专利号:US-6451543-B1 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:GRYPHON SCIENCES 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
专利号:US-7482425-B2 优先权日:1999-08-26 标题:Compositions for lipid matrix-assisted chemical ligation 发明人:KOCHENDOERFER GERD G; HUNTER CHRISTIE L; KENT STEPHEN B H; BOTTI PAOLO 权利人:AMYLIN PHARMACEUTICALS INC 摘要:The present invention relates to methods and compositions for lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides that are incorporated in a lipid matrix. The invention is exemplified in production of a prefolded membrane polypeptide embedded within a lipid matrix via stepwise chemoselective chemical ligation of unprotected peptide segments, where at least one peptide segment is embedded in a lipid matrix. Any chemoselective reaction chemistry amenable for ligation of unprotected peptide segments can be employed. Suitable lipid matrices include liposomes, micelles, cell membrane patches and optically isotropic cubic lipidic phase matrices. Prefolded synthetic and semi-synthetic membrane polypeptides synthesized according to the methods and compositions of the invention also permit site-specific incorporation of one or more detectable moieties, such as a chromophore, which can be conveniently introduced during synthesis. The methods and compositions of the invention have multiple uses. For example, they can be used to assay ligand binding to membrane polypeptides and domains comprising a receptor, and thus are extremely useful for structure/function studies, drug screening/selection/design, and diagnostics and the like, including high-throughput applications. The methods and compositions of the invention are particularly suited for FRET analyses of previously inaccessible membrane polypeptides.
专利号:WO-2023031623-A2 优先权日:2021-09-03 标 题 :Synthesis of bicycle toxin conjugates, and intermediates thereof
专利号:US-2003018169-A1 优先权日:1999-08-26 标 题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides
参考文献:10.1007/s00203-002-0404-8 摘要:Miller SR, Martin M, Touchton J, Castenholz RW. Effects of nitrogen availability on pigmentation and carbon assimilation in the cyanobacterium Synechococcus sp. strain SH-94-5. Arch Microbiol. 2002 May;177(5):392–400. doi: 10.1007/s00203-002-0404-8. 参考文献:10.1110/ps.03542104 摘要:De Filippis V, De Boni S, De Dea E, Dalzoppo D, Grandi C, Fontana A. Incorporation of the fluorescent amino acid 7-azatryptophan into the core domain 1-47 of hirudin as a probe of hirudin folding and thrombin recognition. Protein Sci. 2004 Jun;13(6):1489–502. 参考文献:10.1111/j.1751-1097.1999.tb08275.x|10.1562/0031-8655(1999)070<0719:fportc>2.3.co;2 摘要:Das K, Ashby KD, Smirnov AV, Reinach FC, Petrich JW, Farah CS. Fluorescence Properties of Recombinant Tropomyosin Containing Tryptophan, 5‐Hydroxytryptophan and 7‐Azatryptophan. Photochem & Photobiology. 1999 Nov;70(5):719–30. doi: 10.1111/j.1751-1097.1999.tb08275.x.