CAS: 50935-71-2; Kirromycin

专利信息

专利号:US-9625466-B2
优先权日:2011-04-06
标题 :Signal amplification methods for the imaging of protein synthesis and neurotransmitter transport
发明人：BLANCHARD SCOTT C; ALTMAN ROGER B
权利人:BLANCHARD SCOTT C; ALTMAN ROGER B; UNIV CORNELL
摘要:The present invention describes the synthesis of biological samples that can be used for the purpose of enhancing the signal-to-noise ratios achievable during the imaging of protein synthesis, amino acid transport and neurotransmitter transport, particularly in applications where single-molecule resolution is demanded. The present invention provides quencher-labeled elongation factor (EF-Tu) and fluorophore-labeled tRNA. When these molecules are present in a ternary complex with GTP, the fluorescently-labeled tRNA is quantitatively quenched. Once the tRNA is incorporated into an actively translating ribosome, however, a burst of fluorescence is released and can be detected by a variety of techniques, including smFRET imaging. The invention further provides novel EF-Tu constructs for achieving quencher labeling at high levels while retaining native or near native activity in the translation reactions, as well as methods for preparing stable ternary complexes, methods of protein sequencing, methods of detecting amino acid transport using a proteoliposome assay system and the proteoliposomes systems and methods of imaging translation events in single living cells. The present invention should have an immediate impact on next-generation sequencing technologies and the detection of neurotransmitter transporter activities in both in vitro and in vivo settings, a critical component of drug activity/screening assays targeting this important class of molecules.

专利号:US-9612244-B2
优先权日:2007-06-22
标题:Fluorescent labeling of transfer RNA and study of protein synthesis
发明人：COOPERMAN BARRY S; SMILANSKY ZEEV; GOLDMAN YALE E; PAN DONGLI
权利人:UNIV PENNSYLVANIA; ANIMA CELL METROLOGY INC
摘要:Provided are methods for labeling transfer RNA comprising replacing the uracil component of a dihydrouridine of said transfer RNA with a fluorophore. The disclosed methods may comprise fluorescent labeling of natural tRNAs (i.e., tRNAs that have been synthesized in a cell, for example, in a bacterium, a yeast cell, or a vertebrate cell) at dihydrouridine (D) positions, or fluorescent labeling of synthetic tRNAs. In another aspect, the present invention provides methods for assessing protein synthesis in a translation system comprise providing a tRNA having a fluorophore substitution for the uracil component of a dihydrouridine in a D loop of the tRNA; introducing the labeled tRNA into the translation system; irradiating the translation system with electromagnetic radiation, thereby generating a fluorescence signal from the fluorophore; detecting the fluorescence signal; and, correlating the fluorescence signal to one or more characteristics of the protein synthesis in the translation system. The disclosed methods are useful in single molecule as well as in ensemble settings.

专利号:US-10174358-B2
优先权日:2013-10-31
标题:Assay for identification of therapeutics targeting ternary complex formation in protein synthesis
发明人：MANDECKI WLODEK; GOLDMAN EMANUEL; CHUDAEV MAXIM
权利人:UNIV RUTGERS
摘要:The present invention provides a novel assay that allows high-throughput screening of chemical compounds for the inhibition of binding between EF-Tu and tRNA.

专利号:EP-0635577-B1
优先权日:1993-07-23
标 题 :Screen for inhibitors of melanin biosynthesis
发明人：BRINDLE FRANCES HARRIET ELIZAB; FROELIGER EUNICE HARRIET
权利人:BASF AG
摘要:A method for the identification of agents that inhibit melanin biosynthesis involves the incubation of test samples in cultures of a fungus that produces melanin. Observation of altered pigmentation in the culture or culture area containing test sample indicates inhibition of melanin biosynthesis. Preferred cultures for the screen contain a fungus that pigments in the light or the dark such as Cladosporium cucumerinum. Preferred embodiments employ test samples on disks or in wells in solidified cultures and a known melanin synthesis inhibitor as a positive control which is compared to the test sample by simple visual inspection.

专利号:US-6660832-B1
优先权日:1999-08-20
标题:Macrocyclic compounds and preparation methods thereof
发明人：JEFFERSON ELIZABETH; SWAYZE ERIC EDWARD
权利人:ISIS PHARMACEUTICALS INC
摘要:The present invention is directed to macrocyclic compounds of the formula (I)wherein Q, X, R1 and R5 are as defined herein. Compounds of the invention are useful for therapeutic and prophylactic treatment of bacterial infection in mammals. Solid phase synthetic procedures are provided effecting synthesis of the macrocyclic rings attached to a solid support.

专利号:US-2010204310-A1
优先权日:2008-09-12
标题:New modalities for treatment of drug-resistant tuberculosis and other diseases
发明人：ZAMECNIK PAUL C; PIERSON KAREN; TABATADZE DAVID
权利人:ZATA PHARMACEUTICALS INC
摘要:The invention provides antibacterial compounds comprising an oligonucleotide having a sequence complementary to a translation initiation region of an mRNA encoding a mycolyl transferase of Mycobacterum tuberculosis selected from protein 30, 32A and 32B, and further having 5′ and 3′ palindromic hairpin-forming sequences, said compound being covalently linked to a protein synthesis inhibiting antibiotic via a linker. The invention further provides pharmaceutical formulations of such compounds and methods of use thereof for treating tuberculosis. Other diseases may similarly be treated by tethering and antibiotic which targets a ribosomal protein to an antisense oligonucleotide complementary to an mRNA involved in the disease.