- DNA-TEMPLATED MACROCYCLE LIBRARY
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The present invention provides nucleic acid templates (e.g., including orthogonal codon sets (e.g., codons from orthogonal codon sets depicted in Tables 5 or 7)) for DNA-templated methods of synthesizing, selecting, and amplifying compounds (e.g., polymers and/or small molecules) described herein. Also provided are novel macrocyclic compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, libraries, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing a disease (e.g., a disease associated with aberrant enzyme activity (e.g., aberrant protease and/or kinase activity (e.g., aberrant IDE activity)), impaired insulin signaling, or insulin resistance in a subject (e.g., a subject having diabetes). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit aberrant protease activity (e.g., aberrant IDE activity).
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Paragraph 00232; 00234
(2019/09/18)
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- Readily functionalizable phosphonium-tagged fluorescent coumarins for enhanced detection of conjugates by mass spectrometry
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Fluorescent coumarins are an important class of small-molecule organic fluorophores ubiquitous in different well-established and emerging fields of research including, among others, biochemistry and chemical biology. The present work aims at covering the poor detectability of coumarin-based conjugates by mass spectrometry while keeping important photophysical properties of the coumarin core. In this context, the synthesis of readily functionalizable phosphonium-tagged coumarin derivatives enabling a dual mass-tag and fluorescence labelling of analytes or (bio)molecules of interest through a single-step protocol, is reported. The utility of these coumarins is illustrated through the preparation of fluorogenic substrates that facilitated identification of the peptide fragment released by specific proteolytic cleavages.
- Lizzul-Jurse, Antoine,Bailly, Laetitia,Hubert-Roux, Marie,Afonso, Carlos,Renard, Pierre-Yves,Sabot, Cyrille
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supporting information
p. 7777 - 7791
(2016/08/24)
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- HAPTENS AND IMMUNOREACTIVE AGENTS AND USE THEREOF FOR PRODUCING FAMILY ANTIBODIES AND IMMUNOASSAYS FOR QUINOLONES
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The invention relates to haptens, immunogens and secondary immunoreactive agents, to the use thereof for producing wide-spectrum antibodies against quinolone-type antibiotics, to the application thereof to immunochemical analysis techniques, and to a kit enabling the detection of said antibiotics in biological samples from food products of animal origin.
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Page/Page column 0092; 0111-0112; 0114
(2013/10/22)
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- Rifamycins as inhibitors of retroviral reverse transcriptase from M-MuLV, RAV-2, and HIV-1
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29 Rifamycins were tested for inhibition of Reverse Transcriptase (RT) as potential anti HIV drugs. Two purified commercial enzymes from M-MuLV and RAV-2 were used. Anti-RT activity was also measured on a crude lysate of HIV-1. The results show that some derivatives have interesting levels of activity on isolated M-MuLV and RAV-2 RTs, while they are less active on the RT in the crude HIV-1 lysate. The active derivatives include oximes and hydrazones, alkylaminoderivatives, open ansa-chain derivatives and derivatives carrying a modified nucleoside.
- Bartolucci,Cellai,Di Filippo,Segre,Brufani,Filocamo,Bianco,Guiso,Brizzi,Benedetto,Di Caro,Elia
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p. 1367 - 1383
(2007/10/02)
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