Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-01-24
1997-03-25
Hendricks, Keith D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514558, 514559, 514560, 424417, 424450, A01N 4320, A01N 2526, A61K 31335, A61K 9127
Patent
active
056145519
ABSTRACT:
Fatty acid synthase (FAS) is overexpressed by certain infectious organisms that are resistant to most currently available antibiotics. Contrarywise, little FAS expression is identified in patient tissues. Inhibition of fatty acid synthesis is thus selectively toxic to invasive cells, while patient cells with low FAS activity are resistant. This invention provides a method of treating septic patients where fatty acid synthesis by invading cells is inhibited with resultant interruption of the disease process.
REFERENCES:
patent: 3535309 (1970-10-01), Hata et al.
patent: 3630846 (1971-12-01), Hata et al.
patent: 3897428 (1975-07-01), Omura et al.
patent: 3909361 (1975-09-01), Hata et al.
patent: 4000164 (1976-12-01), Parker
patent: 4011334 (1977-03-01), Parker
patent: 4032647 (1977-06-01), Parker
patent: 4110351 (1978-08-01), Parker
patent: 4146623 (1979-03-01), Parker
patent: 4328246 (1982-05-01), Gold
patent: 4602099 (1986-07-01), Parker
patent: 4738984 (1988-04-01), Parker
patent: 4789630 (1988-12-01), Bloch et al.
patent: 4877782 (1989-10-01), Cazers et al.
patent: 4883665 (1989-11-01), Miyazima et al.
patent: 4968494 (1990-11-01), Claremon et al.
patent: 5070009 (1991-12-01), Crepin
patent: 5110731 (1992-05-01), Fisher
patent: 5143907 (1992-09-01), Spielvogel
patent: 5185149 (1993-02-01), Baldwin et al.
patent: 5188830 (1993-02-01), Atkinson et al.
patent: 5190969 (1993-03-01), Blumenstein et al.
patent: 5539132 (1996-07-01), Royer et al.
Bacchi, et al., "Effects of Some Antitumor Agents on Growth and Glycolytic Enzymes of the Flagellate Crithidia," J. Bacteriol., 98:23-28 (1969).
Furnica, et al., "Mecanismes Biochimiques Impliques Dans La Sensibilisation Des Organismes Vivants Par Des Agents Chimiques A L'Action Des Radiations et Des Cytostatiques," Rev. Roum. Biochim., 8:117-122 (1971).
Omura, et al., "Relationship Between the Structures of Fatty Acid Amide Derivatives and Their Antimicrobial Activities," Antimicrobial Agents and Chemotherapy, 6:207-215 (1974).
Omura, Satoshi, "The Antibiotic Cerulenin, a Novel Tool for Biochemistry as an Inhibitor of Fatty Acid Synthesis," Bacteriological Reviews, 40:681-697 (1976).
Altenbern, Robert A., "Cerulenin-Inhibited Cells of Staphylococcus aureus Resume Growth When Supplemented with Either a Saturated or an Unsaturated Fatty Acid," Antimicrobial Agents and Chemotherapy, 11:574-576 (1977).
Altenbern, Robert A., "Extreme Sensitivity of Staphylococcal Enterotoxin B and C Production in Inhibition by Cerulenin," Antimicrobial Agents and Chemotherapy, 11:906-908 (1977).
Partida, et al., "Comparative Effects of Diphenylglioxal and its Superoxide on Experimental Tumors," Arch. de Farmacol. y Toxicol, III:231-240 (1977).
Chen, et al., "The Cerulenin-Induced Formation of 1-Acyl-Lysophosphatidyl Glycerol in Bacillus megaterium," Biochem. Biophys. Res. Comm., 80:126-132 (1978).
Carson, et al., "Effect of Cerulenin on Streptococcus faecalis Macromolecular Synthesis and Cell Division," J. Bacteriol., 133:472-476 (1978).
Leung, et al., "Streptococcus mutans Dextransucrase: Effect of Cerulenin on Lipid Synthesis and Enzyme Production," Infection and Immunity, 28:846-852 (1980).
Smith, et al., "Thioesterase II, a New Marker Enzyme for Human Cells of Breast Epithelial Origin," JNCI, 73:323-329 (1981).
Carson, et al., "Effect of Cerulenin on Cellular Autolytic Activity and Lipid Metabolism During Inhibition of Protein Synthesis in Streptococcus faecalis," J. Bacteriol., 146:590-604 (1981).
Bocquet-Pages, et al., "Lipid-Synthesis-Dependent Biosynthesis (or Assembly) of Major Outer-Membrane Proteins of Escherichia oli," Eur. J. Biochem., 118:105-111 (1981).
Omura, Satoshi, Chapter 39 "Cerulenin" in Methods in Enzymology, 72:520-532 (1981).
Thompson, et al., "Purification and Properties Of Fatty Acid Synthetase From A Human Breast Cell Line," Biochim. Biophys. Acta, 662:125-130 (1981).
Ahmad, et al., "Studies on Acetyl-CoA Carboxylase and Fatty Acid Synthase from Rat Mammary Gland and Mammary Tumors," Biochem. J., 208:443-452 (1982).
Clements, et al., "Irreversible Inhibition of Fatty Acid Synthase from Rat Mammary Gland with S-(4-bromo-2,3-dioxobutyl)-CoA," Biochem. J., 207:291-296 (1982).
Thompson, et al., "Lack of Coordinated Regulation Of Lipogenic Enzymes In A Human Breast Cell Line SKBr3," Biochem. Biophys. Acta, 712:217-220 (1982).
M ants al a, et al., "Secretion of .beta.-lactamase by Escherichia coli in vivo and in vitro: Effect of Cerulenin," Antonie van Leeuwenhoek, 48:353-364 (1982).
Hayashi, et al., "Mechanism of Action of the Antibiotic Thiolactomycin Inhibition of Fatty Acid Synthesis of Escherichia coli," Biochem. Biophys. Res. Comm., 115:1108-1113 (1983).
Spiegelman, et al., "Fibronectin Modulation of Cell Shape and Lipogenic Gene Expression in 3T2-Adipocytes," Cell, 35:657-666 (1983).
Mendoza, et al., "Thermal Regulation of Membrane Fluidity in Escherichia coli," J. Biol. Chem., 258:2098-2101 (1983).
Mahajan, et al., "Cerulenin Inhibition of Lipid Synthesis and Its Reversal by Exogenous Fatty Acids in Mycobacterium smegmatis ATTC 607," Can. J. Biochem. Cell Biol., 63:85-90 (1984).
Mahajan et al., "Cerulenin Effect on Phospholipid Metabolism in Mycobacterium smegmatis ATTC 607," Biochim. Biophys. Acta, 795:493-498 (1984).
Hait, et al., "Inhibition of Growth of Leukemic Cells by Inhibitors Of Calmodulin: Phenothiazines and Melittin," Cancer Chemother. Pharmacol., 14:202-205 (1985).
Rainwater, et al., "Fatty Acid Biosynthesis in Mycobacterium tuberculosis var. bovis Bacillus Calmette-Guerin," J. Biol. Chem., 260:616-623 (1985).
Abraham, et al., "Lipid Metabolism and Enzyme Activities In Hormone-Dependent and Hormone-Independent Mammary Adenocarcinoma in GR Mice," JNCI, 77:233-239 (1986).
Chalbos, et al., "Cloning of cDNA Sequences Of a Progestin-regulated mRNA from MCF7 Human Breast Cancer Cells," Nucl. Acids Res., 14:965-981 (1986).
Pawlak, et al., "Evaluation of Thioesterase II as a Serum Marker for Rat Mammary Cancer," Cancer Research, 46:4712-4719 (1986).
Nishida, et al., "Effect of Thiolactomycin on the Individual Enzymes of the Fatty Acid Synthase System in Escherichia coli," J. Biochem., 99:1447-1454 (1986).
Hoberg, et al., "Characterization of Cerulenin-Resistant Mutants of Candida albicans," Infection and Immunity, 51:102-109 (1986).
Tomada, et al., "Inhibition of acyl-CoA Synthetase by Triacsins," Biochim. Biophys. Acta, 921:595-598 (1987).
Chalbos, et al., "Fatty Acid Synthetase and Its mRNA Are Induced By Progestins in Breast Cancer Cells," J. Biol. Chem., 262:9923-9926 (1987).
Debs, et al., "Selective Enhancement of Pentamidine Uptake in the Lung by Aerosolization and Delivery in Liposomes," Amer. Rev. Respir. Dis., 135:731-737 (1987).
McAllister, et al., "The Effect of Tumour Growth on Liver Pantothenate, CoA, and Fatty Acid Synthetase Activity in the Mouse," Br. J. Cancer, 57:83-86 (1988).
Wilder, et al., "Altered Metabolic Rate and Fatty Acid Distribution in Adriamycin Resistant P388 Cells," Proceedings of AACR, 29-318, Abstr. 1265 (1988).
Tisdale, et al., "Changes in Host Liver Fatty Acid Synthase in Tumour-Bearing Mice," Cancer Letters, 42:231-235 (1988).
Bolla, et al., "The Assembly of the Major Outer Membrane Protein OmpF of Escherichia coli Depends on Lipid Synthesis," The EMBO Journal, 7:3595-3599 (1988).
Harris, et al., "Inhibition of Phenolic Glycolipid-1 Synthesis in Extracellular Mycobacterium leprae as an Indicator of Antimicrobial Activity," International Journal of Leprosy, 56:588-591 (1988).
Debs, et al., "Lung-Specific Delivery of Cytokines Induces Sustained Pulmonary and Systemic Immunomodulation in Rats," J. Immunol., 140:3482-3488 (1988).
Spydevold, et al., "Activities of Enzymes of Lipid Metabolism in Morris Hepatoma," Biochim. Biophys. Acta, 1003:80-83 (1989).
Chambon, et al., "Progestins and Androgens Stimulate Lipid Accumulation In T47D Breast Cancer Cells Via Their Own Receptors," J. Steroid Biochem., 33:915-922 (1989).
Wall et al., "Covalent Reaction of Cerulenin at the Active Site of acyl-CoA Reductase of Photobacterium phosphoreum," Biochem. Cell Biol., 67:163-167 (1989).
Joyeux, et al., "Proge
Dick James D.
Kuhajda Francis P.
Hendricks Keith D.
Moore William W.
The Johns Hopkins University
LandOfFree
Inhibitors of fatty acid synthesis as antimicrobial agents does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Inhibitors of fatty acid synthesis as antimicrobial agents, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Inhibitors of fatty acid synthesis as antimicrobial agents will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2203886