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-8314209-B2 优先权日:2007-12-12 标 题 :Lipid-assisted synthesis of polymer compounds and methods for their use 发明人:RAJAMANI SUDHA; OLASAGASTI FELIX; DEAMER DAVID W; BENNER SEICO 权利人:RAJAMANI SUDHA; OLASAGASTI FELIX; DEAMER DAVID W; BENNER SEICO; UNIV CALIFORNIA 摘要:The invention herein disclosed provides for methods for the synthesis of polymers from monomers. In particular the method provides for the synthesis of polynucleotides from mononucleotides in the absence of catalytic enzymes. The method comprises providing an aqueous solution having a plurality of phospholipid molecules and monomer molecules; subjecting the aqueous solution to fluctuating temperature conditions; subjecting the aqueous solution to fluctuating cycles of drying and hydrating conditions; subjecting the aqueous solution to fluctuating [H + ] conditions; the fluctuating conditions thereby allowing formation of a chemical bond between at least two monomers to create a polymer. The invention is of particular use in the fields of molecular biology, structural biology, cell biology, molecular switches, molecular circuits, and molecular computational devices, and the manufacture thereof.
专利号:US-6171614-B1 优先权日:1996-10-15 标 题 :Synthesis of glycophospholipid and peptide-phospholipid conjugates and uses thereof 发明人:CHAIKOF ELLIOT L; SUN LIJUN 权利人:UNIV EMORY 摘要:The present invention provides glycophospholipid and peptide-phospholipid conjugates comprising a phospholipid moiety and a saccharide or peptide moiety joined by an ether linkage comprising a secondary or tertiary amine. The conjugate structure of the invention comprises a flexible spacer arm between the phospholipid and saccharide or peptide moieties which, being variable in length, serves to optimize saccharide or peptide bioactivity. This invention further provides a method for the synthesis of such conjugates comprising the step of reductive amination. The method is efficient, economical and provides a high yield of product. Glycophospholipid and peptide-phospholipid conjugates of the invention can be incorporated and, optionally, chemically polymerized in self-assembling systems such as membranes, bilayers, films, liposomes and the like, and find utility diagnostically and therapeutically in medical and immuno-biological applications.
专利号:US-2013302247-A1 优先权日:2012-05-09 标 题:Synthesis of fluoroarachidonic acid and methods of use thereof 发明人:PICHIKA RAMAIAH; ECKELMAN WILLIAM C; RAPOPORT STANLEY I; TAHA AMEER; KOTTA KISHORE 权利人:US HEALTH; UNIV CALIFORNIA 摘要:There are provided, inter alia, methods for diagnosis of the extent of neuroinflammation in a subject. The methods include administering an 18 F-labeled arachidonic acid to a subject in need thereof, obtaining a positron emission tomography (PET) scan of the subject, and determine the extent of neuroinflammation from the PET scan. There are provided, inter alia, methods of synthesis of reagents useful for the production of an 18 F-labeled arachidonic acid.
专利号:WO-2021126118-A1 优先权日:2019-12-20 标 题:Synthesis of 2-(substitutedphenyl)-5-(substitutedheteroaryl)- 1h-benzimidazole derivatives and investigation of their biological effects 发明人:KAPLANCIKLI ZAFER ASIM; ÖZKAY YUSUF; ACAR ÇEVİK ULVIYE; SAÄžLIK BEGÜM NURPELIN; OSMANİYE DERYA; LEVENT SERKAN; KAYA ÇAVUÅžOÄžLU BETÜL; ATLI EKLİOÄžLU ÖZLEM; KARADUMAN ABDULLAH BURAK 权利人:ANADOLU UENIVERSITESI 摘要:The invention is related to the synthesis of 2-((5-(2-(4-Substitutedphenyl)-1H-benzo[d]imidazole-6-yl)-1,3,4-oxadiazole-2-yl)thio)-1-(4substitutedpiperazine-1-yl)-ethane-1-one derivative compounds and investigation of their biological effects. Cytotoxicity of the obtained compounds on 5 different cancer cell lines was evaluated and their selectivity indices were calculated.
专利号:US-6217901-B1 优先权日:1999-05-25 标题:Liposome-assisted synthesis of polymeric nanoparticles 发明人:PERROTT MICHAEL G; BARRY STEPHEN E 权利人:ALNIS LLC 摘要:Synthetic polymer complements (SPCs) are provided, as well as methods for their synthesis and use. The SPCs range in size from about 20 to about 1000 nm. The SPCs have surfaces that are complementary to surface sites of target molecules, resulting in the ability of the SPCs to selectively bind to molecular targets. The molecular recognition capability of these particles enables their use in diagnostic, therapeutic, and separation applications. The SPC is formed by contacting a target template molecule with a set of building blocks solubilized in the interior of a liposome, which building blocks are then polymerized into a network to form the synthetic polymer complement in the interior of the liposome. The target templates are removed to produce complementary sites in a SPC that map the surface of the target, resulting in a water-soluble SPC nanoparticle of similar dimensions as the interior of the liposome that originally supported it and capable of molecular recognition.