247193-74-4Relevant academic research and scientific papers
Selective cleavage of the HIV-1 TAR-RNA with a peptide-cyclen conjugate
Michaelis, Katrin,Kalesse, Markus
, p. 2243 - 2245 (1999)
Covalent linkage of the arginine-rich fragment of the Tat protein to 1,4,7,10-tetraazacyclododecane (cyclen) results in the selective cleavage of the TAR-RNA of HIV-1 (see picture; the biotin at the 5' end acts as a label for the subsequent analysis of the cleavage fragments). The cleavage occurs at room temperature and is diminished when Eu(III) ions are present - at a concentration of about 1/10 of the concentration of the peptide-cyclen conjugate. The pH dependence indicates that two ammonium ions are responsible for the cleavage reaction. The white arrows in the schematic diagram mark the cleavage sites in RNaseT1, and the black arrows the sites in the peptide- cyclen conjugate.
Neomycin B-cyclen conjugates and their Zn(II) complexes as RNA-binding agents
Kong, Bopha,Joshi, Tanmaya,Belousoff, Matthew J.,Tor, Yitzhak,Graham, Bim,Spiccia, Leone
, p. 334 - 342 (2016)
Three new conjugates featuring the aminoglycoside antibiotic neomycin B linked to the 1,4,7,10-tetraazacyclododecane (cyclen) macrocycle via alkyl chains of varying lengths were synthesized from suitably protected derivatives of these precursors via conve
ANTIBACTERIAL COMPOUNDS
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Page/Page column 42; 45, (2014/10/15)
The invention relates to antibacterial compounds, methods for synthesis and use thereof in antibacterial applications.
Zinc(II)cyclen-peptide conjugates interacting with the weak effector binding state of Ras
Schmidt, Florian,Rosnizeck, Ina C.,Spoerner, Michael,Kalbitzer, Hans Robert,K?nig, Burkhard
experimental part, p. 38 - 48 (2011/03/22)
Zinc(II)cyclen-peptide hybrid compounds and bis-zinc(II)cyclen complexes are prepared as potential binders of the guanine nucleotide binding protein Ras, an important molecular switch in cellular signal transduction. The design of the compounds is based on the previous observation that zinc(II)cyclen complexes could serve as lead compounds for inhibitors of Ras-effector interaction and thus be able to interrupt Ras induced signal transduction. Zinc(II)cyclen selectively stabilizes conformational state 1 of active Ras, a conformational state with drastically decreased affinity to effector proteins like Raf-kinase. To achieve higher binding affinities of such Ras-Raf interaction inhibitors, zinc(II)cyclen conjugates with short peptides, derived from the sequence of the Ras-activator SOS, were prepared by solid phase synthesis protocols. Dinuclear bis-zinc(II)cyclen complexes were obtained from alkyne-azide cycloaddition reactions. NMR investigations of the prepared compounds revealed that the peptide conjugates do not lead to an increase in Ras binding affinity of the metal complex-peptide conjugates. The dinuclear zinc complexes lead to an immediate precipitation of the protein prohibiting spectroscopic investigations of their binding.
Protein-cleaving catalyst selective for protein substrate
Jeon, Joong Won,Son, Sang Jun,Yoo, Chang Eun,Hong, In Seok,Song, Jung Bae,Suh, Junghun
, p. 4155 - 4158 (2007/10/03)
(matrix presented) A protein-cleaving catalyst specific for a disease-related protein can be used as a catalytic drug. As the first protein-cleaving catalyst selective for a protein substrate, a catalyst for myoglobin was designed by attaching Cu(II) or C
Synthetic catalyst for selective cleavage of protein and method for selective cleavage of protein using the same
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, (2008/06/13)
The present invention relates to a synthetic catalyst of the following formula (A) which can selectively recognize and cleave a specific protein among a protein mixture, and to a method for selective cleavage of a target protein using the same: (R)(Z)sub
