210355-19-4Relevant academic research and scientific papers
Design and synthesis of new cationic water-soluble pyrene containing dendrons for DNA sensory applications
Chen, Ching-Yi,Ito, Yumiko,Chiu, Yu-Cheng,Wu, Wen-Chung,Higashihara, Tomoya,Ueda, Mitsuru,Chen, Wen-Chang
, p. 297 - 305 (2012)
A series of new water-soluble cationic pyrene-dendron derivatives, G1, G2, and G3, was successfully synthesized and characterized. These new dendrons were designed with the quaternized amino moieties at the periphery of the dendrons for DNA detection and functionalized with pyrene as a fluorescent probe. The electrostatic interactions between the plasmid DNA (pDNA) and cationic charged dendrons in an aqueous solution resulted in a change in the photophysical properties of pyrene, which could be shown in the UV-vis and fluorescence spectra. Pyrene dendrons showed a high and rapid fluorescence response upon the addition of pDNA, which was strongly dependent on the size and hydrophobicity of the dendrons.
A Guanidyl-Based Bivalent Peptidomimetic Inhibits K-Ras Prenylation and Association with c-Raf
Tsubamoto, Mai,Le, Toan Khanh,Li, Minghua,Watanabe, Taku,Matsumi, Chiemi,Parvatkar, Prakash,Fujii, Hiroshi,Kato, Nobuo,Sun, Jiazhi,Ohkanda, Junko
supporting information, p. 13531 - 13536 (2019/10/28)
Unusual lipid modification of K-Ras makes Ras-directed cancer therapy a challenging task. Aiming to disrupt electrostatic-driven protein–protein interactions (PPIs) of K-Ras with FTase and GGTase I, a series of bivalent dual inhibitors that recognize the active pocket and the common acidic surface of FTase and GGTase I were designed. The structure-activity-relationship study resulted in 8 b, in which a biphenyl-based peptidomimetic FTI-277 was attached to a guanidyl-containing gallate moiety through an alkyl linker. Cell-based evaluation demonstrated that 8 b exhibited substantial inhibition of K-Ras processing without apparent interference with Rap-1A processing. Fluorescent imaging showed that 8 b disrupts localization of K-Ras to the plasma membrane and impairs interaction with c-Raf, whereas only FTI-277 was found to be inactive. These results suggest that targeting the PPI interface of K-Ras may provide an alternative method of inhibiting K-Ras.
Synthesis of novel dendrimers incorporating a dye into the core
Zhang, Jidong,Drugeon, Gérémy,L'hermite, Nathalie
, p. 3599 - 3601 (2007/10/03)
Dendrimers 1a and 1b, with six and nine terminal tert-butyloxycarbonyl (t-Boc) protected amine groups, respectively, have been prepared by an efficient divergent synthetic approach. These novel dendrimers contain a dye Red-1 incorporated into the core, which adds to them, in addition to their physicochemical properties proper to dendrimers, an additional one that is the visibility perceptible to human eyes. This new property was particularly interesting in relation to our research of new carriers for active entities and/or antibodies.
Amino-functionalized, second-generation dendritic building blocks
Klopsch, Rainer,Koch, Sabine,Schlueter, A. Dieter
, p. 1275 - 1283 (2007/10/03)
The multi-gram scale synthesis of first- and second-generation dendrons with Boc- and Cbz-protected amino groups in the periphery and methyl/ethyl esters at the focal points is described. Saponification of the esters and deprotection of the amines are shown to be strictly orthogonal processes which makes these dendrons valuable building blocks for future constructions.
