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:WO-2009080631-A2 优先权日:2007-12-21 标 题 :Chemo-enzymatic synthesis of a c-terminal aryl amide of an amino acid or peptide 发明人:QUAEDFLIEG PETER JAN LEONARD MARIO; NUIJENS TIMO; CUSAN CLAUDIA 权利人:DSM IP ASSETS BV; QUAEDFLIEG PETER JAN LEONARD MARIO; NUIJENS TIMO; CUSAN CLAUDIA 摘要:The present invention relates to a method for preparing an aryl amide, comprising reacting an aryl amine with a compound selected from N-protected amino acids and optionally N-protected peptides in the presence of a hydrolytic enzyme. The invention further relates to the use of a compound obtained in a method according to the invention in the manufacture of a diagnostic. In addition the invention relates to the use of a compound obtained in a method according to the invention as a substrate for a proteolytic enzyme.
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:US-2003018169-A1 优先权日:1999-08-26 标 题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides
专利号:JP-2002527358-A 优先权日:1998-08-31 标题:Lipid matrix assisted chemical ligation method and synthesis of membrane polypeptide
专利号:EP-1107979-A2 优先权日:1998-08-31 标题:Lipid matrix-assisted chemical ligation and synthesis of membrane polypeptides
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