: a novel target for antiglioma therapy. Br J Cancer. 2006;95:869-78 pubmed
    ..Incubating glioma cells with the FAS inhibitor cerulenin decreased endogenous fatty acid synthesis by approximately 50%...
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    ..It is, however, strongly induced when fatty acid biosynthesis is inhibited by diazaborine or cerulenin. Treatment with either compound also causes dose-dependent inhibition of phospholipid biosynthesis whose degree ..
  76. Ghosh M, Amudha R, Jayachandran S, Sakthivel N. Detection and quantification of phytotoxic metabolites of Sarocladium oryzae in sheath rot-infected grains of rice. Lett Appl Microbiol. 2002;34:398-401 pubmed
    ..study describes the detection and quantification of the Sarocladium oryzae metabolites, helvolic acid and cerulenin in extracts of rice grains collected from plants infected with sheath rot...
  77. Hać S, Dobosz M, Kaczor J, Rzepko R. Influence of molecule CD 11b blockade on the course of acute ceruleine pancreatitis in rats. Exp Mol Pathol. 2004;77:57-65 pubmed
    ..Neutrophil aggregation within pancreatic gland modulated by monoclonal antibody CD11b contribute to the extent of injury during the early stage of ceruleine experimental pancreatitis in rats...
  78. Theodorou E, Theodorou M, Kyriakidis D. AtoSC two-component system is involved in cPHB biosynthesis through fatty acid metabolism in E. coli. Biochim Biophys Acta. 2011;1810:561-8 pubmed publisher
    ..We have shown previously that AtoSC two-component system regulates the biosynthesis of E. coli cPHB [complexed poly-(R)-3-hydroxybutyrate]...
  79. Yitzhaki S, Rostron J, Xu Y, Rideout M, Authement R, Barlow S, et al. Similarities between exogenously- and endogenously-induced envelope stress: the effects of a new antibacterial molecule, TPI1609-10. PLoS ONE. 2012;7:e44896 pubmed publisher
    ..The synergy between SM10, and cerulenin, a fatty acid synthesis inhibitor, together with the SM10 hypersensitivity of cpx and rpoE mutants, further ..
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    The transepithelial transport of Cerulenin across Caco-2 cell monolayers was examined in this study...
  81. Sharma S, Sharma S, Modak R, Karmodiya K, Surolia N, Surolia A. Mass spectrometry-based systems approach for identification of inhibitors of Plasmodium falciparum fatty acid synthase. Antimicrob Agents Chemother. 2007;51:2552-8 pubmed
    ..Using known inhibitors of the enzymes of the elongation module, cerulenin, triclosan, NAS-21/91, and (-)-catechin gallate, we demonstrate that accumulation of intermediates resulting ..