📜L-酪氨酸置于四磷十氧化物,磷酸体系中,化学反应 26.0H,以67%的收率获得l-磷酸酪氨酸 参考文献:Synthesis Of Six Phenylalanine Derivatives And Their Cell Toxicity Effect On Human Colon Cancer Cell Line Ht-29 标题:Synthesis Of Six Phenylalanine Derivatives And Their Cell Toxicity Effect On Human Colon Cancer Cell Line Ht-29 摘要:一些苯丙氨酸(phe)衍生物在药理学中具有重要作用,并可能用作药物原料和药物中间体.为了解苯丙氨酸衍生物的细胞毒性,我们合成了l-4-溴苯丙氨酸(brp),L-4-碘苯丙氨酸(ip),L-4-硝基苯丙氨酸(np),L-4-磺酸苯丙氨酸(sp),L-4-磷酸苯丙氨酸(pp)和l-4-氨基苯丙氨酸(np).我们通过质谱(ms),红外光谱(ir)或氢-1核磁共振谱(1H-NMR)以及高效液相色谱(HPLC)检测这些产品的正确性,Mtt法和hoechst33258染色检测它们对人结肠癌ht-29细胞的细胞毒性效应.结果显示,这些产品是正确的,Pp,Ip,Sp和np的细胞毒性对ht-29细胞基本无影响.此外,Pp,Ip和sp诱导细胞凋亡,其他三种苯丙氨酸衍生物既不诱导凋亡也不诱导坏死. Doi:10.2174/1570180812666141206001604
专利号:US-2020010502-A1 优先权日:2018-07-05 标题 :Synthesis of multiphosphorylated peptides 发明人:FRIEDLER ASSAF; MAMDI SAMARA SIMHA REDDY; HUREVICH MATTAN 权利人:YISSUM RES DEV CO OF HEBREW UNIV JERUSALEM LTD 摘要:The present invention relates to a new approach for the synthesis of multiphosphorylated peptides. Specifically, the present invention provides a process, which enables the synthesis of multiphosphorylated peptides with up to seven phosphorylated Serine (pSer) and Threonine (pThr) residues, including such residues that are close in sequence.
专利号:US-7301006-B2 优先权日:2002-07-16 标 题 :Methods and materials for the synthesis of modified peptides 发明人:YOUNG TRAVIS G; KIESSLING LAURA L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.
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-5977301-A 优先权日:1992-09-24 标题 :Synthesis of N-substituted oligomers 发明人:ZUCKERMAN RONALD N; KERR JANICE M; KENT STEPHEN B H; MOOS WALTER H; SIMON REYNA J; GOFF DANE A 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.
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-2024199310-A1 优先权日:2023-03-31 标 题 :Method for enzymatic synthesis of capped mrna in one tube 发明人:LI YALI; ZHU HUAXING; ZHANG QINGYI 权利人:NOVOPROTEIN SCIENT INC 摘要:Provided is a method for enzymatic synthesis of capped mRNA in one tube. In the method, the step of purifying mRNA after IVT is omitted, and a capped product having a higher capping efficiency and fewer by-products is obtained. The method provided for enzymatic synthesis of capped mRNA is simple, convenient and short in terms of the process, and is rapid and efficient, so that the production process of a capped mRNA product is simplified, and a production cost is reduced, which is conducive to industrial production.
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合成参考文献
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