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-0100609-A1 优先权日:1999-06-29 标题:Method for synthesis of n-homocysteine thiolactonyl retinamide 发明人:KAZIMIR MICHAEL; WILSON RAY E II 权利人:UNIV BAYLOR; KAZIMIR MICHAEL; WILSON RAY E II 摘要:The present invention describes methods of synthesis for N-homocysteine thiolactonyl retinamide (thioretinamide), a compound that has anticancer and antiatherogenic properties. The present invention further describes methods for the synthesis of N-homocysteine thiolactonyl retinamido cobalamin (thioretinaco), a compound that has potential anticancer, antineoplastic, antiviral, and antiatherogenic properties.
专利号:US-2024082435-A1 优先权日:2021-02-26 标 题 :Solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates and their use as precursors for therapeutic and/or diagnostic agents 发明人:PINTO ARTUR; BONTEMPS ALEXIS; LEMAIRE LUCAS 权利人:TELIX INT INNOVATIONS PTY LTD 摘要:The disclosure provides methods for the solid phase synthesis of glutamate-urea-lysine derived (GUL derived) prostate-specific membrane antigen (PSMA) targeting conjugates. The disclosure also relates to key intermediates of this process and methods for their preparation such as a method of preparing a compound of formula (V). Also disclosed are use of the conjugates as precursors for therapeutic and/or diagnostic agents, including treating and diagnosing prostate cancer.
专利号:US-2024240209-A1 优先权日:2021-04-20 标 题:Synthesis of enantiopure cis-a-irone from a renewable carbon source 发明人:CHEN XIXIAN; ZHANG CONGQIANG; T REHKA; SHUKAL SUDHA; SMITH DEREK; ANDRÉ ISABELLE; JEREMY ESQUE 权利人:AGENCY SCIENCE TECH & RES; INSTITUT NATIONAL DE RECH POUR L AGRICULTURE LALIMENTATION ET LENVIRONMENT; CENTRE NAT RECH SCIENT; INSTITUT NAT DES SCIENCES APPLIQUEES DE TOULOUSE 摘要:Synthesis of enantiopure cis-α-irone from a renewable carbon source Disclosed herein are natural and synthetic enzymes capable of performing a method of producing cis-α-irone. The method comprises providing an enzyme capable of converting psi-ionone to cis-α-irone; and contacting the enzyme and psi-ionone under suitable conditions to produce cis-α-irone. The enzyme may be a methyltransferase from Streptomyces albireticuli (SaMT), a promiscuous bifunctional methyltransferase/cyclase (pMT1) enzyme from Streptomyces, or a modified pMT1 enzyme with at least one substitution. The enzymes allow the in-vivo and in-vitro production of cis-α-irone including the use of glucose as feedstock for the biotransformation into cis-α-irone.
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