专利号:US-2013224804-A1 优先权日:2010-09-01 标 题 :Expression of steady state metabolic pathways 发明人:KNIGHT ERIC 权利人:KNIGHT ERIC 摘要:The present disclosure pertains to a method for increasing the production of a desired product having: identifying a steady state metabolic pathway for the synthesis of a desired product from a desired substrate; producing a polynucleotide encoding one or more polypeptide that participates in the steady state metabolic pathway for the synthesis of the desired product from the desired substrate; introducing the polynucleotide encoding a polypeptide into a host cell; transforming a host cell with an expression vector having an expressible polynucleotide encoding a polypeptide; and cultivating the host cell under a culture condition that induces the production of the desired product.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-11919928-B2 优先权日:2016-03-16 标题 :Method for producing dihydrotentoxin 发明人:KUBO TAKASHI; MACHIDA MASAYUKI; FUJIOKA TOMONORI; YAMAGUCHI Shigenari; KAWAI KIYOSHI 权利人:KUMIAI CHEMICAL INDUSTRY CO 摘要:An object of the present invention is to identify an enzyme having activity of synthesizing dihydrotentoxin that is a tentoxin precursor and an enzyme having activity of synthesizing tentoxin using dihydrotentoxin as a substrate. The present invention concerns a tentoxin synthesis-related gene encoding a protein comprising the amino acid sequence of SEQ ID NO: 16 and having activity of nonribosomal peptide synthesis of dihydrotentoxin and a tentoxin synthesis-related gene encoding a protein comprising the amino acid sequence of SEQ ID NO: 18 and having activity of converting dihydrotentoxin to tentoxin.
专利号:EP-0869784-B1 优先权日:1995-11-17 标 题:Inhibition of fatty acid synthase as a means to reduce adipocyte mass 发明人:KUHAJDA FRANCIS P; PASTERNACK GARY R; TOWNSEND CRAIG A; MANI NEELAKANDHA S 权利人:UNIV JOHNS HOPKINS 摘要:Weight loss was noted in nude mice treated with cerulenin, a non-competitive inhibitor of FAS. Sustained reduction of adipocyte mass in humans without toxicity would significantly impact disease prevention worldwide. Aside from psychological and self-esteem improvement, weight loss via reduction of adipocyte mass may: (1) ameliorate hyperglycemia associated with non-insulin-dependent diabetes mellitus thereby reducing diabetic complications such as arterial disease, blindness, cataracts, etc., (2) reduce hypertension, (3) reduce risk of coronary artery vascular disease and stroke, and (4) reduce the risk of other complications of massive obesity such as osteoarthritis, surgical complications, etc. There is also potential use in livestock and poultry to reduce the saturated fat content of meat products. Therefore FAS inhibitors are disclosed herein as novel agents for weight reduction. A family of compounds ( gamma -substituted- alpha -methylene- beta -carboxy- gamma -butyrolactones) whose synthesis was based on the cerulenin motif is shown herein to inhibit fatty acid synthesis, inhibit growth in certain susceptible tumor cells, and induce weight loss.
专利号:US-5981575-A 优先权日:1996-11-15 标 题 :Inhibition of fatty acid synthase as a means to reduce adipocyte mass 发明人:KUHAJDA FRANCIS P; PASTERNACK GARY R; TOWNSEND CRAIG A; MANI NEELAKANDHA S 权利人:UNIV JOHNS HOPKINS 摘要:Weight loss was noted in nude mice treated with cerulenin, a non-competitive inhibitor of FAS. Sustained reduction of adipocyte mass in humans without toxicity would significantly impact disease prevention worldwide. Aside from psychological and self-esteem improvement, weight loss via reduction of adipocyte mass may: (1) ameliorate hyperglycemia associated with non-insulin-dependent diabetes mellitus thereby reducing diabetic complications such as arterial disease, blindness, cataracts, etc., (2) reduce hypertension, (3) reduce risk of coronary artery vascular disease and stroke, and (4) reduce the risk of other complications of massive obesity such as osteoarthritis, surgical complications, etc. There is also potential use in livestock and poultry to reduce the saturated fat content of meat products. Therefore FAS inhibitors are disclosed herein as novel agents for weight reduction. A family of compounds (γ-substituted-α-methylene-β-carboxy-γ-butyrolactones) whose synthesis was based on the cerulenin motif is shown herein to inhibit fatty acid synthesis, inhibit growth in certain susceptible tumor cells, and induce weight loss.
专利号:CN-119979591-A 优先权日:2025-01-06 标 题 :Method for regulating and controlling synthesis of cis-catechin of tea tree based on CsAHL gene and application
1: Henderson CJ, Cameron AR, Chatham L, Stanley LA, Wolf CR. Evidence that the capacity of nongenotoxic carcinogens to induce oxidative stress is subject to marked variability. Toxicol Sci. 2015 May;145(1):138-48. doi: 10.1093/toxsci/kfv039. Epub 2015 Feb 17. 2: Wahlang B, Falkner KC, Clair HB, Al-Eryani L, Prough RA, States JC, Coslo DM, Omiecinski CJ, Cave MC. Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture. Toxicol Sci. 2014 Aug 1;140(2):283-97. doi: 10.1093/toxsci/kfu083. Epub 2014 May 8. 3: Mogilenko DA, Dizhe EB, Shavva VS, Lapikov IA, Orlov SV, Perevozchikov AP. Role of the nuclear receptors HNF4 alpha, PPAR alpha, and LXRs in the TNF alpha-mediated inhibition of human apolipoprotein A-I gene expression in HepG2 cells. Biochemistry. 2009 Dec 22;48(50):11950-60. doi: 10.1021/bi9015742. doi: 10.1016/j.tiv.2009.07.027. Epub 2009 Jul 30. Epub 2007 Dec 13.
合成参考文献
参考文献:10.1155/2011/937843 摘要:Shirinsky IV, Shirinsky VS. Targeting Nuclear Hormone Receptors: PPARαAgonists as Potential Disease-Modifying Drugs for Rheumatoid Arthritis. International Journal of Rheumatology. 2011;2011():1–8. doi: 10.1155/2011/937843.