专利号:US-4753985-A 优先权日:1981-10-07 标题 :Synthesis of organic compounds using deformable gel in porous rigid support 发明人:ROSEVEAR ALAN; SHEPPARD ROBERT C 权利人:ATOMIC ENERGY AUTHORITY UK 摘要:The present invention relates to the synthesis of chemical compounds and more particularly to the synthesis of organic compounds, for example, peptides and oligonucleotides. n The invention provides a composite material for use in the synthesis of organic compounds comprising a support material and, supported on the support material, an organic compound synthesizing substance. n It is preferred that the organic compound synthesizing substance is a gel (e.g. a dimethylacrylamide co-polymer gel). n The invention also provides a method for preparing a composite material for use in the synthesis of organic compounds and a method for the synthesis of organic compounds.
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-12188072-B2 优先权日:2018-03-19 标题 :Compositions and methods for rapid in vitro synthesis of bioconjugate vaccines in vitro via production and N-glycosylation of protein carriers in detoxified prokaryotic cell lysates 发明人:JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN 权利人:UNIV NORTHWESTERN; UNIV CORNELL 摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated carrier proteins. The glycosylated carrier proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated carrier proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated carrier proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.
专利号:US-12365930-B2 优先权日:2016-07-14 标题:Method for rapid in vitro synthesis of glycoproteins via recombinant production of N-glycosylated proteins in prokaryotic cell lysates 发明人:JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN 权利人:UNIV NORTHWESTERN; UNIV CORNELL 摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated proteins. The glycosylated proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.
专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-2023313255-A1 优先权日:2020-07-15 标题:Massively Parallel Enzymatic Synthesis of Polynucleotides 发明人:HORGAN ADRIAN; LACHAIZE HENRI; VERARDO DOMIANO; GODRON XAVIER 权利人:DNA SCRIPT 摘要:The invention is directed to methods and compositions for inkjet assisted synthesis of a plurality of polynucleotides at reaction sites on a substrate using template-free polymerases, such as, terminal deoxynucleotidyl transferases (TdTs). Compositions of the invention include formulations of synthesis reagents for inkjet delivery including, but not limited to, TdT coupling reaction buffers and 3′-O-protected dNTP monomers.
1: Palanirajan SK, Gummadi SN. Rapid method for an enhanced recovery of biologically active human phospholipid scramblase1 from inclusion bodies. Anal Biochem. 2018 Jun 29. pii: S0003-2697(18)30603-1. doi: 10.1016/j.ab.2018.06.028. [Epub ahead of print] doi: 10.1016/j.jinorgbio.2018.06.009. [Epub ahead of print] doi: 10.1016/j.ejmech.2018.05.052. [Epub ahead of print] doi: 10.1016/j.jep.2018.05.015. Epub 2018 May 17. doi: 10.1021/acs.joc.8b00169. Epub 2018 May 29. doi: 10.1021/acssynbio.8b00093. Epub 2018 May 25. doi: 10.12659/MSM.909949. 16: Flores FM, Torres Sánchez RM, Dos Santos Afonso M. Some aspects of the adsorption of glyphosate and its degradation products on montmorillonite. Environ Sci Pollut Res Int. 2018 Jun;25(18):18138-18146. doi: 10.1007/s11356-018-2073-4. Epub 2018 Apr 25. doi: 10.1016/j.ejpb.2018.04.021. Epub 2018 Apr 20. doi: 10.1039/c8an00425k. Plant Physiol Biochem. 2018 Jun;127:248-255. doi: 10.1016/j.plaphy.2018.03.032. Epub 2018 Mar 30. doi: 10.1016/j.enzmictec.2018.02.010. Epub 2018 Mar 1.
合成参考文献
摘要:HANSCH,C ET AL. (1995) 参考文献:10.1016/j.bbrc.2014.05.064 摘要:Luka Z, Pakhomova S, Loukachevitch LV, Newcomer ME, Wagner C. Folate in demethylation: The crystal structure of the rat dimethylglycine dehydrogenase complexed with tetrahydrofolate. Biochemical and Biophysical Research Communications. 2014 Jul;449(4):392–8. doi: 10.1016/j.bbrc.2014.05.064. 参考文献:10.1515/cclm.2003.248 摘要:Boulat O, Gradwohl M, Matos V, Guignard JP, Bachmann C. Organic acids in the second morning urine in a healthy Swiss paediatric population. Clin Chem Lab Med. 2003 Dec;41(12):1642–58. doi: 10.1515/cclm.2003.248.