专利号:US-8273790-B2 优先权日:2005-01-14 标 题:Exo-selective synthesis of himbacine analogs 发明人:THIRUVENGADAM TIRUVETTIPURAM K; SUDHAKAR ANANTHA; LIM NGIAP KIE; KWOK DAW-IONG; WU GEORGE G; WANG TAO; HUANG MINGSHENG; GREEN MICHAEL D 权利人:THIRUVENGADAM TIRUVETTIPURAM K; SUDHAKAR ANANTHA; LIM NGIAP KIE; KWOK DAW-IONG; WU GEORGE G; WANG TAO; HUANG MINGSHENG; GREEN MICHAEL D; SCHERING CORP 摘要:This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence:
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-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-2007122842-A1 优先权日:2005-11-30 标题 :Massively parallel synthesis of proteinaceous biomolecules 发明人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 权利人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 摘要:Methods for fabricating dense arrays of polymeric molecules in a highly multiplexed manner are provided using semiconductor-processing-derived lithographic methods. Advantageously, the methods are adaptable to the synthesis of a variety of polymeric compounds. For example, arrays of peptides and polymers joined by peptide bonds may be fabricated in a highly multiplexed manner.
专利号:US-4242256-A 优先权日:1977-03-15 标 题 :Synthesis of peptide analogues 发明人:SHARPE ROBERT; SZELKE MICHAEL 权利人:SHARPE ROBERT; SZELKE MICHAEL 摘要:Compounds being analogues of a dipeptide in which the nitrogen atom of the linking amide group of the dipeptide is replaced by trivalent group ##STR1## and in which, optionally, the carbonyl function of this linking group is replaced by the divalent group --CH 2 -- are of value in the synthesis of isosterically modified peptides.
专利号:US-2007122841-A1 优先权日:2005-11-30 标题:Massively parallel synthesis of proteinaceous biomolecules 发明人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 权利人:RAJASEKARAN JOHN J; TIWARI GUNJAN; CABEZAS EDELMIRA; FIDANZA JACQUELINE A; SUNDARARAJAN NARAYAN 摘要:Methods for fabricating dense arrays of polymeric molecules in a highly multiplexed manner are provided using semiconductor-processing-derived lithographic methods. Advantageously, the methods are adaptable to the synthesis of a variety of polymeric compounds. For example, arrays of peptides and polymers joined by peptide bonds may be fabricated in a highly multiplexed manner.
摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 401. 摘要:Personal Communication from G.D. Stoner, Dept. of Community Medicine, School of Medicine, Univ. of California, La Jolla, CA 92037, May 25, 1975, 27MAY1975 摘要:W. P. Jencks and J. Carriuolo. J. Biol. Chem. 234, 1272 (1959). 参考文献:10.1007/s00726-008-0048-3 摘要:Patkar KA, Highsmith WE, Aldrich JV. Solid phase and solution synthesis of NvocLys(CO(CH2)5NH-NBD)OCH2CN, a trifunctional fluorescent lysine derivative. Amino Acids. 2009 Feb;36(2):203–7. doi: 10.1007/s00726-008-0048-3. 参考文献:10.1007/bf02979154 摘要:Seo SK, Liu XW, Lee HJ, Kim HK, Kim MR, Sok DE. Regulation and inactivation of brain phosphocholine-phosphatase activity. Arch Pharm Res. 1999 Oct;22(5):464–73. doi: 10.1007/bf02979154.