专利号:US-7306938-B2 优先权日:1999-12-29 标 题:High throughput screen for inhibitors of fatty acid biosynthesis in bacteria 发明人:MURPHY CHRISTOPHER; YOUNGMAN PHILIP 权利人:MILLENNIUM PHARM INC 摘要:Methods for identifying compounds that are inhibitors of bacterial fatty acid biosynthesis are disclosed. Such compounds can be used as lead compounds in methods for preparing antibacterial agents for treating bacterial infections (e.g., in humans, animals, and plants). Inhibitors of bacterial fatty acid synthesis can also be tested for their ability to inhibit synthesis of acylated homoserine lactones. Compounds that inhibit synthesis of acylated homoserine lactones can be used as inhibitors of bacterial virulence. The disclosed methods allow for high throughput screening of libraries of test compounds.
专利号:US-7579167-B2 优先权日:2002-10-08 标题:Polypeptides involved in the biosynthesis of spiramycins, nucleotide sequences encoding these polypeptides and applications thereof 发明人:BLONDELET-ROUAULT MARIE-HELENE; DOMINGUEZ HELENE; DARBON-RONGERE EMMANUELLE; GERBAUD CLAUDE; GONDRAN ANNE; KARRAY FATMA; LACROIX PATRICIA; OESTREICHER-MERMET-BOUVIER NATHALIE; JEAN-LUC PERNODET; TUPHILE KARINE 权利人:AVENTIS PHARMA S; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the isolation and identification of novel genes of the biosynthetic pathway for spiramycins and to novel polypeptides involved in this biosynthesis. The invention also relates to a method for producing these polypeptides. It also relates to the use of these genes for the purpose of increasing the levels of production and the purity of the spiramycin produced. The invention relates in particular to a microorganism which produces spiramycin I but which does not produce spiramycin II and III, and to the use of such a microorganism. The invention also relates to the use of the genes of the biosynthetic pathway for spiramycins for constructing mutants which can lead to the synthesis of novel antibiotics or to derived forms of spiramycins. The invention also relates to the molecules produced through the expression of these genes and to pharmacologically active compositions of a molecule produced through the expression of such genes.
专利号:US-8124794-B2 优先权日:2002-04-17 标题:Method for the asymmetric synthesis of beta-lactone compounds 发明人:SMITH JEFFREY W; AXELROD FUMIKO; KRIDEL STEVEN J; ROMO DANIEL; PUROHIT VIKRAM; MA GIL 权利人:SMITH JEFFREY W; AXELROD FUMIKO; KRIDEL STEVEN J; ROMO DANIEL; PUROHIT VIKRAM; MA GIL; SANFORD BURNHAM MED RES INST 摘要:The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds.
专利号:US-6051383-A 优先权日:1995-06-26 标题:Sequences for production of 2,4-diacetylphloroglucinol and methods 发明人:THOMASHOW LINDA S; BANGERA MAHALAXMI; WELLER DAVID M; COOK R JAMES 权利人:US AGRICULTURE; UNIV WASHINGTON 摘要:DNA sequences which function specifically in the synthesis of 2,4-diacetylphloroglucinol (Phl) are described. The sequences include phl genes which encode phl gene proteins and coding and regulatory sequences for production of Phl as well as sequences containing phl genes, which sequences have the capability of conferring or enhancing Phl biosynthetic capability in bacterial strains. The transformed strains are useful as biocontrol agents against fungal pathogens.
专利号:US-7994222-B2 优先权日:2006-09-05 标 题:Monitoring of the inhibition of fatty acid synthesis by iodo-nitrobenzamide compounds 发明人:OSSOVSKAYA VALERIA S; SHERMAN BARRY M 权利人:BIPAR SCIENCES INC 摘要:The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.
专利号:US-5614551-A 优先权日:1994-01-24 标题:Inhibitors of fatty acid synthesis as antimicrobial agents 发明人:DICK JAMES D; KUHAJDA FRANCIS P 权利人:UNIV JOHNS HOPKINS 摘要: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.
1: Tamura H, Okada H, Kume K, Koyano T, Goshima T, Nakamura R, Akao T, Shimoi H, Mizunuma M, Ohya Y, Hirata D. Isolation of a spontaneous cerulenin-resistant sake yeast with both high ethyl caproate-producing ability and normal checkpoint integrity. Biosci Biotechnol Biochem. 2015;79(7):1191-9. doi: 10.1080/09168451.2015.1020756. Epub 2015 Mar 19. doi: 10.1021/cb500758s. Epub 2014 Oct 23. doi: 10.1111/febs.12785. Epub 2014 Apr 9. doi: 10.1002/mbo3.154. Epub 2014 Feb 14. 5: Cheng G, Palanisamy AP, Evans ZP, Sutter AG, Jin L, Singh I, May H, Schmidt MG, Chavin KD. Cerulenin blockade of fatty acid synthase reverses hepatic steatosis in ob/ob mice. PLoS One. 2013 Sep 27;8(9):e75980. doi: 10.1371/journal.pone.0075980. eCollection 2013. 6: Dridi S, Decuypere E, Buyse J. Cerulenin upregulates heat shock protein-70 gene expression in chicken muscle. Poult Sci. 2013 Oct;92(10):2745-53. doi: 10.3382/ps.2013-03242. doi: 10.3892/ijo.2013.1978. Epub 2013 Jun 7. doi: 10.1186/2191-0855-2-64.
合成参考文献
参考文献:10.1074/jbc.m603548200 摘要:Gaspar ML, Aregullin MA, Jesch SA, Henry SA. Inositol Induces a Profound Alteration in the Pattern and Rate of Synthesis and Turnover of Membrane Lipids in Saccharomyces cerevisiae. Journal of Biological Chemistry. 2006 Aug;281(32):22773–85. doi: 10.1074/jbc.m603548200. 参考文献:10.3402/ljm.v6i0.5870 摘要:Askoura M, Mattawa W, Abujamel T, Taher I. Efflux pump inhibitors (EPIs) as new antimicrobial agents against Pseudomonas aeruginosa. Libyan Journal of Medicine. 2011 Jan;6(1):5870. doi: 10.3402/ljm.v6i0.5870. 参考文献:10.1111/j.1600-6143.2004.00546.x 摘要:Chavin KD, Fiorini RN, Shafizadeh S, Cheng G, Wan C, Evans Z, Rodwell D, Polito C, Haines JK, Baillie GM, Schmidt MG. Fatty Acid Synthase Blockade Protects Steatotic Livers from Warm Ischemia Reperfusion Injury and Transplantation. American Journal of Transplantation. 2004 Sep;4(9):1440–7. doi: 10.1111/j.1600-6143.2004.00546.x. 参考文献:10.1194/jlr.m600329-jlr200 摘要:Schweitzer SC, Reding AM, Patton HM, Sullivan TP, Stubbs CE, Villalobos-Menuey E, Huber SA, Newell MK. Endogenous versus exogenous fatty acid availability affects lysosomal acidity and MHC class II expression. J Lipid Res. 2006 Nov;47(11):2525–37. doi: 10.1194/jlr.m600329-jlr200. 参考文献:10.1371/journal.pone.0002329 摘要:Zeng L, Wu GZ, Goh KJ, Lee YM, Ng CC, You AB, Wang J, Jia D, Hao A, Yu Q, Li B. Saturated fatty acids modulate cell response to DNA damage: implication for their role in tumorigenesis. PLoS One. 2008 Jun 04;3(6):e2329.