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D-生物素置于n-羟基丁二酰亚胺,N,N'-二环己基碳二亚胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 8.0H,反应生成(+)生物素-N-琥珀酰亚胺基酯
参考文献:用于探测nur77蛋白诱导途径的生物素化强心苷的设计与合成.
标题:用于探测nur77蛋白诱导途径的生物素化强心苷的设计与合成.
摘要:孤儿核受体nur77(也称为tr3或神经生长因子诱导的克隆b Ngfi-B)在调节靶基因表达中起核转录因子的作用,并且在分化,增殖,凋亡,和许多不同细胞类型的存活率 最近的研究表明,Nur77还涉及许多重要的生理和病理过程,包括癌症,炎症和免疫力,心血管疾病和骨骼疾病.我们以前的研究表明强心苷可以诱导nur77蛋白的表达及其从细胞核到细胞质的转运,然后靶向线粒体,从而导致癌细胞凋亡.为了探测nur77蛋白的诱导途径,我们设计并合成了一系列新型的生物素化的强心苷,它们分别来自β-安提香和α-安提香,这是两种来自安提阿里斯毒株的典型强心苷.评价了这些生物素化强心苷nur77蛋白表达的诱导及其对nih-H460癌细胞增殖的抑制作用.结果表明,一些生物素化的强心苷可以显着诱导nur77蛋白的表达,与它们的母体化合物β-Antiarin和α-Antiarin相当.而且,评估了它们的抗生蛋白链菌素结合
Doi:10.1016/j.Bmcl.2019.01.015

专利信息

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-2010304368-A1
优先权日:2006-09-20
标 题:Components and method for enzymatic synthesis of nucleic acids
发明人：CHERKASOV DMITRY; BAEUML ENGLEBERT; BAEUML ELISABETH
权利人:CHERKASOV DMITRY; BAEUML ENGLEBERT; BAEUML ELISABETH
摘要:Novel methods for enzymatic synthesis of nucleic acid chains and the substrates for the same are disclosed. The methods are based on a step-wise enzymatic reaction. The sequencing of nucleic acids is an example of the use of the claimed methods.

专利号:WO-2024186075-A1
优先权日:2023-03-03
标题 :Synthesis method of antibody-drug conjugates using proximity effect-based site-selective antibody labeling
发明人：LEE HYUN SOO; KIM SOOIN; KWEON YONGSEOK
权利人:UNIV SOGANG RES & BUSINESS DEVELOPMENT FOUND; RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIV
摘要:The present invention relates to a method for the synthesis of an antibody-drug conjugate using proximity effect-based site-selective antibody labeling. Provided according to the present invention may be a method for the synthesis of an antibody-drug conjugate by site-selectively introducing a drug into an antibody using a pyridinium oxime derivative (labeling mediator protein) introduced into a binding protein containing a non-standard amino acid.

专利号:US-6238875-B1
优先权日:1991-03-12
标题:Diagnostic methods useful in the characterization of lymphoproliferative disease characterized by increased EPR-1
发明人：ALTIERI DARIO C
权利人:SCRIPPS RESEARCH INST
摘要:A new class of cellular receptors extensively homologous but not identical to coagulation factors V and VIII is identified. These new cell surface receptors are designated effector cell protease receptors (EPRs) and include EPR-1, which is shown to bind protease ligands. The DNA and amino acid residue sequences of the receptor are also described. The invention also discloses methods, sequences and vectors useful in the purification and synthesis of cellular receptors of the present invention. n Antibody compositions capable of immunoreacting with the receptor or with polypeptides containing the identified amino acid residue sequences and related therapeutic and diagnostic protocols are also described, as are polypeptides, compositions and methods relating to the inhibition of T lymphocyte proliferation using the antibodies disclosed herein. The receptors are also demonstrated to bind coagulation factor Xa, which binding is inhibited by various disclosed monoclonal antibodies to the receptors. The present invention also discloses polypeptides, antibodies and compositions capable of stimulating or co-stimulating lymphocyte proliferation.

专利号:US-7338932-B2
优先权日:2000-05-11
标题 :Methods of modulating functions of polypeptide GalNAc-transferases and of screening test substances to find agents herefor, pharmaceutical compositions comprising such agents and the use of such agents for preparing medicaments
发明人：CLAUSEN HENRIK; BENNETT ERIC PAUL; HASSAN HELLE; REIS CELSO ALBUQUERQUE
权利人:GLYCOZYM APS
摘要:Attachment of O-glycans to proteins is controlled by a large family of homologous polypeptide GalNAc-transferases. Polypeptide GalNAc-transferases contain a C-terminal sequence with similarity to lectins. This invention discloses that the putative lectin domains of GalNAc-transferase isoforms, GalNAc-T4, -T7, -T2, and -T3, are functional and recognize carbohydrates, glycopeptides, and peptides and discloses the lectin domains of GalNAc-T1-T16. These lectin domains have different binding specificities and modulate the functions of GalNAc-transferase isoforms differently. Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the β-anomeric configuration of GalNAc-benzyl, GalNAcβ-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.

专利号:US-10029014-B2
优先权日:2013-09-10
标题:Synthesis of novel asymmetric bow-tie PAMAM dendrimer-based conjugates for tumor-targeting drug delivery
发明人：OJIMA IWAO; WANG TAO; TENG YU-HAN
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present disclosure relates to a dendrimer-based conjugate of the formula V m -D-C-D′-(T-F) n , which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.